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Gene Symbol | PIK3CA | ||||||||||
Synonyms | CCM4 | CLAPO | CLOVE | CWS5 | HMH | MCAP | MCM | MCMTC | p110-alpha | PI3K | PI3K-alpha | ||||||||||
Gene Description | PIK3CA, phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha, activates PI3K/AKT/mTOR signaling to promote cell proliferation (PMID: 23411347, PMID: 31905960). PIK3CA activating mutations have been identified in a number of tumor types such as breast cancer (PMID: 32234362, PMID: 32404150), colon cancer (PMID: 32099598), endometrial cancer, glioblastoma, skin cancer, ovarian cancer (PMID: 20535651, PMID: 31892193), and mammary angiosarcoma (PMID: 32123305), and PIK3CA amplification has been observed in esophageal adenocarcinoma (PMID: 31865178). | ||||||||||
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Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
PIK3CA H1047R | breast cancer | sensitive | Trametinib | Preclinical | Actionable | In a preclinical study, Mekinist (trametinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA H1047R in culture (PMID: 26627007). | 26627007 |
PIK3CA H1047R | Advanced Solid Tumor | sensitive | Trametinib | Preclinical | Actionable | In a preclinical study, Mekinist (trametinib) inhibited survival of transformed cell lines overexpressing PIK3CA H1047R in culture (PMID: 26627007). | 26627007 |
PIK3CA H1047R | ovarian cancer | sensitive | A66 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, A66 delayed tumor growth in an ovarian cancer cell line xenograft model harboring PIK3CA H1047R (PMID: 21668414). | 21668414 |
PIK3CA H1047R | Advanced Solid Tumor | sensitive | A66 | Preclinical | Actionable | In a preclinical study, A66 delayed tumor growth in human tumor xenograft models harboring PIK3CA H1047R mutations (PMID: 21668414). | 21668414 |
PIK3CA H1047R | breast cancer | sensitive | Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, a breast cancer cell line harboring PIK3CA H1047R demonstrated sensitivity to treatment with Miransertib (ARQ092) in culture, resulting in inhibition of cell proliferation (PMID: 26469692). | 26469692 |
PIK3CA H1047R | breast cancer | sensitive | Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, Miransertib (ARQ092) treatment did not increase cell death but inhibited proliferation of breast cancer cells harboring PIK3CA H1047R in culture (PMID: 32439931). | 32439931 |
PIK3CA H1047R | stomach cancer | sensitive | Capivasertib | Preclinical - Pdx | Actionable | In a preclinical study, Truqap (capivasertib) inhibited growth in a patient-derived xenograft model of gastric cancer harboring a PIK3CA H1047R mutation (PMID: 24088382). | 24088382 |
PIK3CA H1047R | lung cancer | sensitive | Dactolisib | Preclinical | Actionable | In a preclinical study, BEZ235 reduced tumor size in mouse models of lung cancer carrying PIK3CA H1047R (PMID: 19029981). | 19029981 |
PIK3CA H1047R | breast cancer | sensitive | Dactolisib | Preclinical | Actionable | In a preclinical study, BEZ235 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA H1047R in culture (PMID: 26627007). | 26627007 |
PIK3CA H1047R | lung squamous cell carcinoma | sensitive | Dactolisib | Preclinical - Cell culture | Actionable | In a preclinical study, BEZ235 induced apoptosis, inhibited cell proliferation, migration, and invasion of lung squamous cell carcinoma cells over expressing PIK3CA H1047R in culture (PMID: 26013318). | 26013318 |
PIK3CA H1047R | lung adenocarcinoma | sensitive | Dactolisib | Preclinical | Actionable | In a preclinical study, BEZ235 promoted tumor regression in a mouse lung adenocarcinoma model expressing PIK3CA H1047R (PMID: 19029981). | 19029981 |
PIK3CA H1047R | urinary bladder cancer | sensitive | Dactolisib | Preclinical - Pdx | Actionable | In a preclinical study, BEZ235 inhibited tumor growth in a patient-derived xenograft (PDX) model of bladder cancer harboring PIK3CA H1047R (PMID: 26270481). | 26270481 |
PIK3CA H1047R | breast cancer | sensitive | Buparlisib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, a breast cancer cell line xenograft model harboring PIK3CA H1047R demonstrated tumor regression within the mammary fat pad when treated with Buparlisib (BKM120) (PMID: 28539475). | 28539475 |
PIK3CA H1047R | transitional cell carcinoma | no benefit | Buparlisib | Case Reports/Case Series | Actionable | In a Phase II trial, Buparlisib (BKM120) treatment resulted in progressive disease in a patient with metastatic urothelial carcinoma harboring PIK3CA H1047R (PMID: 32767682; NCT01551030). | 32767682 |
PIK3CA H1047R | lung squamous cell carcinoma | sensitive | Buparlisib | Preclinical - Cell culture | Actionable | In a preclinical study, Buparlisib (BKM120) induced apoptosis, inhibited cell proliferation, migration, and invasion of lung squamous cell carcinoma cells expressing PIK3CA H1047R in culture (PMID: 26013318). | 26013318 |
PIK3CA H1047R | endometrial cancer | predicted - sensitive | Alpelisib | Case Reports/Case Series | Actionable | In a clinical case study, Piqray (alpelisib) resulted in a partial response after 4 months in a patient with endometrial endometrioid cancer harboring PIK3CA H1047R, with treatment ongoing at 7 months (PMID: 36713525). | 36713525 |
PIK3CA H1047R | endometrial cancer | predicted - sensitive | Alpelisib | Case Reports/Case Series | Actionable | In a clinical study, Piqray (alpelisib) treatment was well tolerated and demonstrated activity in patients with advanced gynecologic cancer harboring activating mutations in PIK3CA and resulted in an overall response rate (ORR) of 28% (10/36), with an ORR of 35% (6/17, all partial responses) in endometrial cancer patients, including disease control in 7 of 9 patients harboring PIK3CA H1047R (PMID: 38518529; NCT04085653). | 38518529 |
PIK3CA H1047R | breast cancer | sensitive | Alpelisib | Preclinical | Actionable | In a preclinical study, Alpelisib (BYL719) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA H1047R in culture (PMID: 26627007). | 26627007 |
PIK3CA H1047R | breast cancer | sensitive | Alpelisib | Preclinical - Cell culture | Actionable | In a preclinical study, Piqray (alpelisib) inhibited growth of breast cancer organoids harboring PIK3CA H1047R in culture (PMID: 37272756). | 37272756 |
PIK3CA H1047R | lung squamous cell carcinoma | sensitive | Alpelisib | Preclinical - Cell culture | Actionable | In a preclinical study, Alpelisib (BYL719) induced apoptosis, inhibited cell proliferation, migration, and invasion of lung squamous cell carcinoma cells over expressing PIK3CA H1047R in culture (PMID: 26013318). | 26013318 |
PIK3CA H1047R | colorectal cancer | resistant | Alpelisib | Preclinical - Cell culture | Actionable | In a preclinical study, a colorectal cancer cell line harboring PIK3CA H1047R was resistant to Piqray (alpelisib) in culture (PMID: 37493631). | 37493631 |
PIK3CA H1047R | Advanced Solid Tumor | predicted - sensitive | Alpelisib | Preclinical - Cell culture | Actionable | In a preclinical study, Piqray (Alpelisib) decreased Akt phosphorylation and inhibited PI3K signaling, and demonstrated dose-dependent inhibition of survival in human pluripotent stem cells harboring PIK3CA H1047R in culture (PMID: 30948643). | 30948643 |
PIK3CA H1047R | head and neck squamous cell carcinoma | resistant | Cetuximab | Preclinical - Cell culture | Actionable | In a preclinical study, head and neck squamous cell carcinoma cells harboring PIK3CA H1047R were resistant to Erbitux (cetuximab) in culture (PMID: 30962319). | 30962319 |
PIK3CA H1047R | colorectal cancer | sensitive | Cetuximab | Case Reports/Case Series | Actionable | In a retrospective analysis, Erbitux (cetuximab) combined with radiation therapy resulted in stable disease for 6 months in a colorectal carcinoma patient harboring a PIK3CA H1047R mutation (PMID: 25714871). | 25714871 |
PIK3CA H1047R | estrogen-receptor positive breast cancer | predicted - sensitive | Everolimus | Clinical Study - Cohort | Actionable | In a retrospective analysis, combination of Afinitor (everolimus) and hormone therapy resulted in improved median progression-free survival (8.8 vs 4.1 months, p=0.02) in patients with hormone receptor-positive metastatic breast cancer harboring PIK3CA H1047R (n=6) compared to patients without PIK3CA H1047R (n=10) (PMID: 31088410). | 31088410 |
PIK3CA H1047R | progesterone-receptor positive breast cancer | predicted - sensitive | Everolimus | Clinical Study - Cohort | Actionable | In a retrospective analysis, combination of Afinitor (everolimus) and hormone therapy resulted in improved median progression-free survival (8.8 vs 4.1 months, p=0.02) in patients with hormone receptor-positive metastatic breast cancer harboring PIK3CA H1047R (n=6) compared to patients without PIK3CA H1047R (n=10) (PMID: 31088410). | 31088410 |
PIK3CA H1047R | Her2-receptor negative breast cancer | no benefit | Everolimus | Phase III | Actionable | In a retrospective analysis of a Phase III trial (BOLERO-2), Afinitor (everolimus) demonstrated comparable progression-free survival benefit in patients with hormone receptor-positive, Erbb2 (Her2)-negative breast cancer harboring wild-type (HR=0.43) or mutant (HR=0.37) PIK3CA, similar benefit was observed in subgroups harboring PIK3CA H1047R (HR=0.37) and PIK3CA E545K/E542K (HR=0.30) (PMID: 28183140; NCT00863655). | 28183140 |
PIK3CA H1047R | breast cancer | predicted - sensitive | Ipatasertib | Preclinical - Cell culture | Actionable | In a preclinical study, Ipatasertib (GDC-0068) treatment did not increase cell death but inhibited proliferation of breast cancer cells harboring PIK3CA H1047R in culture (PMID: 32439931). | 32439931 |
PIK3CA H1047R | colon cancer | no benefit | Pictilisib | Preclinical - Cell culture | Actionable | In a preclinical study, Pictilisib (GDC-0941) treatment did not affect cell viability in a colon cancer cell line expressing PIK3CA H1047R in culture (PMID: 34544753). | 34544753 |
PIK3CA H1047R | urinary bladder cancer | sensitive | Pictilisib | Preclinical - Pdx | Actionable | In a preclinical study, Pictilisib (GDC-0941) inhibited Akt phosphorylation and tumor growth, prolonged survival in patient-derived xenograft (PDX) models of bladder cancer harboring PIK3CA H1047R (PMID: 28808038). | 28808038 |
PIK3CA H1047R | breast cancer | sensitive | Lapatinib | Preclinical | Actionable | In a preclinical study, Tykerb (lapatinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA H1047R in culture (PMID: 26627007). | 26627007 |
PIK3CA H1047R | oral squamous cell carcinoma | decreased response | Ribociclib | Preclinical - Cell culture | Actionable | In a preclinical study, oral squamous cell carcinoma cells expressing PIK3CA H1047R demonstrated reduced sensitivity to Kisqali (ribociclib) treatment compared to cells expressing wild-type PIK3CA in culture (PMID: 31516747). | 31516747 |
PIK3CA H1047R | oral squamous cell carcinoma | decreased response | Abemaciclib | Preclinical - Cell culture | Actionable | In a preclinical study, oral squamous cell carcinoma cells expressing PIK3CA H1047R demonstrated reduced sensitivity to Verzenio (abemaciclib) treatment compared to cells expressing wild-type PIK3CA in culture (PMID: 31516747). | 31516747 |
PIK3CA H1047R | breast cancer | sensitive | MK2206 | Preclinical - Cell culture | Actionable | In a preclinical study, MK2206 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA H1047R in culture (PMID: 26627007). | 26627007 |
PIK3CA H1047R | breast cancer | sensitive | MK2206 | Preclinical - Cell culture | Actionable | In a preclinical study, MK2206 treatment did not increase cell death but inhibited proliferation of breast cancer cells harboring PIK3CA H1047R in culture (PMID: 32439931). | 32439931 |
PIK3CA H1047R | thyroid cancer | sensitive | MK2206 | Preclinical - Cell culture | Actionable | In a preclinical study, MK2206 inhibited AKT activation, proliferation, and growth of thyroid cancer cell lines with PI3K/AKT pathway alterations in culture, including an anaplastic thyroid cancer cell line harboring PIK3CA H1047R (PMID: 21289267). | 21289267 |
PIK3CA H1047R | breast cancer | sensitive | Neratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Nerlynx (neratinib) inhibited growth of breast cancer organoids harboring PIK3CA H1047R in culture (PMID: 37272756). | 37272756 |
PIK3CA H1047R | breast cancer | sensitive | Neratinib | Preclinical | Actionable | In a preclinical study, Nerlynx (neratinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA H1047R in culture (PMID: 26627007). | 26627007 |
PIK3CA H1047R | oral squamous cell carcinoma | resistant | Palbociclib | Preclinical - Cell culture | Actionable | In a preclinical study, oral squamous cell carcinoma cells expressing PIK3CA H1047R demonstrated resistance to Ibrance (palbociclib) treatment in culture (PMID: 31516747). | 31516747 |
PIK3CA H1047R | ovarian cancer | sensitive | PF-04691502 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, PF-04691502 inhibited Pi3k signaling, resulted in growth inhibition of ovarian cancer cells harboring PIK3CA H1047R in culture and in cell line xenograft models (PMID: 21750219). | 21750219 |
PIK3CA H1047R | colon cancer | sensitive | Pimasertib | Preclinical - Cell culture | Actionable | In a preclinical study, Pimasertib (MSC1936369B) inhibited viability of a colon cancer cell line expressing PIK3CA H1047R in culture (PMID: 27636997). | 27636997 |
PIK3CA H1047R | colon cancer | sensitive | Selumetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Koselugo (selumetinib) inhibited viability of a colon cancer cell line expressing PIK3CA H1047R in culture (PMID: 27636997). | 27636997 |
PIK3CA H1047R | lung cancer | no benefit | Sirolimus | Preclinical | Actionable | In a preclinical study, Sirolimus (rapamycin) did not induce tumor shrinkage in mouse lung cancer models carrying PIK3CA H1047R (PMID: 19029981). | 19029981 |
PIK3CA H1047R | lung adenocarcinoma | no benefit | Sirolimus | Preclinical | Actionable | In a preclinical study, Sirolimus (rapamycin) failed to inhibit tumor growth in a mouse lung adenocarcinoma model expressing the PIK3CA H1047R mutation (PMID: 19029981). | 19029981 |
PIK3CA H1047R | Advanced Solid Tumor | sensitive | Sirolimus | Preclinical | Actionable | In a preclinical study, transformed cells expressing PIK3CA H1047R were sensitive to Rapamune (sirolimus), resulting in inhibition of transformation in culture (PMID: 15647370). | 15647370 |
PIK3CA H1047R | ovarian cancer | predicted - sensitive | Temsirolimus | Case Reports/Case Series | Actionable | In a Phase II trial (TAPUR), Torisel (temsirolimus) treatment resulted in a partial response ongoing at 86 weeks in a patient with ovarian cancer harboring PIK3CA H1047R (J Clin Oncol 41, 2023 (suppl 16; abstr 3117); NCT02693535). | detail... |
PIK3CA H1047R | breast cancer | sensitive | BAY1125976 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, BAY1125976 inhibited proliferation of breast cancer cell lines harboring PIK3CA H1047R in culture, and inhibited AKT signaling and tumor growth in a PIK3CA H1047R-mutant cell line xenograft model (PMID: 27699769). | 27699769 |
PIK3CA H1047R | myxoid liposarcoma | predicted - sensitive | Copanlisib | Case Reports/Case Series | Actionable | In a Phase II trial (NCI MATCH EAY131-Z1F), Aliqopa (copanlisib) treatment resulted in a partial response and progression-free survival of 23.7 months and an overall survival of 25.8 months in a patient with myxoid liposarcoma harboring PIK3CA H1047R (PMID: 35133871; NCT02465060). | 35133871 |
PIK3CA H1047R | bone ameloblastoma | predicted - sensitive | Copanlisib | Case Reports/Case Series | Actionable | In a Phase II trial (NCI MATCH EAY131-Z1F), Aliqopa (copanlisib) treatment resulted in a partial response and progression-free survival of 24.6 months and an overall survival of 25.8 months in a patient with ameloblastoma of the mandible harboring PIK3CA H1047R (PMID: 35133871; NCT02465060). | 35133871 |
PIK3CA H1047R | colon cancer | sensitive | Taselisib | Preclinical - Cell culture | Actionable | In a preclinical study, Taselisib (GDC-0032) treatment led to decreased cell viability in a colon cancer cell line expressing PIK3CA H1047R in culture (PMID: 34544753). | 34544753 |
PIK3CA H1047R | breast cancer | sensitive | Taselisib | Phase I | Actionable | In a Phase I trial, four patients with breast cancer harboring PIK3CA H1047R demonstrated a confirmed partial response when treated with Taselisib (GDC-0032) (PMID: 28331003). | 28331003 |
PIK3CA H1047R | lung squamous cell carcinoma | no benefit | Taselisib | Case Reports/Case Series | Actionable | In a Phase I (SWOG S1400B) trial, Taselisib (GDC-0032) treatment did not meet primary endpoint in patients with lung squamous cell carcinoma harboring PIK3CA mutations, resulting in no responses in patients harboring PIK3CA H1047R (n=4) (PMID: 31158500; NCT02785913). | 31158500 |
PIK3CA H1047R | breast cancer | sensitive | Metformin | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Glucophage (metformin) inhibited cell proliferation of a dietary restriction-resistant PIK3CA H1047R-harboring human breast cancer cell line in culture, and inhibited tumor growth in xenograft models (PMID: 23986086). | 23986086 |
PIK3CA H1047R | colorectal cancer | sensitive | Metformin | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Glucophage (metformin) demonstrated efficacy in treating dietary restriction-resistant human colorectal cancer cell line xenograft tumors harboring PIK3CA H1047R (PMID: 23986086). | 23986086 |
PIK3CA H1047R | breast cancer | sensitive | M2698 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, a breast cancer xenograft model harboring PIK3CA H1047R was sensitive to M2698 (MSC2363318A), demonstrating inhibition of tumor growth (PMID: 27186432). | 27186432 |
PIK3CA H1047R | breast cancer | sensitive | Gedatolisib | Preclinical | Actionable | In a preclinical study, Gedatolisib (PKI-587) inhibited growth of human breast cancer cells harboring PIK3CA H1047R in culture (PMID: 21325073, PMID: 17314276). | 17314276 21325073 |
PIK3CA H1047R | head and neck squamous cell carcinoma | sensitive | Gedatolisib | Preclinical - Cell culture | Actionable | In a preclinical study, head and neck squamous cell carcinoma cell lines harboring PIK3CA H1047R demonstrated sensitivity to treatment with Gedatolisib (PF-05212384) in culture (PMID: 25977343). | 25977343 |
PIK3CA H1047R | Advanced Solid Tumor | sensitive | Rigosertib Sodium | Preclinical - Cell culture | Actionable | In a preclinical study, Rigosertib (ON 01910.Na) inhibited oncogenic transformation in fibroblast cells over-expressing Pik3ca H1047R in culture (PMID: 27104980). | 27104980 |
PIK3CA H1047R | estrogen-receptor positive breast cancer | predicted - sensitive | Alpelisib + Everolimus | Preclinical - Patient cell culture | Actionable | In a preclinical study, combination treatment with Piqray (albelisib) and Afinitor (everolimus) synergistically inhibited cell viability of patient-derived ESR1 (ER)-positive breast cancer cells harboring PIK3CA H1047R and ESR1 (ER alpha) Y537S in culture (PMID: 36900375). | 36900375 |
PIK3CA H1047R | breast metaplastic carcinoma | predicted - sensitive | Buparlisib + Paclitaxel | Case Reports/Case Series | Actionable | In a clinical case study, Buparlisib (BKM120) in combination with Taxol (paclitaxel) resulted in a durable partial response in a patient with breast metaplastic carcinoma harboring PIK3CA H1047R, with a total response period of 70 weeks and an overall survival of 42 months (PMID: 30577988). | 30577988 |
PIK3CA H1047R | urinary bladder cancer | sensitive | Cisplatin + Pictilisib | Preclinical - Pdx | Actionable | In a preclinical study, combination of or sequential treatment with Pictilisib (GDC-0941) and Platinol (cisplatin) significantly delayed tumor growth and prolonged survival in patient-derived xenograft (PDX) models of bladder cancer harboring PIK3CA H1047R (PMID: 28808038). | 28808038 |
PIK3CA H1047R | colorectal cancer | resistant | Cetuximab + Fluorouracil | Preclinical - Cell culture | Actionable | In a preclinical study, colorectal cancer cells over expressing PIK3CA H1047R were resistant to Erbitux (cetuximab) and Fluorouracil combination treatment in culture (PMID: 28424201). | 28424201 |
PIK3CA H1047R | ovarian cancer | sensitive | AZD8835 | Preclinical | Actionable | In a preclinical study, AZD8835 inhibited tumor growth in mouse xenografts of ovarian cancer with a Pik3ca H1047R mutation (AACR; Cancer Res 2015;75(15 Suppl):Abstract nr 2830). | detail... |
PIK3CA H1047R | head and neck squamous cell carcinoma | predicted - sensitive | Sulindac | Preclinical - Cell culture | Actionable | In a preclinical study, head and neck squamous cell carcinoma cell lines harboring PIK3CA H1047R demonstrated increased sensitivity to Clinoril (sulindac) compared to cell lines with wild-type PIK3CA, resulting in decreased proliferation in culture (PMID: 30683736). | 30683736 |
PIK3CA H1047R | breast cancer | sensitive | MEN1611 | Preclinical | Actionable | In a preclinical study, MEN1611 (CH5132799) inhibited proliferation of breast cancer cells harboring PIK3CA H1047R in culture (PMID: 21558396). | 21558396 |
PIK3CA H1047R | breast cancer | sensitive | MEN1611 | Preclinical - Cell culture | Actionable | In a preclinical study, MEN1611 (CH5132799) inhibited viability and induced degradation of p110alpha in breast cancer cell lines harboring PIK3CA H1047R in culture (PMID: 36913051). | 36913051 |
PIK3CA H1047R | ovarian cancer | predicted - sensitive | MEN1611 | Case Reports/Case Series | Actionable | In a Phase I trial, MEN1611 (CH5132799) demonstrated safety and preliminary efficacy in patients with advanced solid tumors, including a partial response in a patient with ovarian cancer harboring PIK3CA H1047R (PMID: 25231405). | 25231405 |
PIK3CA H1047R | breast cancer | predicted - sensitive | GSK690693 | Preclinical - Cell culture | Actionable | In a preclinical study, GSK690693 treatment did not increase cell death but inhibited proliferation of breast cancer cells harboring PIK3CA H1047R in culture (PMID: 32439931). | 32439931 |
PIK3CA H1047R | head and neck squamous cell carcinoma | sensitive | Sirolimus + Trametinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Rapamune (sirolimus) worked synergistically with Mekinist (trametinib) to inhibit proliferation of head and neck squamous carcinoma cell lines harboring PIK3CA H1047R in culture and to reduce tumor growth in cell line xenograft models (PMID: 26882569). | 26882569 |
PIK3CA H1047R | head and neck squamous cell carcinoma | sensitive | Radiotherapy + Taselisib | Preclinical | Actionable | In a preclinical study, Taselisib (GDC-0032) enhanced the effects of radiation induced apoptosis of head and neck squamous carcinoma cells harboring PIK3CA H1047R (PMID: 26589432). | 26589432 |
PIK3CA H1047R | breast cancer | sensitive | ARQ 751 | Preclinical - Cell culture | Actionable | In a preclinical study, a breast cancer cell line harboring PIK3CA H1047R demonstrated sensitivity to treatment with ARQ 751 in culture, resulting in inhibition of cell proliferation (PMID: 26469692). | 26469692 |
PIK3CA H1047R | breast cancer | sensitive | ARQ 751 | Preclinical - Cell culture | Actionable | In a preclinical study, ARQ 751 treatment did not increase cell death but inhibited proliferation of breast cancer cells harboring PIK3CA H1047R in culture (PMID: 32439931). | 32439931 |
PIK3CA H1047R | high grade glioma | sensitive | Buparlisib + Selumetinib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination therapy of Buparlisib (BKM120) and Koselugo (selumetinib) led to a synergistic effect, resulting in growth inhibition of astrocytoma cells expressing PIK3CA H1047R, but did not result in an effect as high as that seen in cells expressing PIK3CA R88Q or PIK3CA E542K in culture (PMID: 29975751). | 29975751 |
PIK3CA H1047R | thyroid cancer | sensitive | MK2206 + Temsirolimus | Preclinical - Cell culture | Actionable | In a preclinical study, MK2206 and Torisel (temsirolimus) demonstrated synergy in inhibiting growth of an anaplastic thyroid cancer cell line harboring PIK3CA H1047R in culture (PMID: 21289267). | 21289267 |
PIK3CA H1047R | colon cancer | sensitive | Inavolisib | Preclinical - Cell culture | Actionable | In a preclinical study, Itovebi (inavolisib) treatment led to decreased cell viability in a colon cancer cell line expressing PIK3CA H1047R in culture (PMID: 34544753). | 34544753 |
PIK3CA H1047R | breast cancer | sensitive | DHM25 | Preclinical - Cell culture | Actionable | In a preclinical study, DHM25 increased cell death in breast cancer cell lines harboring PIK3CA H1047R in culture (PMID: 26237138). | 26237138 |
PIK3CA H1047R | head and neck squamous cell carcinoma | predicted - sensitive | SHR-A1307 | Preclinical - Cell culture | Actionable | In a preclinical study, head and neck squamous cell carcinoma cells harboring PIK3CA H1047R treated with SHR-A1307 demonstrated inhibition of cell growth in culture (PMID: 30962319). | 30962319 |
PIK3CA H1047R | breast cancer | sensitive | CYH33 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, CYH33 inhibited proliferation of breast cancer cell lines harboring PIK3CA H1047R in culture, inhibited tumor progression in a transgenic mouse model, and induced cell cycle arrest, and inhibited PI3K signaling and tumor growth in cell line xenograft models (PMID: 30003928). | 30003928 |
PIK3CA H1047R | breast cancer | sensitive | Borussertib | Preclinical - Cell culture | Actionable | In a preclinical study, borussertib inhibited proliferation of a breast cancer cell line harboring PIK3CA H1047R in culture (PMID: 30858154). | 30858154 |
PIK3CA H1047R | head and neck squamous cell carcinoma | sensitive | Alpelisib + Tipifarnib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination of Piqray (alpelisib) and Zarnestra (tipifarnib) inhibited Mtor and Rsk phosphorylation, induced cell cycle arrest and apoptosis, and synergistically inhibited viability of head and neck cancer squamous cell carcinoma cell lines harboring PIK3CA H1047R in culture and inhibited Mtor signaling, induced cell cycle arrest and apoptosis, inhibited proliferation, and induced tumor regression in a cell line xenograft model (PMID: 37339176). | 37339176 |
PIK3CA H1047R | colon cancer | sensitive | T-2143 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, T-2143 treatment inhibited Akt phosphorylation and proliferation of colon cancer cells harboring PIK3CA H1047R in culture, and inhibited tumor growth in a cell line xenograft model (PMID: 32499300). | 32499300 |
PIK3CA H1047R | breast cancer | predicted - sensitive | TAS-117 | Case Reports/Case Series | Actionable | In a Phase II trial, TAS-117 treatment in a breast cancer patient harboring PIK3CA H1047R led to initial stable disease, however, disease progression was observed at 12 weeks after treatment along with an increase of non-target lesions, following which treatment was discontinued (PMID: 33723724; NCT03017521). | 33723724 |
PIK3CA H1047R | breast cancer | sensitive | RLY-2608 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, RLY-2608 inhibited viability of hormone receptor-positive breast cancer cells harboring PIK3CA H1047R in culture, and inhibited tumor growth in a cell line xenograft model (PMID: 37916956). | 37916956 |
PIK3CA H1047R | breast cancer | predicted - sensitive | LOXO-783 | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, LOXO-783 (LOX-22783) treatment led to growth inhibition in breast cancer cell lines harboring PIK3CA H1047R, and led to tumor regression in cell line xenograft and patient-derived xenograft (PDX) models (Mol Cancer Ther 2021;20(12 Suppl):Abstract nr P142). | detail... |
PIK3CA H1047R | estrogen-receptor positive breast cancer | predicted - sensitive | Afatinib + Alpelisib | Preclinical - Patient cell culture | Actionable | In a preclinical study, combination treatment with Piqray (albelisib) and Gilotrif (afatinib) synergistically inhibited cell viability of patient-derived ESR1 (ER)-positive breast cancer cells harboring PIK3CA H1047R and ESR1 (ER alpha) Y537S in culture (PMID: 36900375). | 36900375 |
PIK3CA H1047R | head and neck squamous cell carcinoma | sensitive | STX-478 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, STX-478 inhibited viability in head and neck squamous cell cancer cell lines harboring PIK3CA H1047R in culture, and inhibited tumor growth and induced tumor regression in a cell line xenograft model (PMID: 37623743). | 37623743 |
PIK3CA H1047R | Her2-receptor positive breast cancer | sensitive | STX-478 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, STX-478 inhibited viability in a hormone receptor-negative, ERBB2 (HER2)-positive breast cancer cell line harboring PIK3CA H1047R in culture, and inhibited tumor growth in a cell line xenograft model (PMID: 37623743). | 37623743 |
PIK3CA H1047R | Her2-receptor negative breast cancer | sensitive | STX-478 | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, STX-478 inhibited viability in an ESR1-positive, ERBB2 (HER2)-negative breast cancer cell line harboring PIK3CA H1047R in culture and inhibited tumor growth and induced tumor regression with high-dose STX-478 in a cell line xenograft model and inhibited tumor growth in a patient-derived xenograft (PDX) model (PMID: 37623743). | 37623743 |
PIK3CA H1047R | Her2-receptor negative breast cancer | predicted - sensitive | HS-10352 | Case Reports/Case Series | Actionable | In a Phase I trial, HS-10352 treatment resulted in an objective response rate (ORR) of 27.8% (5/18, all partial responses), disease control rate (DCR) of 55.6%, and median progression-free survival (mPFS) of 3.9 mo in HR-positive, ERBB2 (HER2)-negative advanced breast cancer patients overall, and in the 6mg group led to an ORR of 66.7% and DCR of 83.3%, with an ORR of 75.0% (3/4) and DCR of 100% in patients with PIK3CA mutations (E542K, E545K, E545D, H1047L, H1047R) (PMID: 38037839; NCT04631835). | 38037839 |
PIK3CA H1047R | Advanced Solid Tumor | predicted - sensitive | OKI-219 | Preclinical - Pdx | Actionable | In a preclinical study, OKI-219 decreased Akt phosphorylation and proliferation in tumor cell lines harboring PIK3CA H1047R in culture and inhibited tumor growth in cell line xenograft models and patient-derived xenograft (PDX) models (Mol Cancer Ther (2023) 22 (12_Supplement): B163). | detail... |
PIK3CA H1047R | Her2-receptor positive breast cancer | sensitive | ZM-PI05 | Preclinical - Cell culture | Actionable | In a preclinical study, ZM-PI05 induced cell cycle arrest and decreased viability of ERBB2 (HER2)-positive breast cancer cell lines harboring PIK3CA H1047R in culture (PMID: 38986734). | 38986734 |
PIK3CA P539R PIK3CA H1047R | breast cancer | sensitive | Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, breast cancer cells harboring PIK3CA P539R and H1047R were sensitive to Miransertib (ARQ092) in culture, demonstrating inhibition of cell growth (PMID: 26469692). | 26469692 |
PIK3CA P539R PIK3CA H1047R | breast cancer | sensitive | PF-04691502 | Preclinical - Cell culture | Actionable | In a preclinical study, PF-04691502 inhibited Akt phosphorylation and proliferation of breast cancer cells harboring both PIK3CA P539R and H1047R in culture (PMID: 21750219). | 21750219 |
PIK3CA P539R PIK3CA H1047R | breast cancer | sensitive | ARQ 751 | Preclinical - Cell culture | Actionable | In a preclinical study, ARQ 751 inhibited cell growth in a breast cancer cell line harboring PIK3CA P539R and H1047R in culture (PMID: 26469692). | 26469692 |
PIK3CA P539R PIK3CA H1047R | Advanced Solid Tumor | sensitive | STX-478 | Preclinical - Cell culture | Actionable | In a preclinical study, STX-478 inhibited viability of a cell line harboring PIK3CA H1047R and P539R in culture (PMID: 37623743). | 37623743 |
BRAF V600E PIK3CA H1047R | colorectal cancer | resistant | Vemurafenib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Zelboraf (vemurafenib) treatment did not inhibit proliferation of colorectal cancer cells harboring BRAF V600E and PIK3CA H1047R in culture, and did not inhibit tumor growth in a cell line xenograft model (PMID: 22180495). | 22180495 |
BRAF V600E PIK3CA H1047R | thyroid gland carcinoma | resistant | Everolimus | Case Reports/Case Series | Actionable | In a clinical case study, a patient with anaplastic thyroid carcinoma co-harboring BRAF V600E and PIK3CA H1047R demonstrated resistance to treatment with Afinitor (everolimus) (PMID: 27797976). | 27797976 |
BRAF V600E PIK3CA H1047R | colorectal cancer | predicted - sensitive | MK2206 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, MK2206 treatment resulted in a modest tumor growth inhibition in a cell line xenograft model of colorectal cancer harboring BRAF V600E and PIK3CA H1047R (PMID: 22180495). | 22180495 |
BRAF V600E PIK3CA H1047R | thyroid gland carcinoma | resistant | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, a patient with anaplastic thyroid carcinoma co-harboring BRAF V600E and PIK3CA H1047R demonstrated resistance to the combination therapy, Mekinist (trametinib) and Tafinlar (dabrafenib) (PMID: 27797976). | 27797976 |
BRAF V600E PIK3CA H1047R | anaplastic thyroid carcinoma | sensitive | Dasatinib + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Sprycel (dasatinib) and Mekinist (trametinib) inhibited viability of an anaplastic thyroid cancer cell line harboring BRAF V600E and PIK3CA H1047R in culture (PMID: 37713162). | 37713162 |
BRAF V600E PIK3CA H1047R | colorectal cancer | sensitive | MK2206 + Vemurafenib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Zelboraf (vemurafenib) treatment in combination with MK2206 induced apoptosis and synergistically inhibited proliferation of colorectal cancer cells harboring BRAF V600E and PIK3CA H1047R in culture, and inhibited tumor growth in a cell line xenograft model (PMID: 22180495). | 22180495 |
BRAF V600E PIK3CA H1047R | thyroid gland carcinoma | predicted - sensitive | Dabrafenib + Everolimus + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, a patient with anaplastic thyroid carcinoma co-harboring BRAF V600E and PIK3CA H1047R demonstrated tumor regression when treated with the triple combination, Tafinlar (dabrafenib), Mekinist (trametinib), and Afinitor (everolimus) (PMID: 27797976). | 27797976 |
BRAF V600E PIK3CA H1047R TP53 wild-type | colorectal cancer | sensitive | PD-0325901 + Sapanisertib | Preclinical - Cell culture | Actionable | In a preclinical study, Sapanisertib (MLN0128) and PD-0325901 synergistically inhibited Erk and PI3K signaling and proliferation, induced apoptosis in TP53-wild-type colorectal cancer cells harboring BRAF V600E and PIK3CA H1047R in culture (PMID: 26272063). | 26272063 |
PIK3CA H1047R PTEN E307K | breast cancer | sensitive | BAY1125976 | Preclinical - Cell culture | Actionable | In a preclinical study, BAY1125976 inhibited proliferation of a breast cancer cell line harboring PIK3CA H1047R and PTEN E307K in culture (PMID: 27699769). | 27699769 |
PIK3CA H1047R PTEN loss | breast cancer | sensitive | Taselisib | Preclinical - Cell culture | Actionable | In a preclinical study, a breast cancer cell line harboring a PIK3CA H1047R and PTEN loss was sensitive to treatment with Taselisib (GDC-0032) in culture, demonstrating decreased cell viability (PMID: 31534012). | 31534012 |
PIK3CA H1047R PTEN loss | breast cancer | no benefit | Dactolisib + Venetoclax | Preclinical - Cell culture | Actionable | In a preclinical study, inhibition of Pi3k signaling by BEZ235 did not sensitize breast cancer cell lines harboring PIK3CA H1047R and PTEN loss to Venclexta (venetoclax) in culture (PMID: 27974663). | 27974663 |
PIK3CA H1047R PTEN loss | breast cancer | predicted - sensitive | Dactolisib + WEHI-539 | Preclinical - Cell culture | Actionable | In a preclinical study, inhibition of Pi3k signaling by BEZ235 sensitized breast cancer cell lines harboring PIK3CA H1047R and PTEN loss to WEHI-539 in culture (PMID: 27974663). | 27974663 |
PIK3CA H1047R PTEN loss | triple-receptor negative breast cancer | predicted - sensitive | ABT-737 + Dactolisib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, ABT-737 and BEZ235 combination treatment resulted in tumor regression in cell line xenograft models of triple-receptor negative breast cancer harboring PIK3CA H1047R and PTEN loss (PMID: 27974663). | 27974663 |
PIK3CA H1047R PTEN loss | triple-receptor negative breast cancer | predicted - sensitive | ABT-737 + Sapanisertib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, ABT-737 and Sapanisertib (MLN0128) combination treatment resulted in inhibition of tumor growth in cell line xenograft models of triple-receptor negative breast cancer harboring PIK3CA H1047R and PTEN loss (PMID: 27974663). | 27974663 |
PIK3CA H1047R PTEN loss | breast cancer | predicted - sensitive | CYH33 | Preclinical - Cell culture | Actionable | In a preclinical study, CYH33 inhibited proliferation of a breast cancer cell line harboring PIK3CA H1047R and PTEN loss in culture (PMID: 30003928). | 30003928 |
PIK3CA H1047R TP53 S90fs | ovarian clear cell adenocarcinoma | decreased response | DS-7423 | Preclinical - Cell culture | Actionable | In a preclinical study, an ovarian clear cell adenocarcinoma cell line harboring PIK3CA H1047R and TP53 S90fs*33 demonstrated reduced sensitivity to DS-7423 in culture (PMID: 24504419). | 24504419 |
NRAS mut PIK3CA H1047R | melanoma | predicted - resistant | Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, one of two NRAS-mutant melanoma cell lines expressing PIK3CA H1047R demonstrated resistance to treatment with Mekinist (trametinib) in culture (PMID: 30819666). | 30819666 |
PIK3CA E726K PIK3CA H1047R | breast cancer | resistant | Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA E726K was resistant to Miransertib (ARQ092) in culture (PMID: 37916958). | 37916958 |
PIK3CA E726K PIK3CA H1047R | breast cancer | sensitive | Alpelisib | Preclinical - Cell culture | Actionable | In a preclinical study, breast epithelial cells expressing PIK3CA E726K and PIK3CA H1047R in cis demonstrated increased sensitivity to growth inhibition by Piqray (Alpelisib) treatment compared to cells expressing individual PIK3CA mutations in culture, while cells expressing PIK3CA E726K and PIK3CA H1047R in trans did not (PMID: 31699932). | 31699932 |
PIK3CA E726K PIK3CA H1047R | breast cancer | sensitive | Alpelisib | Preclinical - Biochemical | Actionable | In a preclinical study, Piqray (alpelisib) decreased viability of a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA E726K in culture (PMID: 37916958). | 37916958 |
PIK3CA E726K PIK3CA H1047R | breast cancer | sensitive | Everolimus | Preclinical - Cell culture | Actionable | In a preclinical study, breast epithelial cells expressing PIK3CA E726K and PIK3CA H1047R in cis demonstrated increased sensitivity to growth inhibition by Afinitor (everolimus) treatment compared to cells expressing individual PIK3CA mutations in culture (PMID: 31699932). | 31699932 |
PIK3CA E726K PIK3CA H1047R | breast cancer | sensitive | Ipatasertib | Preclinical - Cell culture | Actionable | In a preclinical study, Ipatasertib (GDC-0068) decreased viability of a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA E726K in culture (PMID: 37916958). | 37916958 |
PIK3CA E726K PIK3CA H1047R | breast cancer | resistant | Pictilisib | Preclinical - Cell culture | Actionable | In a preclinical study, a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA E726K was resistant to Pictilisib (GDC-0941) in culture (PMID: 37916958). | 37916958 |
PIK3CA E726K PIK3CA H1047R | breast cancer | sensitive | Taselisib | Preclinical - Cell culture | Actionable | In a preclinical study, Taselisib (GDC-0032) decreased viability of a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA E726K in culture (PMID: 37916958). | 37916958 |
PIK3CA E726K PIK3CA H1047R | breast cancer | sensitive | Inavolisib | Preclinical - Cell culture | Actionable | In a preclinical study, breast epithelial cells expressing PIK3CA E726K and PIK3CA H1047R in cis demonstrated increased sensitivity to growth inhibition by Itovebi (inavolisib) treatment compared to cells expressing individual PIK3CA mutations in culture (PMID: 31699932). | 31699932 |
PIK3CA E726K PIK3CA H1047R | breast cancer | sensitive | Inavolisib | Preclinical - Cell culture | Actionable | In a preclinical study, Itovebi (inavolisib) decreased viability of a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA E726K in culture (PMID: 37916958). | 37916958 |
PIK3CA E726K PIK3CA H1047R | breast cancer | resistant | RLY-2608 | Preclinical - Cell culture | Actionable | In a preclinical study, a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA E726K was resistant to RLY-2608 treatment in culture (PMID: 37916958). | 37916958 |
PIK3CA E453Q PIK3CA H1047R | breast cancer | sensitive | Alpelisib | Preclinical - Cell culture | Actionable | In a preclinical study, breast epithelial cells expressing PIK3CA E453Q and PIK3CA H1047R in cis demonstrated increased sensitivity to growth inhibition by Piqray (Alpelisib) treatment compared to cells expressing individual PIK3CA mutations in culture (PMID: 31699932). | 31699932 |
PIK3CA E453Q PIK3CA H1047R | breast cancer | sensitive | Everolimus | Preclinical - Cell culture | Actionable | In a preclinical study, breast epithelial cells expressing PIK3CA E453Q and PIK3CA H1047R in cis demonstrated increased sensitivity to growth inhibition by Afinitor (everolimus) treatment compared to cells expressing individual PIK3CA mutations in culture (PMID: 31699932). | 31699932 |
PIK3CA E453Q PIK3CA H1047R | breast cancer | sensitive | Inavolisib | Preclinical - Cell culture | Actionable | In a preclinical study, breast epithelial cells expressing PIK3CA E453Q and PIK3CA H1047R in cis demonstrated increased sensitivity to growth inhibition by Itovebi (inavolisib) treatment compared to cells expressing individual PIK3CA mutations in culture (PMID: 31699932). | 31699932 |
PIK3CA Q1033R PIK3CA H1047R | Burkitt lymphoma | predicted - sensitive | Idelalisib | Case Reports/Case Series | Actionable | In a clinical case study, Zydelig (idelalisib) treatment resulted in tumor shrinkage and decreased plasma LDH that continued for 10 months before recurrence in a patient with relapsed Burkitt lymphoma harboring PIK3CA H1047R and PIK3CA Q1033R (PMID: 32193631). | 32193631 |
BRAF V600E PIK3CA H1047R PTEN Y68fs | melanoma | predicted - resistant | Vemurafenib | Case Reports/Case Series | Actionable | In a clinical study, a melanoma patient harboring BRAF V600E and PTEN Y68fs treated with Zelboraf (vemurafenib) was found to have acquired PIK3CA H1047R in the post-progression tumor biopsy (PMID: 24265153). | 24265153 |
HRAS G13R PIK3CA H1047R | Advanced Solid Tumor | resistant | Alpelisib | Preclinical - Cell culture | Actionable | In a preclinical study, HRAS-null, NRAS-null, and KRAS knockout cells expressing HRAS G13R and PIK3CA H1047R were resistant to Piqray (alpelisib) in culture (PMID: 39152269). | 39152269 |
HRAS G13R PIK3CA H1047R | Advanced Solid Tumor | resistant | Pictilisib | Preclinical - Cell culture | Actionable | In a preclinical study, HRAS-null, NRAS-null, and KRAS knockout cells expressing HRAS G13R and PIK3CA H1047R were resistant to Pictilisib (GDC-0941) in culture (PMID: 39152269). | 39152269 |
HRAS G13R PIK3CA H1047R | Advanced Solid Tumor | resistant | Tipifarnib | Preclinical - Cell culture | Actionable | In a preclinical study, HRAS-null, NRAS-null, and KRAS knockout cells expressing HRAS G13R and PIK3CA H1047R were resistant to Zarnestra (tipifarnib) in culture (PMID: 39152269). | 39152269 |
NRAS G13R PIK3CA H1047R | rhabdomyosarcoma | resistant | Ganitumab + Trametinib | Preclinical - Pdx | Actionable | In a preclinical study, a patient-derived xenograft (PDX) model of rhabdomyosarcoma harboring NRAS G13R and PIK3CA H1047R was resistant to the Mekinist (trametinib) and Ganitumab (AMG-479) combination treatment (PMID: 36322002). | 36322002 |
ALK F1174L PIK3CA H1047R | neuroblastoma | predicted - resistant | Lorlatinib | Case Reports/Case Series | Actionable | In a Phase I trial, a neuroblastoma patient harboring ALK F1174L developed progressive disease on treatment with Lorbrena (lorlatinib) and was found to have acquired PIK3CA H1047R via circulating tumor DNA (PMID: 37147298; NCT03107988). | 37147298 |
PIK3CA D350N PIK3CA H1047R | Advanced Solid Tumor | sensitive | STX-478 | Preclinical - Cell culture | Actionable | In a preclinical study, STX-478 inhibited viability of a cell line harboring PIK3CA H1047R and D350N in culture (PMID: 37623743). | 37623743 |
PIK3CA K111R PIK3CA H1047R | lung carcinoma | sensitive | STX-478 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, STX-478 inhibited viability in a lung carcinoma cell line harboring PIK3CA H1047R and K111R in culture, and inhibited tumor growth in a cell line xenograft model (PMID: 37623743). | 37623743 |
PIK3CA W780R PIK3CA H1047R | breast cancer | sensitive | Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, Miransertib (ARQ092) decreased viability of a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA W780R in culture (PMID: 37916958). | 37916958 |
PIK3CA W780R PIK3CA H1047R | breast cancer | resistant | Alpelisib | Preclinical - Cell culture | Actionable | In a preclinical study, a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA W780R was resistant to Piqray (alpelisib) in culture (PMID: 37916958). | 37916958 |
PIK3CA W780R PIK3CA H1047R | breast cancer | sensitive | Ipatasertib | Preclinical - Cell culture | Actionable | In a preclinical study, Ipatasertib (GDC-0068) decreased viability of a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA W780R in culture (PMID: 37916958). | 37916958 |
PIK3CA W780R PIK3CA H1047R | breast cancer | resistant | Pictilisib | Preclinical - Cell culture | Actionable | In a preclinical study, a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA W780R was resistant to Pictilisib (GDC-0941) in culture (PMID: 37916958). | 37916958 |
PIK3CA W780R PIK3CA H1047R | breast cancer | resistant | Taselisib | Preclinical - Cell culture | Actionable | In a preclinical study, a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA W780R was resistant to Taselisib (GDC-0032) in culture (PMID: 37916958). | 37916958 |
PIK3CA W780R PIK3CA H1047R | breast cancer | resistant | Inavolisib | Preclinical - Cell culture | Actionable | In a preclinical study, a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA W780R was resistant to Itovebi (inavolisib) in culture (PMID: 37916958). | 37916958 |
PIK3CA W780R PIK3CA H1047R | breast cancer | sensitive | RLY-2608 | Preclinical - Cell culture | Actionable | In a preclinical study, RLY-2608 inhibited downstream signaling and viability in a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA W780R in culture (PMID: 37916958). | 37916958 |
PIK3CA Q859H PIK3CA H1047R | breast cancer | sensitive | Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, Miransertib (ARQ092) decreased viability of a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA Q859H in culture (PMID: 37916958). | 37916958 |
PIK3CA Q859H PIK3CA H1047R | breast cancer | resistant | Alpelisib | Preclinical - Cell culture | Actionable | In a preclinical study, a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA Q859H was resistant to Piqray (alpelisib) in culture (PMID: 37916958). | 37916958 |
PIK3CA Q859H PIK3CA H1047R | breast cancer | sensitive | Ipatasertib | Preclinical - Cell culture | Actionable | In a preclinical study, Ipatasertib (GDC-0068) decreased viability of a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA Q859H in culture (PMID: 37916958). | 37916958 |
PIK3CA Q859H PIK3CA H1047R | breast cancer | sensitive | Pictilisib | Preclinical - Cell culture | Actionable | In a preclinical study, Pictilisib (GDC-0941) decreased viability of a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA Q859H in culture (PMID: 37916958). | 37916958 |
PIK3CA Q859H PIK3CA H1047R | breast cancer | resistant | Taselisib | Preclinical - Cell culture | Actionable | In a preclinical study, a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA Q859H was resistant to Taselisib (GDC-0032) in culture (PMID: 37916958). | 37916958 |
PIK3CA Q859H PIK3CA H1047R | breast cancer | resistant | Inavolisib | Preclinical - Cell culture | Actionable | In a preclinical study, a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA Q859H was resistant to Itovebi (inavolisib) in culture (PMID: 37916958). | 37916958 |
PIK3CA Q859H PIK3CA H1047R | breast cancer | sensitive | RLY-2608 | Preclinical - Cell culture | Actionable | In a preclinical study, RLY-2608 inhibited downstream signaling and viability in a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA Q859H in culture (PMID: 37916958). | 37916958 |
PIK3CA Q859K PIK3CA H1047R | breast cancer | sensitive | Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, Miransertib (ARQ092) decreased viability of a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA Q859K in culture (PMID: 37916958). | 37916958 |
PIK3CA Q859K PIK3CA H1047R | breast cancer | resistant | Alpelisib | Preclinical - Cell culture | Actionable | In a preclinical study, a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA Q859K was resistant to Piqray (alpelisib) in culture (PMID: 37916958). | 37916958 |
PIK3CA Q859K PIK3CA H1047R | breast cancer | sensitive | Ipatasertib | Preclinical - Cell culture | Actionable | In a preclinical study, Ipatasertib (GDC-0068) decreased viability of a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA Q859K in culture (PMID: 37916958). | 37916958 |
PIK3CA Q859K PIK3CA H1047R | breast cancer | sensitive | Pictilisib | Preclinical - Cell culture | Actionable | In a preclinical study, Pictilisib (GDC-0941) decreased viability of a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA Q859K in culture (PMID: 37916958). | 37916958 |
PIK3CA Q859K PIK3CA H1047R | breast cancer | resistant | Taselisib | Preclinical - Cell culture | Actionable | In a preclinical study, a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA Q859K was resistant to Taselisib (GDC-0032) in culture (PMID: 37916958). | 37916958 |
PIK3CA Q859K PIK3CA H1047R | breast cancer | resistant | Inavolisib | Preclinical - Cell culture | Actionable | In a preclinical study, a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA Q859K was resistant to Itovebi (inavolisib) in culture (PMID: 37916958). | 37916958 |
PIK3CA Q859K PIK3CA H1047R | breast cancer | sensitive | RLY-2608 | Preclinical - Cell culture | Actionable | In a preclinical study, RLY-2608 inhibited downstream signaling and viability in a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA Q859K in culture (PMID: 37916958). | 37916958 |
PIK3CA I817F PIK3CA H1047R | breast cancer | sensitive | Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, Miransertib (ARQ092) decreased viability of a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA I817F in culture (PMID: 37916958). | 37916958 |
PIK3CA I817F PIK3CA H1047R | breast cancer | sensitive | Alpelisib | Preclinical - Cell culture | Actionable | In a preclinical study, Piqray (alpelisib) decreased viability of a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA I817F in culture (PMID: 37916958). | 37916958 |
PIK3CA I817F PIK3CA H1047R | breast cancer | sensitive | Ipatasertib | Preclinical - Cell culture | Actionable | In a preclinical study, Ipatasertib (GDC-0068) decreased viability of a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA I817F in culture (PMID: 37916958). | 37916958 |
PIK3CA I817F PIK3CA H1047R | breast cancer | sensitive | Pictilisib | Preclinical - Cell culture | Actionable | In a preclinical study, Pictilisib (GDC-0941) decreased viability of a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA I817F in culture (PMID: 37916958). | 37916958 |
PIK3CA I817F PIK3CA H1047R | breast cancer | sensitive | Taselisib | Preclinical - Cell culture | Actionable | In a preclinical study, Taselisib (GDC-0032) decreased viability of a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA I817F in culture (PMID: 37916958). | 37916958 |
PIK3CA I817F PIK3CA H1047R | breast cancer | sensitive | Inavolisib | Preclinical - Cell culture | Actionable | In a preclinical study, Itovebi (inavolisib) decreased viability of a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA I817F in culture (PMID: 37916958). | 37916958 |
PIK3CA I817F PIK3CA H1047R | breast cancer | sensitive | RLY-2608 | Preclinical - Cell culture | Actionable | In a preclinical study, RLY-2608 treatment decreased viability of a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA I817F in culture (PMID: 37916958). | 37916958 |
PIK3CA P539R PIK3CA H1047R PTEN del | breast cancer | sensitive | MEN1611 | Preclinical - Cell culture | Actionable | In a preclinical study, MEN1611 (CH5132799) inhibited viability in a breast cancer cell line with deletion of PTEN and harboring PIK3CA H1047R and P539R in culture (PMID: 36913051). | 36913051 |
PIK3CA E453K PIK3CA H1047R | estrogen-receptor positive breast cancer | predicted - sensitive | RLY-2608 | Case Reports/Case Series | Actionable | In a clinical case study, treatment with RLY-2608 resulted in a partial response with a reduction in liver, lung, and soft tissue target lesions in a patient with ESR1/PGR-positive, ERBB2 (HER2)-low breast cancer harboring PIK3CA H1047R and PIK3CA E453K (PMID: 37916956; NCT05216432). | 37916956 |
PIK3CA mutant | Erdheim-Chester disease | sensitive | Trametinib | Guideline | Actionable | Mekinist (trametinib) is included in guidelines as first-line or subsequent-line therapy for patients with Erdheim-Chester disease harboring mutations in the MAPK pathway such as ARAF, NRAS, KRAS, MAP2K1/2, PIK3CA, or with no detectable mutations, or for whom testing is not available (NCCN.org). | detail... |
PIK3CA mutant | female reproductive organ cancer | predicted - sensitive | Capivasertib | Phase I | Actionable | In a Phase I trial, treatment with Truqap (capivasertib) was well-tolerated and resulted in tumor shrinkage in 56% (14/25) patients with PIK3CA-mutant gynecological cancers, however, the response rate was modest with confirmed RECIST responses in 8% (2/26) of patients (PMID: 29066505; NCT01226316). | 29066505 |
PIK3CA mutant | breast cancer | predicted - sensitive | Capivasertib | Phase I | Actionable | In a Phase I trial, treatment with Truqap (capivasertib) was well-tolerated and resulted in tumor shrinkage in 46% (12/26) patients with PIK3CA-mutant breast cancer, with confirmed RECIST responses in 4% (1/28) of patients (PMID: 29066505; NCT01226316). | 29066505 |
PIK3CA mutant | breast cancer | predicted - sensitive | Capivasertib | Preclinical | Actionable | In a preclinical study, Truqap (capivasertib) inhibited growth in breast cancer cell lines and xenograft models expressing PIK3CA mutations (PMID: 22294718). | 22294718 |
PIK3CA mutant | lung squamous cell carcinoma | no benefit | Capivasertib | Case Reports/Case Series | Actionable | In a Phase II trial (NLMT), Truqap (capivasertib) treatment did not result in a confirmed response (0/4) or durable clinical benefit (0/4) in patients with squamous cell lung cancer harboring PIK3CA mutations, thus the cohort was closed due to futility (PMID: 32669708, NCT02664935). | 32669708 |
PIK3CA mutant | lung adenocarcinoma | no benefit | Capivasertib | Case Reports/Case Series | Actionable | In a Phase II trial (NLMT), Truqap (capivasertib) treatment did not result in a confirmed response (0/8) or durable clinical benefit (0/8) in patients with lung adenocarcinoma harboring mutations in PIK3CA, PTEN, or AKT, thus the cohort was closed due to futility (PMID: 32669708, NCT02664935). | 32669708 |
PIK3CA mutant | endometrioid ovary carcinoma | sensitive | Capivasertib | Case Reports/Case Series | Actionable | In a Phase I clinical trial, Truqap (capivasertib) demonstrated safety and efficacy in patients with advanced solid tumors, including prolonged stable disease (156 days) in one patient with a PIK3CA-mutant endometrioid ovarian cancer (Cancer Res 2013;73(8 Suppl):Abstract nr LB-66; NCT01226316, NCT01353781). | detail... |
PIK3CA mutant | stomach cancer | sensitive | BAY1082439 | Preclinical | Actionable | In a preclinical study, BAY1082439 inhibited growth of gastric cancer cells harboring PIK3CA mutations in culture and xenograft models (AACR; 2015. Abstract nr 2674). | detail... |
PIK3CA mutant | Advanced Solid Tumor | sensitive | BAY1082439 | Preclinical | Actionable | In a preclinical study, BAY1082439 induced regression in xenograft models of advanced solid tumors with PIK3CA mutations (Cancer Res April 15, 2012 72; 2799). | detail... |
PIK3CA mutant | colon cancer | sensitive | Dactolisib | Preclinical | Actionable | In a preclinical study, BEZ235 demonstrated efficacy in promoting apoptosis of colon cancer cells harboring a PIK3CA mutation in culture (PMID: 22543857). | 22543857 |
PIK3CA mutant | stomach cancer | sensitive | Dactolisib | Preclinical | Actionable | In a preclinical study, BEZ235 demonstrated efficacy in promoting apoptosis of gastric cancer cells harboring a PIK3CA mutation in culture (PMID: 22543857). | 22543857 |
PIK3CA mutant | endometrial cancer | sensitive | Alpelisib | Case Reports/Case Series | Actionable | In a Phase I trial, Alpelisib (BYL719) treatment resulted in 1 complete response and 1 partial response in patients with endometrial cancer harboring PIK3CA mutations (PMID: 29401002; NCT01219699). | 29401002 |
PIK3CA mutant | cervical cancer | predicted - sensitive | Alpelisib | Case Reports/Case Series | Actionable | In a Phase I trial, Alpelisib (BYL719) treatment resulted in partial response in 3 patients with cervical cancer harboring PIK3CA mutations (PMID: 29401002; NCT01219699). | 29401002 |
PIK3CA mutant | colorectal cancer | sensitive | Alpelisib | Phase I | Actionable | In a Phase I trial, Alpelisib (BYL719) treatment resulted in a disease control rate of 34.3% (12/35, 0 complete response (CR), 2 partial response (PR), 10 stable disease (SD)), and a clinical benefit rate (CR+PR+SD>24 weeks) of 8.6% (3/35) in patients with colorectal cancer harboring PIK3CA mutations (PMID: 29401002; NCT01219699). | 29401002 |
PIK3CA mutant | head and neck cancer | sensitive | Alpelisib | Phase I | Actionable | In a Phase I trial, Alpelisib (BYL719) treatment resulted in a disease control rate of 68.4% (13/19, 0 complete response (CR), 0 partial response (PR), 13 stable disease (SD)), and a clinical benefit rate (CR+PR+SD>24 weeks) of 10.5% (2/19) in patients with head and neck cancer harboring PIK3CA mutations (PMID: 29401002; NCT01219699). | 29401002 |
PIK3CA mutant | Her2-receptor negative breast cancer | sensitive | Alpelisib | Phase I | Actionable | In a Phase I trial, Alpelisib (BYL719) treatment resulted in a disease control rate of 60.9% (14/23, 0 complete response (CR), 1 partial response (PR), 13 stable disease (SD)), and a clinical benefit rate (CR+PR+SD>24 weeks) of 17.4% (4/23) in patients with ER-positive, ERBB2 (HER2)-negative breast cancer harboring PIK3CA mutations (PMID: 29401002; NCT01219699). | 29401002 |
PIK3CA mutant | Advanced Solid Tumor | sensitive | Alpelisib | Phase I | Actionable | In a Phase I trial, Alpelisib (BYL719) demonstrated safety and efficacy in patients with advanced solid tumor harboring PIK3CA mutations, resulted in a disease control rate of 58.2% (78/134, 1 complete response (CR), 7 partial response (PR), 70 stable disease (SD)), and a clinical benefit rate (CR+PR+SD>24 weeks) of 15.7% (21/134) (PMID: 29401002; NCT01219699). | 29401002 |
PIK3CA mutant | Advanced Solid Tumor | sensitive | Alpelisib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, PIK3CA mutations were associated with sensitivity to Alpelisib (BYL719) in human tumor cell lines in culture and in xenograft models (PMID: 24608574). | 24608574 |
PIK3CA mutant | Advanced Solid Tumor | sensitive | Onatasertib | Phase I | Actionable | In a Phase I trial, CC-223 demonstrated safety and preliminary efficacy in patients with solid tumors, including stable disease for greater than 110 days in 2 patients with PIK3CA mutation or PTEN deletion (PMID: 26177599). | 26177599 detail... |
PIK3CA mutant | cervical cancer | decreased response | Cetuximab | Phase II | Actionable | In a Phase II clinical trial, Erbitux (cetuximab) treatment, in addition to radiochemotherapy, did not result in any complete responses (0/8) and demonstrated a worse disease free survival when compared to radiochemotherapy alone in cervical cancer patients harboring PIK3CA mutations (PMID: 25724520). | 25724520 |
PIK3CA mutant | breast cancer | sensitive | CUDC-907 | Preclinical | Actionable | In a preclinical study, CUDC-907 inhibited growth of human breast cancer cell lines harboring PIK3CA mutations in culture (PMID: 22693356). | 22693356 |
PIK3CA mutant | hematologic cancer | sensitive | CUDC-907 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, CUDC-907 inhibited PIK3CA, blocked downstream AKT pathway activation, and induced apoptosis and cell cycle arrest in both PIK3CA wild-type and PIK3CA mutant human cancer cell lines and xenograft models of multiple solid and hematologic cancers (PMID: 22693356). | 22693356 |
PIK3CA mutant | Advanced Solid Tumor | sensitive | CUDC-907 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, CUDC-907 inhibited PIK3CA, blocked downstream AKT pathway activation, and induced apoptosis and cell cycle arrest in both PIK3CA wild-type and PIK3CA mutant human cancer cell lines and xenograft models of multiple tumor types (PMID: 22693356). | 22693356 |
PIK3CA mutant | Erdheim-Chester disease | sensitive | Everolimus | Guideline | Actionable | Afinitor (everolimus) is included in guidelines as first-line or subsequent-line therapy for patients with Erdheim-Chester disease harboring PIK3CA mutations (NCCN.org). | detail... |
PIK3CA mutant | Her2-receptor negative breast cancer | no benefit | Everolimus | Phase III | Actionable | In a retrospective analysis of a Phase III trial (BOLERO-2), the presence of PIK3CA mutations did not significantly affect the efficacy of Afinitor (everolimus) in patients with hormone receptor-positive, Erbb2 (Her2)-negative breast cancer, with a HR for progression-free survival of 0.37 in PIK3CA wild-type group and a HR of 0.51 (p=0.35) in patients with PIK3CA mutations (PMID: 26503204; NCT00863655). | 26503204 |
PIK3CA mutant | estrogen-receptor positive breast cancer | no benefit | Fulvestrant | Phase II | Actionable | In a Phase II trial, Falsodex (fulvestrant) treatment resulted in similar progression free survival in ER positive breast cancer patients harboring PIK3CA mutations and those who were PIK3CA wild-type (PMID: 27174596). | 27174596 |
PIK3CA mutant | endometrial cancer | sensitive | Pictilisib | Preclinical | Actionable | In a preclinical study, endometrioid endometrial cancer cell lines harboring PIK3CA mutations demonstrated increased sensitivity to GDC-0941 (Pictilisib) induced growth inhibition comparing to PIK3CA wild-type cells in culture (PMID: 23674493). | 23674493 |
PIK3CA mutant | breast cancer | sensitive | Pictilisib | Preclinical | Actionable | In a preclinical study, GDC-0941 inhibited growth and induced apoptosis in breast cancer cells expressing PIK3CA mutations (PMID: 24601221). | 24601221 |
PIK3CA mutant | triple-receptor negative breast cancer | sensitive | Pictilisib | Preclinical - Cell culture | Actionable | In a preclinical study, triple-receptor negative breast cancer cell lines harboring PIK3CA mutations demonstrated increased sensitivity to Pictilisib (GDC-0941) in culture (PMID: 27196766). | 27196766 |
PIK3CA mutant | endometrial cancer | sensitive | Apitolisib | Phase II | Actionable | In a Phase II trial, Apitolisib (GDC-0980) was poorly tolerated, but demonstrated efficacy in endometrial cancer patients harboring mutations in PIK3CA, PTEN, or AKT1 (J Clin Oncol 32:5s, 2014 (suppl; abstr 5513)). | detail... |
PIK3CA mutant | Advanced Solid Tumor | predicted - sensitive | Apitolisib | Case Reports/Case Series | Actionable | In a Phase I trial, Apitolisib (GDC-0980) treatment resulted in a partial response in 21% (3/14) and stable disease in 64% (9/14) of patients with advanced solid tumors harboring PIK3CA mutations (PMID: 26787751; NCT00854152). | 26787751 |
PIK3CA mutant | breast cancer | no benefit | GSK2126458 | Phase I | Actionable | In a Phase I trial, GSK2126458 was well-tolerated and resulted in some efficacy in patients with breast cancer harboring a PIK3CA mutation including stable disease in 22% (2/9), however, objective response rate was not associated with PIK3CA mutations when compared to those without PIK3CA mutations (PMID: 26603258). | 26603258 |
PIK3CA mutant | Advanced Solid Tumor | predicted - sensitive | Uprosertib | Phase I | Actionable | In a Phase I clinical trial, GSK2141795 demonstrated safety and preliminary efficacy in patients with advanced solid tumors, with 4 patients with PIK3CA mutations and/or PTEN loss achieving stable disease for greater than 6 months (J Clin Oncol 29: 2011 (suppl; abstr 3003)). | detail... |
PIK3CA mutant | estrogen-receptor positive breast cancer | predicted - sensitive | Letrozole | Phase III | Actionable | In a Phase III trial, estrogen-receptor positive breast cancer patients harboring a PIK3CA mutation demonstrated a greater benefit when treated with Femara (letrozole) compared to Nolvadex (tamoxifen) (PMID: 29902286; NCT00004205). | 29902286 |
PIK3CA mutant | endometrial cancer | no benefit | MK2206 | Phase II | Actionable | In a Phase II trial, MK2206 demonstrated limited benefit in endometrial cancer patients regardless of PIK3CA status, with partial responses in 6% (2/37) of patients, 19% (7/37; 5 with serous histology) remaining progression-free for at least 6 mo, and a median progression-free survival (PFS) of 2.0 mo in the overall population, and partial responses in 11% (11/9), 33% (3/9) progression-free for 6 mo, and a median PFS of 1.7 mo in the group of patients with PIK3CA mutations (PMID: 31714586; NCT01307631). | 31714586 |
PIK3CA mutant | breast cancer | no benefit | MK2206 | Phase II | Actionable | In a Phase II trial, MK2206 demonstrated limited clinical efficacy in patients with advanced breast cancer harboring mutations in PIK3CA (n=14) or AKT1 (n=4), resulted in an objective response rate of 5.6% (1/18, 1 partial response) and a 6-month progression-free survival rate of 5.6%, with no significant target inhibition in tumor biopsies (PMID: 31277699; NCT01277757). | 31277699 |
PIK3CA mutant | breast cancer | sensitive | OSI-027 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, OSI-027 induced tumor regression in breast cancer cell line xenograft models harboring PIK3CA mutations (PMID: 21673091). | 21673091 |
PIK3CA mutant | ovarian cancer | sensitive | OSI-027 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, OSI-027 inhibited tumor growth in ovarian cancer cell line xenograft models harboring PIK3CA mutations (PMID: 21673091). | 21673091 |
PIK3CA mutant | endometrial cancer | not predictive | Perifosine | Phase II | Actionable | In a Phase II trial , Perifosine (KRX-0401) treatment was well-tolerated, resulted in stable disease as best response in patients with recurrent endometrial cancer, no significant difference in disease control rate (47.1%, 8/17 vs 14.3%, 1/7, p=0.19), median progression-free survival (HR=1.71, p=0.30), or median overall survival (HR=0.92, p=0.88) was identified between PIK3CA wild-type and PIK3CA mutant patients (PMID: 28864978). | 28864978 |
PIK3CA mutant | ovarian cancer | not predictive | Perifosine | Phase II | Actionable | In a Phase II trial , Perifosine (KRX-0401) treatment was well-tolerated, resulted in stable disease as best response in patients with recurrent ovarian cancer, no significant difference in disease control rate (12.5%, 2/16 vs 40%, 2/5, p=0.22), median progression-free survival (HR=0.57, p=0.32), or median overall survival (HR=1.37, p=0.58) was identified between PIK3CA wild-type and PIK3CA mutant patients (PMID: 28864978). | 28864978 |
PIK3CA mutant | cervical cancer | not predictive | Perifosine | Phase II | Actionable | In a Phase II trial , Perifosine (KRX-0401) treatment was well-tolerated, resulted in stable disease as best response in patients with recurrent cervical cancer, no significant difference in disease control rate (11.1%, 2/18 vs 25%, 2/8, p=0.56), median progression-free survival (HR=1.06, p=0.81), or median overall survival (HR=1.66, p=0.26) was identified between PIK3CA wild-type and PIK3CA mutant patients (PMID: 28864978). | 28864978 |
PIK3CA mutant | lung non-small cell carcinoma | sensitive | PF-04691502 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, PF-04691502 inhibited tumor growth in non-small cell lung cancer cell line xenograft models harboring PIK3CA mutations (PMID: 21750219). | 21750219 |
PIK3CA mutant | colon cancer | sensitive | PWT33597 | Preclinical | Actionable | In a preclinical study, PWT33597 decreased signaling of mTOR and PIK3 pathways in colon cancer cells with Pik3ca mutations (Cancer Res 2011;71(8 Suppl):Abstract nr 4485). | detail... |
PIK3CA mutant | lung non-small cell carcinoma | sensitive | PWT33597 | Preclinical | Actionable | In a preclinical study, PWT33597 decreased signaling of mTOR and PIK3 pathways in non-small cell lung cancer cells with Pik3ca mutations (Cancer Res 2011;71(8 Suppl):Abstract nr 4485). | detail... |
PIK3CA mutant | Advanced Solid Tumor | sensitive | PX-866 | Phase I | Actionable | In a Phase I trial, PX-866 demonstrated efficacy and was well tolerated in patients with advanced solid tumor with both PIK3CA wild-type and mutant status (PMID: 22693357). | 22693357 |
PIK3CA mutant | Erdheim-Chester disease | sensitive | Sirolimus | Guideline | Actionable | Rapamune (sirolimus) is included in guidelines as first-line or subsequent-line therapy for patients with Erdheim-Chester disease harboring PIK3CA mutations (NCCN.org). | detail... |
PIK3CA mutant | hepatocellular carcinoma | decreased response | Sorafenib | Clinical Study - Cohort | Actionable | In a clinical case study, Nexavar (sorafenib) treatment of patients with hepatocellular carcinoma harboring Mtor pathway mutations in PIK3CA, PTEN, TSC2, or TSC1 (n=12), resulted in a lower disease control rate (8.3% vs. 40.2%), shorter progression-free survival (1.9 months vs. 5.3 months) and shorter overall survival (10.4 months vs. 17.9 months) compared to patients without mutations in this pathway (n=67) (PMID: 30373752; NCT01775072). | 30373752 |
PIK3CA mutant | endometrial cancer | no benefit | Temsirolimus | Phase II | Actionable | In a retrospective study of a Phase II trial, mutation status of PIK3CA was not associated with progression-free survival or response rate in advanced endometrial cancer patients treated with Torisel (temsirolimus) (PMID: 27016228). | 27016228 |
PIK3CA mutant | breast cancer | no benefit | Temsirolimus | Phase II | Actionable | In a Phase II trial (TAPUR), Torisel (temsirolimus) treatment demonstrated limited efficacy in patients with breast cancer harboring PIK3CA mutations, resulting in an objective response rate of 9% (1/12, 1 partial response) and a disease control rate of 9%, which let to the closing of the cohort due to futility (p=0.83) (J Clin Oncol 41, 2023 (suppl 16; abstr 3117); NCT02693535). | detail... |
PIK3CA mutant | breast cancer | no benefit | Temsirolimus | Phase II | Actionable | In a Phase II trial, Torisel (temsirolimus) treatment resulted in stable disease in 9.7% (3/31) of breast cancer patients positive for ER, PR or ERBB2 (HER2), however there was no association between PIK3CA mutational status and clinical benefits (PMID: 22245973). | 22245973 |
PIK3CA mutant | ovarian cancer | sensitive | Temsirolimus | Case Reports/Case Series | Actionable | In a clinical study, an ovarian cancer patient harboring a PIK3CA E542 mutation demonstrated stable disease when treated with Torisel (temsirolimus) (PMID: 21216929). | 21216929 |
PIK3CA mutant | ovarian cancer | sensitive | Temsirolimus | Phase I | Actionable | In a Phase I clinical trial, Torisel (temsirolimus) demonstrated limited efficacy in ovarian cancer patients with PIK3CA mutations (PMID: 22271473). | 22271473 |
PIK3CA mutant | Ewing sarcoma | predicted - sensitive | Temsirolimus | Preclinical - Pdx | Actionable | In a preclinical study, Torisel (temsirolimus) treatment increased event-free survival in a Ewing sarcoma patient-derived xenograft (PDX) model harboring a PIK3CA mutation (PMID: 37523146). | 37523146 |
PIK3CA mutant | breast cancer | sensitive | VS-5584 | Preclinical | Actionable | In a preclinical study, PIK3CA mutant breast cancer cells showed increased sensitivity to VS-5584 compared to PIK3CA wild-type cells in culture (PMID: 23270925). | 23270925 |
PIK3CA mutant | Advanced Solid Tumor | sensitive | VS-5584 | Preclinical | Actionable | In preclinical studies, VS-5584 demonstrated efficacy in a variety of cancer cell lines, particularly those harboring PIK3CA mutations (PMID: 23270925). | 23270925 |
PIK3CA mutant | endometrial carcinoma | no benefit | Copanlisib | Phase II | Actionable | In a Phase II (NRG-GY008) trial, Aliqopa (copanlisib) was well tolerated but demonstrated limited efficacy, resulted in stable disease as best response in 54.5% (6/11) of patients with endometrial carcinoma harboring PIK3CA mutations, with a median progression-free survival of 2.8 months and a median overall survival of 15.2 months (PMID: 31934607). | 31934607 |
PIK3CA mutant | squamous cell carcinoma | sensitive | Carboxyamidotriazole Orotate | Phase I | Actionable | In a Phase I clinical trial, carboxyamidotriazole orotate treatment demonstrated some efficacy in patients with various solid tumors including squamous cell carcinomas (tonsil) with PI3KCA and NRAS mutations (J Clin Oncol 31, 2013 (suppl; abstr 2518)). | detail... |
PIK3CA mutant | Advanced Solid Tumor | sensitive | Carboxyamidotriazole Orotate | Phase I | Actionable | In a Phase I clinical trial, carboxyamidotriazole orotate treatment demonstrated some efficacy in patients with various solid tumors, including patients harboring PIK3CA mutations (J Clin Oncol 31, 2013 (suppl; abstr 2518)). | detail... |
PIK3CA mutant | Erdheim-Chester disease | sensitive | Cobimetinib | Guideline | Actionable | Cotellic (cobimetinib) is included in guidelines as preferred first-line or subsequent-line therapy for patients with Erdheim-Chester disease harboring mutations in the MAPK pathway such as ARAF, NRAS, KRAS, MAP2K1/2, PIK3CA, or with no detectable mutations, or for whom testing is not available (NCCN.org). | detail... |
PIK3CA mutant | lung squamous cell carcinoma | no benefit | Taselisib | Phase I | Actionable | In a Phase I (SWOG S1400B) trial, Taselisib (GDC-0032) treatment did not meet its primary endpoint for response rate in patients with lung squamous cell carcinoma harboring PIK3CA mutations, resulting in only 1 response in the primary analysis population (n=21) (PMID: 31158500; NCT02785913). | 31158500 |
PIK3CA mutant | Advanced Solid Tumor | sensitive | Taselisib | Phase I | Actionable | In a Phase I trial, Taselisib (GDC-0032) demonstrated activity in patients with PIK3CA-mutant advanced solid tumors, in the absence of alterations in the MAPK or PTEN pathways (Cancer Res October 1, 2014 74:915). | detail... |
PIK3CA mutant | breast adenocarcinoma | sensitive | Acalisib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Acalisib (GS-9820) resulted in tumor growth inhibition in xenograft models of breast adenocarcinoma harboring a PIK3CA mutation (Mol Cancer Ther 2009;8(12 Suppl):B136). | detail... |
PIK3CA mutant | breast cancer | predicted - sensitive | Serabelisib | Case Reports/Case Series | Actionable | In a Phase I trial, MLN1117 (INK1117) treatment resulted in partial response in 3 patients with breast cancer harboring PI3CA mutations (PMID: 28490463; NCT01449370). | 28490463 |
PIK3CA mutant | stomach cancer | predicted - sensitive | Serabelisib | Case Reports/Case Series | Actionable | In a Phase I trial, MLN1117 (INK1117) treatment resulted in a partial response in one patient with gastric cancer harboring a PIK3CA mutation (PMID: 28490463; NCT01449370). | 28490463 |
PIK3CA mutant | Advanced Solid Tumor | sensitive | Serabelisib | Phase I | Actionable | In a Phase I trial, MLN1117 demonstrated safety and preliminary efficacy in a variety of patients with advanced solid tumors carrying PIK3CA mutations (Journal of Clinical Oncology, 2015 ASCO Annual Meeting Vol 33, No 15_suppl., 2015: 2501). | detail... |
PIK3CA mutant | Advanced Solid Tumor | sensitive | Serabelisib | Preclinical | Actionable | In a preclinical study, MLN1117 inhibited proliferation of tumor cells harboring oncogenic PIK3CA mutations in culture and inhibited tumor growth in PIK3CA mutant xenograft models (Cancer Ther 2011;10(11 Suppl):Abstract nr A171). | detail... |
PIK3CA mutant | Advanced Solid Tumor | sensitive | M2698 | Preclinical | Actionable | In a preclinical study, MSC2363318A demonstrated anti-proliferative activity against many solid tumor cell lines with PI3K pathway genomic alterations, and inhibited tumor growth in several human cancer xenograft models of breast, pancreatic, glioblastoma and ovarian cancers (Mol Cancer Ther 2013;12(11 Suppl):A162). | detail... |
PIK3CA mutant | Advanced Solid Tumor | sensitive | XL147 | Phase I | Actionable | In a Phase I clinical trial, XL147 (SAR24508) was shown to be safe and potentially efficacious, with clinical activity seen irrespective of tumor PI3K pathway molecular alterations (PMID: 24166903). | 24166903 |
PIK3CA mutant | Advanced Solid Tumor | sensitive | XL147 | Preclinical | Actionable | In a preclinical study, tumor cell lines with PIK3CA mutations demonstrated sensitivity to XL147 in culture (PMID: 25637314). | 25637314 |
PIK3CA mutant | Advanced Solid Tumor | sensitive | Bevacizumab + Pegylated liposomal doxorubicin + Temsirolimus | Clinical Study | Actionable | In a clinical study, the combination of Torisel (temisirolimus) plus Avastin (bevacizumab) and Doxil (pegylated liposomal-doxirubicin) resulted in stable disease in patients with advanced solid tumors harboring PIK3CA mutations (PMID: 21216929). | 21216929 |
PIK3CA mutant | Advanced Solid Tumor | sensitive | Bevacizumab + Pegylated liposomal doxorubicin + Temsirolimus | Clinical Study | Actionable | In a clinical study, the combination of Torisel (temsirolimus) plus Avastin (bevacizumab) and Doxil (pegylated liposomal-doxorubicin) resulted in a partial response in patients with advanced solid tumors harboring PIK3CA mutations (PMID: 21216929). | 21216929 |
PIK3CA mutant | breast cancer | sensitive | Sapanisertib | Preclinical | Actionable | In a preclinical study, Sapanisertib (MLN0128) demonstrated efficacy in PIK3CA mutant breast cancer xenograft models (PMID: 23085766). | 23085766 |
PIK3CA mutant | Advanced Solid Tumor | sensitive | Sapanisertib | Preclinical | Actionable | In a preclinical study, human cancer cell lines harboring PIK3CA mutations were sensitive to Sapanisertib (MLN0128) as demonstrated by significant growth inhibition (PMID: 25261369). | 25261369 |
PIK3CA mutant | Advanced Solid Tumor | no benefit | Alpelisib + Infigratinib | Phase Ib/II | Actionable | In a Phase Ib trial, treatment with the combination of Piqray (alpelisib) and Truseltiq (infigratinib) resulted in partial response (PR) in 9.7% (6/62) and disease control (PR or stable disease) in 61.3% (34/62) of patients with advanced solid tumors harboring a PIK3CA mutation with or without an FGFR alteration, however, the efficacy was not deemed great enough to pursue further development (JCO Precision Oncology 2019 :3, 1-13). | detail... |
PIK3CA mutant | Her2-receptor positive breast cancer | not predictive | Ado-trastuzumab emtansine | Phase III | Actionable | In a retrospective analysis of a Phase III trial (KATHERINE), adjuvant Kadcyla (ado-trastuzumab emtansine) treatment demonstrated similar invasive disease-free survival benefit over Herceptin (trastuzumab) in PIK3CA mutant (HR=0.54) and PIK3CA wild-type (HR=0.48) patients with Erbb2 (Her2)-positive breast cancer who had residual invasive disease after neoadjuvant therapy (PMID: 36730339; NCT01772472). | 36730339 |
PIK3CA mutant | Her2-receptor positive breast cancer | sensitive | CCT128930 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, CCT128930 induced growth arrest and inhibited tumor growth in a xenograft model of a ERBB2 (HER2)-positive human breast cancer cell line harboring a PIK3CA mutation (PMID: 21191045). | 21191045 |
PIK3CA mutant | breast cancer | sensitive | AZD8835 | Preclinical | Actionable | In a preclinical study, AZD8835 inhibited tumor growth in breast cancer xenograft models harboring PIK3CA mutations (AACR; 2015. Abstract nr 2665). | detail... |
PIK3CA mutant | estrogen-receptor positive breast cancer | sensitive | AZD8835 | Preclinical | Actionable | In a preclinical study, AZD8835 inhibited proliferation of estrogen receptor (ER)-positive breast cancer cells harboring PIK3CA mutations in culture and suppressed tumor growth in xenograft models (PMID: 26839307). | 26839307 |
PIK3CA mutant | Advanced Solid Tumor | sensitive | AZD8835 | Preclinical | Actionable | In a preclinical study, AZD8835 inhibited growth of a variety of advanced solid tumor models with Pik3ca mutations in culture (PMID: 26839307). | 26839307 |
PIK3CA mutant | lung non-small cell carcinoma | predicted - sensitive | Sulindac | Preclinical - Cell culture | Actionable | In a preclinical study, non-small cell lung cancer cell lines harboring either a PIK3CA mutation or PIK3CA amplification demonstrated increased sensitivity to Clinoril (sulindac) compared to cell lines with wild-type PIK3CA, resulting in decreased proliferation in culture (PMID: 30683736). | 30683736 |
PIK3CA mutant | endometrial cancer | sensitive | MEN1611 | Preclinical | Actionable | In a preclinical study, MEN1611 (CH5132799) inhibited proliferation of endometrial cancer cells with PIK3CA mutations in culture (PMID: 21558396). | 21558396 |
PIK3CA mutant | breast cancer | sensitive | MEN1611 | Preclinical | Actionable | In a preclinical study, breast cancer cells with PIK3CA mutations, both with and without ERBB2 (HER2) amplification, demonstrated sensitivity to MEN1611 (CH5132799) in culture (PMID: 21558396). | 21558396 |
PIK3CA mutant | ovarian cancer | sensitive | MEN1611 | Preclinical | Actionable | In a preclinical study, MEN1611 (CH5132799) inhibited proliferation of ovarian cancer cells with PIK3CA mutations in culture (PMID: 21558396). | 21558396 |
PIK3CA mutant | prostate cancer | sensitive | MEN1611 | Preclinical | Actionable | In a preclinical study, MEN1611 (CH5132799) inhibited proliferation of prostate cancer cells with PIK3CA mutations in culture (PMID: 21558396). | 21558396 |
PIK3CA mutant | ovarian cancer | sensitive | Buparlisib + Olaparib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination of Buparlisib (BKM120) and Lynparza (olaparib) worked synergistically to induce apoptosis and inhibit growth of ovarian cancer cell lines harboring PIK3CA mutations in culture, and induced apoptosis and decreased proliferation of PIK3CA-mutant ovarian cancer cell line xenograft models (PMID: 26909613). | 26909613 |
PIK3CA mutant | Her2-receptor negative breast cancer | no benefit | Capivasertib + Paclitaxel | Phase II | Actionable | In a Phase II trial, the addition of Truqap (capivasertib) to Taxol (paclitaxel) therapy did not improve progression-free survival compared to placebo (10.9 vs 10.8 months) in patients with PIK3CA-mutant, Esr1-positive, Erbb2 (Her2)-negative breast cancer (PMID: 30860570; NCT01625286). | 30860570 |
PIK3CA mutant | Advanced Solid Tumor | sensitive | AT-7867 | Preclinical | Actionable | In a preclinical study, AT-7867 inhibited proliferation in several human tumor cell lines harboring PIK3CA mutations in culture (PMID: 20423992). | 20423992 |
PIK3CA mutant | Advanced Solid Tumor | sensitive | A-443654 | Preclinical | Actionable | In a preclinical study, cells expressing mutant PIK3CA demonstrated increased sensitivity to A-443654 compared to cells expressing wild-type PIK3CA (PMID: 19208828). | 19208828 |
PIK3CA mutant | gastric adenocarcinoma | sensitive | Fluorouracil + PI-103 | Preclinical | Actionable | In a preclinical study, PI-103 enhanced sensitivity to 5-FU in gastric cancer cells with mutant PIK3CA (PMID: 22336586). | 22336586 |
PIK3CA mutant | breast cancer | sensitive | AT13148 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, a ERBB3 (HER3) positive breast cancer cell line xenograft model harboring a PIK3CA mutation was demonstrated decreased tumor growth when treated with AT13148 (PMID: 22781553). | 22781553 |
PIK3CA mutant | triple-receptor negative breast cancer | sensitive | Palbociclib + Pictilisib | Preclinical | Actionable | In a preclinical study, Ibrance (palbociclib) and Pictilisib (GDC-0941) worked synergistically to inhibit the survival of triple-receptor negative breast cancer cell lines harboring PIK3CA mutations in culture (PMID: 27020857). | 27020857 |
PIK3CA mutant | head and neck squamous cell carcinoma | sensitive | Radiotherapy + Taselisib | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, Taselisib (GDC-0032) enhanced the effects of radiation induced apoptosis in HNSCC cell lines, cell line xenograft models, and a patient derived xenograft (PDX) model, all with PIK3CA mutations (PMID: 26589432). | 26589432 |
PIK3CA mutant | breast cancer | sensitive | Letrozole + Taselisib | Phase Ib/II | Actionable | In a Phase Ib trial, Taselisib (GDC-0032) and Femara (letrozole) combination therapy resulted in an overall response rate of 38% in breast cancer patients with PIK3CA mutations, compared to 9% in patients with wild-type PIK3CA (Cancer Res May 1, 2015 75; PD5-2). | detail... |
PIK3CA mutant | estrogen-receptor positive breast cancer | no benefit | Fulvestrant + Pictilisib | Phase II | Actionable | In a Phase II trial, Falsodex (fulvestrant) and Pictilisib (GDC-0941) combination treatment resulted in similar progression free survival in ER positive breast cancer patients harboring PIK3CA mutations and those who were PIK3CA wild-type (PMID: 27174596). | 27174596 |
PIK3CA mutant | breast cancer | sensitive | Alpelisib + GSK2334470 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, GSK2334470 resensitized Alpelisib (BYL719)-resistant breast cancer cell lines harboring PIK3CA mutations to Alpelisib (BYL719) in culture and in cell line xenograft models (PMID: 27451907). | 27451907 |
PIK3CA mutant | colorectal cancer | predicted - sensitive | MS417 + Pictilisib | Preclinical - Cell culture | Actionable | In a preclinical study, Pictilisib (GDC-0941) and MS417 in combination resulted in improved growth inhibition and increased cell death compared to either agent alone in colorectal cancer cell lines harboring PIK3CA mutations in culture (PMID: 26058079). | 26058079 |
PIK3CA mutant | breast cancer | predicted - sensitive | Inavolisib | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, Itovebi (inavolisib) inhibited proliferation and induced apoptosis in PIK3CA-mutant breast cancer cell lines in culture, and induced apoptosis and tumor regression in PIK3CA-mutant breast cancer cell line and patient-derived xenograft models (AACR; Cancer Res 2017;77(13 Suppl):Abstract nr 156). | detail... |
PIK3CA mutant | invasive bladder transitional cell carcinoma | predicted - resistant | Cisplatin + Gemcitabine + Sorafenib | Phase II | Actionable | In a Phase II trial, PIK3CA mutations were more frequent in muscle-invasive urothelial bladder cancer patients that did not respond to Nexavar (sorafenib), Platinol (cisplatin) and Gemzar (gemcitabine) combination therapy than those who did respond (J Clin Oncol 35, 2017 (suppl 6S; abstract 345)). | detail... |
PIK3CA mutant | head and neck squamous cell carcinoma | predicted - sensitive | Carboplatin + Paclitaxel + Temsirolimus | Phase II | Actionable | In a Phase II trial, two patients with head and neck squamous cell carcinoma harboring a PIK3CA mutation who had stable disease demonstrated some tumor regression when treated with the combination of Torisel (temsirolimus), Paraplatin (carboplatin), and Taxol (paclitaxel) (PMID: 28961834). | 28961834 |
PIK3CA mutant | colorectal cancer | predicted - sensitive | Copanlisib + Nivolumab | Phase Ib/II | Actionable | In a Phase I/II trial, treatment with the combination of Aliqopa (copanlisib) and Opdivo (nivolumab) was well tolerated and resulted in 3 partial responses in 22 patients with microsatellite stable colorectal cancer harboring PIK3CA mutations (Cancer Res (2024) 84 (7_Supplement): CT007; NCT03711058). | detail... |
PIK3CA mutant | breast cancer | predicted - sensitive | CYH33 | Preclinical - Cell culture | Actionable | In a preclinical study, breast cancer cell lines harboring PIK3CA mutations demonstrated increased sensitivity to CYH33 compared to cell lines with wild-type PIK3CA in culture (p<0.01) (PMID: 30003928). | 30003928 |
PIK3CA mutant | cervical cancer | predicted - sensitive | WX390 | Case Reports/Case Series | Actionable | In a Phase I trial, WX390 treatment resulted in a partial responses in a patient with cervical cancer harboring PIK3CA mutation (J Clin Oncol 39, no. 15_suppl (May 20, 2021) 3106-3106; NCT03730142). | detail... |
PIK3CA mutant | head and neck cancer | predicted - sensitive | WX390 | Case Reports/Case Series | Actionable | In a Phase I trial, WX390 treatment resulted in a partial responses in a patient with head and neck cancer harboring PIK3CA mutation, and stable disease with tumor shrinkage for 8 months in another patient with PIK3CA-mutant head and neck cancer (J Clin Oncol 39, no. 15_suppl (May 20, 2021) 3106-3106; NCT03730142). | detail... |
PIK3CA mutant | Advanced Solid Tumor | predicted - sensitive | TOS-358 | Preclinical - Pdx | Actionable | In a preclinical study, TOS-358 demonstrated efficacy in patient-derived xenograft (PDX) and cell line xenograft models harboring PIK3CA mutations (Cancer Res (2023) 83 (7_Supplement): 4946). | detail... |
PIK3CA mutant | Ewing sarcoma | predicted - sensitive | Irinotecan + Temozolomide + Temsirolimus | Case Reports/Case Series | Actionable | In a clinical study, Torisel (temsirolimus), Temodar (temozolomide), and Camptosar (irinotecan) combination treatment resulted in a partial response in a pediatric patient with Ewing sarcoma harboring a PIK3CA mutation (PMID: 37523146; NCT03336931). | 37523146 |
CDKN2A mut PIK3CA mut | breast cancer | sensitive | Sapanisertib | Preclinical | Actionable | In a preclinical study, a breast cancer cell line harboring mutations in PIK3CA and CDKN2A demonstrated sensitivity to Sapanisertib (MLN0128) in culture (PMID: 25261369). | 25261369 |
PIK3CA mut PTEN loss | breast cancer | sensitive | Buparlisib | Preclinical - Pdx | Actionable | In a preclinical study, Buparlisib (BKM120) inhibited Akt signaling and growth in a PDX model of breast cancer cells harboring a PIK3CA mutation and PTEN loss ( Cancer Res October 1, 2014 74; LB-327 ). | detail... |
PIK3CA mut PTEN loss | breast cancer | resistant | Alpelisib | Case Reports/Case Series | Actionable | In a clinical case study, a breast cancer patient harboring a PIK3CA mutation developed resistance to Alpelisib (BYL719) treatment and progressive disease after initial response, accompanied by a loss of PTEN, and the corrresponding patient-derived xenograft model demonstrated resistance to Alpelisib (BYL719)-induced inhibition of tumor growth (PMID: 25409150). | detail... 25409150 |
PIK3CA mut PTEN loss | prostate cancer | sensitive | PKI-179 | Preclinical - Cell culture | Actionable | In a preclinical study, PKI-179 inhibited growth of prostate cancer cells harboring PIK3CA mutations and PTEN loss in culture (PMID: 20797855). | 20797855 |
PIK3CA mut PTEN loss | breast cancer | sensitive | Alpelisib + AZD6482 | Preclinical - Pdx | Actionable | In a preclinical study, AZD6482 and Alpelisib (BYL719) combination treatment inhibited Akt signaling and growth in a breast cancer patient-derived xenograft (PDX) model harboring a PIK3CA mutation and PTEN loss (Cancer Res October 1, 2014 74; LB-327). | detail... |
FGFR1 over exp PIK3CA mut | estrogen-receptor positive breast cancer | sensitive | Alpelisib + Lucitanib | Preclinical - Cell culture | Actionable | In a preclinical study, an estrogen-receptor positive breast cancer cell line over expressing FGFR1 and expressing a PIK3CA mutation demonstrated sensitivity to the combination of Alpelisib (BYL719) and Lucitanib (E-3810) in culture (PMID: 27126994). | 27126994 |
BRAF V600E PIK3CA mut | colorectal cancer | sensitive | ASN003 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, a colorectal cancer cell line xenograft model co-harboring BRAF V600E and a PIK3CA mutation demonstrated tumor growth inhibition when treated with ASN003 (Mol Cancer Ther 2015;14(12 Suppl 2):Abstract nr B100). | detail... |
PIK3CA wild-type | Her2-receptor negative breast cancer | no benefit | Alpelisib | Phase I | Actionable | In a Phase I trial, Alpelisib (BYL719) treatment resulted in no clinical benefit in 4 patients with ER-positive, ERBB2 (HER2)-negative breast cancer harboring PIK3CA mutations (PMID: 29401002; NCT01219699). | 29401002 |
PIK3CA wild-type | Advanced Solid Tumor | sensitive | PX-866 | Phase I | Actionable | In a Phase I study, PX-866 demonstrated efficacy and was well tolerated in patients with advanced solid tumor with both PIK3CA wild-type and mutant status (PMID: 22693357). | 22693357 |
PIK3CA wild-type | Her2-receptor positive breast cancer | sensitive | Lapatinib + Paclitaxel + Trastuzumab | Phase II | Actionable | In a Phase II trial, the combination of Taxol (paclitaxel) plus Herceptin (trastuzumab) and Tykerb (lapatinib) resulted in a higher pathologic complete remission rate in ERBB2 (HER2)-receptor positive breast cancer patients with PIK3CA wild-type compared to those harboring a PIK3CA mutation (PMID: 26245675). | 26245675 |
PIK3CA wild-type | triple-receptor negative breast cancer | no benefit | Palbociclib + Pictilisib | Preclinical | Actionable | In a preclinical study, the combination of Ibrance (palbociclib) and Pictilisib (GDC-0941) did not improve growth inhibition compared to single drug treatment in PIK3CA wild-type, triple-receptor negative breast cancer cell lines in culture (PMID: 27020857). | 27020857 |
PIK3CA wild-type | breast cancer | no benefit | Dactolisib + WEHI-539 | Preclinical - Cell culture | Actionable | In a preclinical study, inhibition of Pi3k signaling by BEZ235 did not sensitize PIK3CA wild-type breast cancer cell lines to WEHI-539 in culture (PMID: 27974663). | 27974663 |
PIK3CA wild-type | breast cancer | predicted - sensitive | A-1210477 + WEHI-539 | Preclinical - Cell culture | Actionable | In a preclinical study, combination of WEHI-539 and A-1210477 resulted in enhanced apoptosis in PIK3CA wild-type breast cancer cell lines in culture (PMID: 27974663). | 27974663 |
BRAF V600E/K PIK3CA wild-type | melanoma | no benefit | A66 | Preclinical | Actionable | In a preclinical study, A66 did not inhibit proliferation of melanoma cell lines harboring BRAF V600E/K and wild-type PIK3CA in culture (PMID: 26137449). | 26137449 |
BRAF V600E/K PIK3CA wild-type | melanoma | no benefit | Idelalisib | Preclinical | Actionable | In a preclinical study, Zydelig (idelalisib) did not inhibit proliferation of melanoma cell lines harboring BRAF V600E/K and wild-type PIK3CA in culture (PMID: 26137449). | 26137449 |
BRAF V600E/K PIK3CA wild-type | melanoma | sensitive | Dactolisib + Selumetinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Koselugo (selumetinib) and BEZ235 combination treatment inhibited proliferation of melanoma cell lines harboring BRAF V600E/K and wild-type PIK3CA in culture, and synergistically inhibited tumor growth in cell line xenograft models (PMID: 26137449). | 26137449 |
BRAF V600E/K PIK3CA wild-type | melanoma | no benefit | TGX-221 | Preclinical | Actionable | In a preclinical study, TGX-221 did not inhibit proliferation of melanoma cell lines harboring BRAF V600E/K and wild-type PIK3CA in culture (PMID: 26137449). | 26137449 |
BRAF V600E/K PIK3CA wild-type | melanoma | sensitive | Selumetinib + ZSTK474 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Selumetinib (AZD6244) and ZSTK474 combination treatment inhibited proliferation of melanoma cell lines harboring BRAF V600E/K and wild-type PIK3CA in culture, and synergistically inhibited tumor growth in cell line xenograft models (PMID: 26137449). | 26137449 |
BRAF V600E/K PIK3CA wild-type | melanoma | sensitive | Vemurafenib + ZSTK474 | Preclinical | Actionable | In a preclinical study, ZSTK474 and Zelboraf (vemurafenib) worked synergistically to inhibit proliferation of melanoma cell lines harboring BRAF V600E/K and wild-type PIK3CA in culture (PMID: 26137449). | 26137449 |
BRAF V600E/K PIK3CA wild-type | melanoma | sensitive | Selumetinib + Vemurafenib | Preclinical | Actionable | In a preclinical study, Selumetinib (AZD6244) and Zelboraf (vemurafenib) worked synergistically to inhibit proliferation of melanoma cell lines harboring BRAF V600E/K and wild-type PIK3CA in culture (PMID: 26137449). | 26137449 |
BRAF V600E/K PIK3CA wild-type | melanoma | sensitive | Dactolisib + Vemurafenib | Preclinical | Actionable | In a preclinical study, BEZ235 and Zelboraf (vemurafenib) worked synergistically to inhibit proliferation of melanoma cell lines harboring BRAF V600E/K and wild-type PIK3CA in culture (PMID: 26137449). | 26137449 |
PIK3CA wild-type PTEN loss | breast cancer | resistant | AZD8835 | Preclinical | Actionable | In a preclinical study, human breast cancer cells with wild-type PIK3CA and loss of PTEN were resistant to growth inhibition by AZD8835 in culture (PMID: 26839307). | 26839307 |
PIK3CA wild-type PTEN loss | breast cancer | no benefit | Everolimus + Selumetinib | Preclinical - Cell culture | Actionable | In a preclinical study, breast cancer cells harboring PIK3CA wild-type and PTEN loss did not demonstrate any benefit when treated with a combination of Afinitor (everolimus) and Selumetinib (AZD6244) (PMID: 21358673). | 21358673 |
PIK3CA wild-type PTEN loss | breast cancer | no benefit | Everolimus + U0126 | Preclinical - Cell culture | Actionable | In a preclinical study, breast cancer cells harboring PIK3CA wild-type and PTEN loss did not demonstrate any benefit when treated with a combination of Afinitor (everolimus) and U0126 (PMID: 21358673). | 21358673 |
PIK3CA wild-type PTEN loss | breast cancer | sensitive | Torkinib + U0126 | Preclinical - Cell culture | Actionable | In a preclinical study, breast cancer cells harboring PIK3CA wild-type and PTEN loss demonstrated sensitivity to the combination treatment of Torkinib (PP242) and U0126 in culture (PMID: 21358673). | 21358673 |
PIK3CA wild-type PTEN loss | breast cancer | sensitive | Selumetinib + Torkinib | Preclinical - Cell culture | Actionable | In a preclinical study, breast cancer cells harboring PIK3CA wild-type and PTEN loss demonstrated sensitivity to the combination treatment of Torkinib (PP242) and Selumetinib (AZD6244) in culture (PMID: 21358673). | 21358673 |
NRAS mut PIK3CA wild-type | colorectal cancer | predicted - sensitive | TAK-733 | Preclinical - Cell culture | Actionable | In a preclinical study, colorectal cancer cell lines harboring mutations in KRAS or NRAS and with wild-type PIK3CA demonstrated a trend toward increased sensitivity to TAK-733 in culture (PMID: 26439693). | 26439693 |
BRAF mut PIK3CA wild-type | colorectal cancer | predicted - sensitive | TAK-733 | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, mutations in BRAF, KRAS, or NRAS were associated with sensitivity to TAK-733 in colorectal cancer cell lines in culture, and patient-derived xenograft models harboring KRAS or BRAF mutations with wild-type PIK3CA demonstrated a trend toward higher tumor growth inhibition following TAK-733 treatment (PMID: 26439693). | 26439693 |
PIK3CA wild-type PTEN pos | head and neck squamous cell carcinoma | predicted - sensitive | Cetuximab + Cisplatin | Clinical Study - Cohort | Actionable | In a clinical study, combination of Erbitux (cetuximab) with Platinol (cisplatin) tended to improve progression-free survival compared to placebo in PTEN-expressing, PIK3CA wild-type head and neck squamous cell carcinoma patients (HR=0.54, p=0.0502) by multivariable analysis, but not in PTEN null or PIK3CA mutated patients (HR=0.76, p=0.54) (PMID: 30926065). | 30926065 |
PIK3CA act mut | Advanced Solid Tumor | sensitive | Afuresertib | Preclinical | Actionable | In a preclinical study, various tumor cell lines harboring PI3KCA activating mutations demonstrated increased sensitivity to Afuresertib (GSK2110183) in cultured cells (PMID: 24978597). | 24978597 |
PIK3CA act mut | lung non-small cell carcinoma | predicted - resistant | Osimertinib | Case Reports/Case Series | Actionable | In a retrospective analysis, activating PIK3CA mutations were identified in 6 of 100 patients with non-small cell lung cancer at treatment discontinuation of Tagrisso (osimertinib) (PMID: 31839416). | 31839416 |
PIK3CA act mut | ovarian clear cell adenocarcinoma | sensitive | Dactolisib | Preclinical | Actionable | In a preclinical study, BEZ235 demonstrated efficacy in mouse xenograft models of ovarian clear cell adenocarcinoma with PIK3CA mutations (PMID: 24927217). | 24927217 |
PIK3CA act mut | lung squamous cell carcinoma | predicted - sensitive | Buparlisib | Preclinical - Pdx | Actionable | In a preclinical study, Buparlisib (BKM120) treatment resulted in inhibition of AKT and S6 phosphorylation and durable responses in 4/5 lung squamous cell carcinoma patient-derived xenograft (PDX) models harboring PIK3CA E545K or E542K mutations, 3 that also had PIK3CA amplification and 1 with PTEN loss (PMID: 30093452). | 30093452 |
PIK3CA act mut | female reproductive organ cancer | predicted - sensitive | Alpelisib | Clinical Study | Actionable | In a clinical study, Piqray (alpelisib) treatment was well tolerated and demonstrated activity in patients with advanced gynecologic cancers harboring activating mutations in PIK3CA, resulting in an overall response rate of 28% (10/36, all partial responses), a disease control rate of 61% (22/36), including stable disease in 12 patients, a median duration of response of 13 months, and a median progression-free survival of 6.3 months (PMID: 38518529; NCT04085653). | 38518529 |
PIK3CA act mut | endometrial cancer | predicted - sensitive | Alpelisib | Clinical Study | Actionable | In a clinical study, Piqray (alpelisib) treatment was well tolerated and demonstrated activity in patients with advanced gynecologic cancer harboring activating mutations in PIK3CA and resulted in an overall response rate (ORR) of 28% (10/36), with an ORR of 35% (6/17, all partial responses), disease control rate of 71% (12/17), median duration of response of 13 mo, and median progression-free survival of 7.8 mo in endometrial cancer patients (PMID: 38518529; NCT04085653). | 38518529 |
PIK3CA act mut | lung squamous cell carcinoma | predicted - sensitive | Alpelisib | Preclinical - Pdx | Actionable | In a preclinical study, Alpelisib (BYL719) treatment resulted in responses in multiple lung squamous cell carcinoma patient-derived xenograft (PDX) models harboring PIK3CA E545K or E542K mutations, including models with PIK3CA amplification or PTEN loss (PMID: 30093452). | 30093452 |
PIK3CA act mut | Advanced Solid Tumor | sensitive | Everolimus | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Afinitor (everolimus) demonstrated efficacy in multiple cancer cell lines in culture and xenograft models with PIK3CA activating mutations (PMID: 20664172). | 20664172 |
PIK3CA act mut | lung non-small cell carcinoma | sensitive | Pictilisib | Preclinical - Cell line xenograft | Actionable | In preclinical studies, the PI3K inhibitor GDC-0941 demonstrated efficacy against NSCLC tumor cell lines in culture and in xenograft models harboring alterations in the PI3K pathway (PMID: 23136191). | 23136191 |
PIK3CA act mut | breast cancer | sensitive | MK2206 | Preclinical | Actionable | In a preclinical study, breast cancer cell lines harboring activating mutations in PIK3CA had increased sensitivity to MK2206 in cell culture (PMID: 22932669). | 22932669 |
PIK3CA act mut | Advanced Solid Tumor | predicted - sensitive | Temsirolimus | Phase II | Actionable | In a Phase II trial (TAPUR), Torisel (temsirolimus) treatment resulted in an objective response rate of 11% (3/28, 3 partial responses) and a disease control rate of 29% in patients with advanced solid tumors other than breast cancer harboring PIK3CA mutations, with PIK3CA H1047R/L (n=3), E545K (n=2), and E542K (n=2) as the most common mutation in patients achieved disease control (J Clin Oncol 41, 2023 (suppl 16; abstr 3117); NCT02693535). | detail... |
PIK3CA act mut | Advanced Solid Tumor | sensitive | BAY1125976 | Preclinical | Actionable | In a preclinical study, BAY1125976 demonstrated anti-tumor efficacy in multiple xenograft tumor models of different cancers with PIK3CA mutations or PTEN deletions and displayed synergy with other anti-cancer therapies (Cancer Res 2013;73(8 Suppl):Abstract nr 2050). | detail... |
PIK3CA act mut | breast cancer | sensitive | Copanlisib | Case Reports/Case Series | Actionable | In a Phase I clinical trial, treatment with Aliqopa (copanlisib) resulted in partial response in one and stable disease in another patient with breast cancer harboring activating PIK3CA mutations (PMID: 27672108; NCT00962611). | 27672108 |
PIK3CA act mut | breast cancer | sensitive | Copanlisib | Preclinical | Actionable | In a preclinical study, breast cancer cell lines with a PIK3CA activating mutation and/or ERBB2 (HER2) over expression demonstrated increased sensitivity to inhibition of proliferation by Aliqopa (copanlisib) in culture, compared to ERBB2 (HER2)-negative and wild-type PIK3CA cell lines (PMID: 24170767). | 24170767 |
PIK3CA act mut | Advanced Solid Tumor | predicted - sensitive | Copanlisib | Phase II | Actionable | In a Phase II trial (NCI MATCH EAY131-Z1F), Aliqopa (copanlisib) treatment resulted in an objective response rate of 16% (4/25, all partial response), a clinical benefit rate of 36% (9/25), a median progression-free survival of 3.4 months, and a median overall survival of 5.9 months in patients with advanced solid tumors harboring activating PIK3CA mutations (PMID: 35133871; NCT02465060). | 35133871 |
PIK3CA act mut | Advanced Solid Tumor | conflicting | Taselisib | Phase II | Actionable | In a Phase II trial (MATCH), Taselisib (GDC-0032) treatment resulted in limited efficacy in heavily pretreated patients with advanced solid tumors harboring PIK3CA activating mutations, with an objective response rate of 0% (0/61) after a median follow-up of 35.7 months, stable disease in 52% (32/61), a median progression-free survival of 3.1 months, and a median overall survival of 7.2 months (PMID: 35138919; NCT02465060). | 35138919 |
PIK3CA act mut | Advanced Solid Tumor | conflicting | Taselisib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Taselisib (GDC-0032) effectively suppressed growth of multiple tumor types in cell line xenograft models, with greater selectivity for PIK3CA activating mutants (PMID: 23662903). | 23662903 |
PIK3CA act mut | Advanced Solid Tumor | sensitive | Metformin | Preclinical | Actionable | In a preclinical study, Glucophage (metformin) demonstrated efficacy in treating dietary restriction-resistant human xenograft tumors harboring a PIK3CA-activating mutation (PMID: 23986086). | 23986086 |
PIK3CA act mut | head and neck squamous cell carcinoma | sensitive | Gedatolisib | Preclinical | Actionable | In a preclinical study, PF-05212384 decreased viability of head and neck squamous carcinoma cells harboring a PIK3CA activating mutation in cell culture (PMID: 24823695). | 24823695 |
PIK3CA act mut | endometrial cancer | no benefit | LY3023414 | Phase II | Actionable | In a Phase II trial, patients with advanced endometrial cancer harboring a PI3K pathway mutation, including PIK3CA activating mutations, demonstrated only a modest clinical benefit with an overall response rate of 16% (4/25), a clinical benefit rate of 28% (7/25) at 12 weeks, a progression-free survival of 2.5 months, and overall survival of 9.2 months when treated with LY3023414 (PMID: 31880826; NCT01775072). | 31880826 |
PIK3CA act mut | Advanced Solid Tumor | no benefit | LY3023414 | Case Reports/Case Series | Actionable | In a Phase II trial (NCI-COG Pediatric MATCH), Samotolisib (LY3023414) treatment resulted in no objective responses in pediatric patients with advanced solid tumors harboring PI3K/mTOR pathway mutations, including PTEN (n=6), PIK3CA (n=5), TSC1 (n=2), TSC2 (n=3), and PIK3R1 (n=1), and resulted in a 3-month progression-free survival of 12%, a 6-month overall survival of 44%, and a 12-month overall survival of 15% (PMID: 39298693; NCT03155620). | 39298693 |
PIK3CA act mut | triple-receptor negative breast cancer | no benefit | Ipatasertib + Paclitaxel | Phase II | Actionable | In a Phase II trial (LOTUS), Ipatasertib (GDC-0068) in combination with Abraxane (paclitaxel) resulted a median progression free survival of 6.2 vs 4.9 months with placebo in triple-receptor negative breast cancer patients harboring activating mutations in PIK3CA or AKT1, or inactivating mutations in PTEN (PMID: 28800861; NCT02162719). | 28800861 |
PIK3CA act mut | triple-receptor negative breast cancer | no benefit | Ipatasertib + Paclitaxel | Phase III | Actionable | In a Phase III trial (IPATunity 130), the addition of Ipatasertib (GDC-0068) to treatment with Abraxane (paclitaxel) did not result in improved progression-free survival in patients with triple-negative breast cancer harboring PIK3CA and/or AKT activating mutations or PTEN alterations, with a median PFS of 7.4 months with Ipatasertib (GDC-0068) plus Abraxane (paclitaxel) vs. 6.1 months with placebo plus Abraxane (paclitaxel) (SABCS Meeting 2020, Abstract GS3-04; NCT03337724). | detail... |
PIK3CA act mut | Advanced Solid Tumor | sensitive | Ipatasertib + Paclitaxel | Phase I | Actionable | In a Phase Ib trial, the combination of Ipatasertib (GDC-0068) and Taxol (paclitaxel) resulted in an objective response rate (ORR) of 8.0% (2/25, partial responses) in patients with advanced solid tumors (n=25), and ORR was proportionally higher in patients harboring activating PIK3CA mutations (2/6) compared to patients without PIK3CA activating mutations (0/19) (PMID: 32205017; NCT01362374). | 32205017 |
PIK3CA act mut | triple-receptor negative breast cancer | predicted - sensitive | Capivasertib + Paclitaxel | Phase II | Actionable | In a Phase II trial (PAKT), addition of Truqap (capivasertib) to Taxol (paclitaxel) as first-line therapy significantly improved median progression-free survival (9.3 vs 3.7 months, HR=0.30, p=0.01) and reduced risk (66%, HR=0.34, p=0.04) compared to Taxol (paclitaxel) alone in patients with metastatic triple-negative breast cancer harboring activating mutations in AKT1 (E17K, n=1) or PIK3CA (n=17), or inactivating mutations or gene loss in PTEN (n=13) (PMID: 31841354; NCT02423603). | 31841354 |
PIK3CA act mut | Advanced Solid Tumor | sensitive | GSK1059615 | Preclinical | Actionable | In a preclinical study, solid tumor cell lines harboring PIK3CA activating mutations demonstrated increased sensitivity to GSK1059615 in culture (Clin Cancer Res October 1, 2008 14; B37). | detail... |
PIK3CA act mut | Her2-receptor negative breast cancer | predicted - sensitive | Alpelisib + Nab-paclitaxel | Clinical Study - Cohort | Actionable | In a Phase I/II trial, Piqray (Alpelisib) and Abraxane (nab-paclitaxel) combination treatment resulted in improved clinical benefit rate (100% vs 68%; OR=1.47, P=0.013) and median progression-free survival (11.9 vs 7.5 mo.; HR=0.44, P=0.027) and longer median overall survival (26.7 vs. 14.9 mo.; HR=0.59, P=0.19) in patients with ERBB2 (HER2)-negative metastatic breast cancer harboring activating PIK3CA mutations compared to patients without PIK3CA mutations (PMID: 33602685; NCT02379247). | 33602685 |
PIK3CA act mut | breast cancer | predicted - sensitive | MK2206 + Ridaforolimus | Phase I | Actionable | In a Phase I clinical trial, Ridaforolimus in combination with MK-2206 demonstrated clinical activity in breast cancer patients expressing a PI3K pathway dependent gene expression signature, with complete response in 14.3% (2/14), partial response in 12.5% (2/16), and 2 patients achieving stable disease (PMID: 26187616). | 26187616 |
PIK3CA act mut | lung small cell carcinoma | predicted - sensitive | Navitoclax + Pictilisib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination of Navitoclax (ABT-263) and GDC-0941 resulted in increased tumor growth delay and apoptosis in a small cell lung cancer cell line xenograft model harboring a PIK3CA activating mutation compared to either drug alone (PMID: 27197306). | 27197306 |
PIK3CA act mut | castration-resistant prostate carcinoma | predicted - sensitive | CC-115 + Enzalutamide | Case Reports/Case Series | Actionable | In a Phase Ib trial, Xtandi (enzalutamide) plus CC-115 was safe and led to a PSA reduction >= 50% (PSA50) in 80% (32/40) and >=90% (PSA90) in 58% (23/40) of metastatic castration-resistant prostate cancer patients at 12 weeks, and patients with PIK3CA activating mutations or PTEN or TSC1/2 loss of function (n=16) achieved a PSA50, PSA90, and median radiographic progression-free survival of 94%, 63%, and 19.6 mo vs 67%, 47%, and 22.1 mo in PI3K pathway wild-type patients (n=15) (PMID: 37980367; NCT02833883). | 37980367 |
PIK3CA act mut | estrogen-receptor positive breast cancer | predicted - sensitive | Capivasertib + Tamoxifen | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Truqap (capivasertib) and 4-hydroxytamoxifen (4-OHT) worked synergistically or additively to inhibit growth of several estrogen receptor-positive breast cancer cell lines in culture, including cell lines with PIK3CA activating mutations, and overcame tamoxifen resistance in a resistant cell line (PMID: 26116361). | 26116361 |
PIK3CA act mut | breast cancer | no benefit | Dactolisib + Venetoclax | Preclinical - Cell culture | Actionable | In a preclinical study, inhibition of Pi3k signaling by BEZ235 did not sensitize breast cancer cell lines harboring PIK3CA activating mutations to Venclexta (venetoclax) in culture (PMID: 27974663). | 27974663 |
PIK3CA act mut | breast cancer | predicted - sensitive | Dactolisib + WEHI-539 | Preclinical - Cell culture | Actionable | In a preclinical study, inhibition of Pi3k signaling by BEZ235 sensitized breast cancer cell lines harboring PIK3CA activating mutations to WEHI-539 in culture (PMID: 27974663). | 27974663 |
PIK3CA act mut | breast cancer | no benefit | Buparlisib + WEHI-539 | Preclinical - Cell culture | Actionable | In a preclinical study, Buparlisib (BKM120) did not sensitize breast cancer cell lines harboring PIK3CA activating mutations to WEHI-539 in culture (PMID: 27974663). | 27974663 |
PIK3CA act mut | breast cancer | no benefit | Alpelisib + WEHI-539 | Preclinical - Cell culture | Actionable | In a preclinical study, Alpelisib (BYL719) did not sensitize breast cancer cell lines harboring PIK3CA activating mutations to WEHI-539 in culture (PMID: 27974663). | 27974663 |
PIK3CA act mut | breast cancer | predicted - sensitive | Torin 1 + WEHI-539 | Preclinical - Cell culture | Actionable | In a preclinical study, the ATP-competitive mTORC1/2 inhibitor Torin1 sensitized breast cancer cell lines harboring PIK3CA activating mutations to WEHI-539 in culture (PMID: 27974663). | 27974663 |
PIK3CA act mut | breast cancer | predicted - sensitive | Vistusertib + WEHI-539 | Preclinical - Cell culture | Actionable | In a preclinical study, the ATP-competitive mTORC1/2 inhibitor Vistusertib (AZD2014) sensitized breast cancer cell lines harboring PIK3CA activating mutations to WEHI-539 in culture (PMID: 27974663). | 27974663 |
PIK3CA act mut | breast cancer | predicted - sensitive | Sapanisertib + WEHI-539 | Preclinical - Cell culture | Actionable | In a preclinical study, the ATP-competitive mTORC1/2 inhibitor Sapanisertib (MLN0128) sensitized breast cancer cell lines harboring PIK3CA activating mutations to WEHI-539 in culture (PMID: 27974663). | 27974663 |
PIK3CA act mut | triple-receptor negative breast cancer | predicted - sensitive | Bevacizumab + Doxorubicin + Everolimus | Phase I | Actionable | In a Phase I trial, triple-receptor negative breast cancer patients, including those with PIK3CA activating mutations, demonstrated an overall response rate of 21% (11/52) and clinical benefit rate of 40% (21/52) when treated with a combination of Avastin (bevacizumab), Adriamycin (doxorubicin), and either Afinitor (everolimus) or Torisel (temsirolimus) (PMID: 27893038). | 27893038 |
PIK3CA act mut | triple-receptor negative breast cancer | predicted - sensitive | Bevacizumab + Doxorubicin + Temsirolimus | Phase I | Actionable | In a Phase I trial, triple-receptor negative breast cancer patients, including those with PIK3CA activating mutations, demonstrated an overall response rate of 21% (11/52) and clinical benefit rate of 40% (21/52) when treated with a combination of Avastin (bevacizumab), Adriamycin (doxorubicin), and either Afinitor (everolimus) or Torisel (temsirolimus) (PMID: 27893038). | 27893038 |
PIK3CA act mut | head and neck squamous cell carcinoma | predicted - sensitive | AZD8055 + Cetuximab | Preclinical - Pdx | Actionable | In a preclinical study, two head and neck squamous cell carcinoma patient-derived xenograft (PDX) models harboring a PIK3CA activating mutation demonstrated greater delayed tumor growth when treated with a combination of AZD8055 and Erbitux (cetuximab) compared to either agent alone (PMID: 28446642). | 28446642 |
PIK3CA act mut | Advanced Solid Tumor | predicted - sensitive | LY3023414 + Prexasertib | Phase I | Actionable | In a Phase Ib trial, the combination therapy of Samotolisib (LY3023414) and Prexasertib (LY2606368) resulted in an overall response rate of 13.3% (2/15; 2 partial responses) in patients with an advanced solid tumor harboring a PIK3CA activating mutation of either H1047R, H1047L, E542K, or E545K (PMID: 33495309; NCT02124148). | 33495309 |
PIK3CA act mut | Advanced Solid Tumor | no benefit | Atezolizumab + Ipatasertib | Phase II | Actionable | In a Phase II trial (CRAFT), treatment with Ipatasertib (GDC-0068) plus Tecentriq (atezolizumab) demonstrated safety but limited clinical benefit in advanced solid tumor patients harboring PI3K-AKT pathway mutations (n=13), including PTEN deletion/inactivating mutations or activating mutations in PIK3CA or AKT1, with a partial response in a breast cancer patient with AKT1 E17K and stable disease in a prostate cancer patient with PTEN loss (Ann Oncol (2023) 34 (suppl_2): S256-S257;NCT04551521). | detail... |
PIK3CA act mut | Advanced Solid Tumor | predicted - sensitive | Copanlisib + Nivolumab | Phase II | Actionable | In a Phase II trial (BaCoN), treatment with the combination of Aliqopa (copanlisib) and Opdivo (nivolumab) was well tolerated in patients with advanced solid tumors harboring an activating mutation in PIK3CA, and resulted in a complete response/partial response (CR/PR) in 27% (4/15, 1 cPR, 3 uCR/PR) and a clinical benefit rate (CR or PR or stable disease > 4 months) of 40% (Ann Oncol 34 (2023): S487-S488; NCT04317105). | detail... |
PIK3CA act mut | Advanced Solid Tumor | predicted - sensitive | Docetaxel + Ipatasertib | Phase I | Actionable | In a Phase Ib trial, the combination of Ipatasertib (GDC-0068) and Taxotere (docetaxel) resulted in an objective response rate (ORR) of 7.7% (2/26, partial responses) in patients with advanced solid tumors (n=26), and ORR was proportionally higher in patients harboring activating PIK3CA mutations (1/4) compared to patients without PIK3CA activating mutations (1/22) (PMID: 32205017; NCT01362374). | 32205017 |
PIK3CA act mut | Advanced Solid Tumor | predicted - sensitive | Fluorouracil + Ipatasertib + Leucovorin + Oxaliplatin | Phase I | Actionable | In a Phase Ib trial, the combination of Ipatasertib (GDC-0068) and mFOLFOX6 resulted in an objective response rate (ORR) of 6.1% (2/33, partial responses) in patients with advanced solid tumors (n=33), and ORR was proportionally higher in patients harboring activating PIK3CA mutations (1/4) compared to in patients without PIK3CA activating mutations (1/29) (PMID: 32205017; NCT01362374). | 32205017 |
PIK3CA act mut | estrogen-receptor positive breast cancer | predicted - sensitive | Palbociclib + Taselisib | Phase I | Actionable | In a Phase Ib trial (PIPA), the combination of Ibrance (palbociclib) with Taselisib (GDC-0032) was well tolerated in estrogen-receptor negative breast cancer patients harboring PIK3CA activating mutations and resulted in an objective response rate of 10% (1/10), a clinical benefit rate of 30% (4/10), and a median progression-free survival of 3.6 months (PMID: 32958578; NCT02389842). | 32958578 |
PIK3CA act mut | Advanced Solid Tumor | predicted - sensitive | Palbociclib + Taselisib | Phase I | Actionable | In a Phase Ib trial (PIPA), the combination of Ibrance (palbociclib) with Taselisib (GDC-0032) was well tolerated in patients with advanced solid tumors harboring PIK3CA activating mutations and resulted in an objective response rate of 0% (0/12), a clinical benefit rate of 16.7% (2/12), and a median progression-free survival of 3.8 months (PMID: 32958578; NCT02389842). | 32958578 |
PIK3CA act mut | Advanced Solid Tumor | no benefit | TAS-117 | Phase II | Actionable | In a Phase II trial, TAS-117 treatment in advanced solid tumor patients with PIK3CA activating mutations (n=12) or AKT1 E17K (n=1) refractory to standard treatment had minimal activity, and led to an overall response rate of 8% (1/13), disease control rate of 23% (3/13), median progression-free survival of 1.4 months (mo), and a median overall survival of 4.8 mo, however due to poor accrual and lack of durable response to TAS-117 early termination of study was recommended (PMID: 33723724; NCT03017521). | 33723724 |
PIK3CA act mut | Advanced Solid Tumor | predicted - sensitive | RLY-2608 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, RLY-2608 treatment led to inhibition of cell viability in a panel of cancer cell lines harboring PIK3CA hotspot mutations, and led to tumor regression or stasis in cell line xenograft models (Mol Cancer Ther 2021;20(12 Suppl):Abstract nr P251). | detail... |
PIK3CA act mut PTEN dec exp | renal cell carcinoma | no benefit | Everolimus | Case Reports/Case Series | Actionable | In a retrospective analysis from a Phase II clinical trial, patients with metastatic renal cell carcinoma treated with Afinitor (everolimus) had no difference in progression-free survival when stratified by the presence (n=21) or absence (n=17) of PIK3CA activating mutations (PMID: 26951309). | 26951309 |
PIK3CA act mut PTEN dec exp | renal cell carcinoma | no benefit | Apitolisib | Case Reports/Case Series | Actionable | In a retrospective analysis from a Phase II clinical trial, patients with metastatic renal cell carcinoma treated with Apitolisib (GDC-0980) had no difference in progression-free survival when stratified by the presence (n=21) or absence (n=15) of PIK3CA activating mutation and/or decreased Pten expression (PMID: 26951309). | 26951309 |
PIK3CA act mut PTEN wild-type | breast cancer | sensitive | Everolimus | Preclinical - Cell culture | Actionable | In a preclinical study, 8/9 breast cancer cell lines harboring a PIK3CA activating mutation and PTEN wild-type demonstrated sensitivity to treatment with Afinitor (everolimus) in culture, resulting in decreased cell viability (PMID: 21358673). | 21358673 |
PIK3CA act mut PTEN wild-type | breast cancer | sensitive | Torkinib | Preclinical - Cell culture | Actionable | In a preclinical study, 9/9 breast cancer cell lines harboring a PIK3CA activating mutation and PTEN wild-type demonstrated sensitivity to treatment with Torkinib (PP242) in culture, resulting in decreased cell viability (PMID: 21358673). | 21358673 |
CDKN2A loss PIK3CA act mut | lung squamous cell carcinoma | predicted - sensitive | Buparlisib + Palbociclib | Preclinical - Pdx | Actionable | In a preclinical study, treatment with the combination of Buparlisib (BYL719) and Ibrance (palbociclib) resulted in increased tumor growth inhibition compared to either agent alone in patient-derived xenograft (PDX) models of lung squamous cell carcinoma harboring PIK3CA E542K or E545K mutations with p16 (CDKN2A) loss, including models that also had either PIK3CA amplification or PTEN loss (PMID: 30093452). | 30093452 |
PIK3CA act mut TSC1 del | estrogen-receptor positive breast cancer | resistant | Alpelisib | Preclinical - Cell culture | Actionable | In a preclinical study, PIK3CA-mutant, ESR1 (ER)-positive breast cancer cells with knockout of TSC1 demonstrated resistance to growth inhibition by Piqray (alpelisib) in culture, and decreased sensitivity to Piqray (alpelisib) in a cell line xenograft model (PMID: 33685991). | 33685991 |
PIK3CA act mut TSC1 del | estrogen-receptor positive breast cancer | resistant | Taselisib | Preclinical - Cell culture | Actionable | In a preclinical study, PIK3CA-mutant, ESR1 (ER)-positive breast cancer cell lines with knockout of TSC1 were resistant to treatment with Taselisib (GDC-0032) in culture (PMID: 33685991). | 33685991 |
PIK3CA act mut TSC2 del | estrogen-receptor positive breast cancer | resistant | Alpelisib | Preclinical - Cell culture | Actionable | In a preclinical study, PIK3CA-mutant, ESR1 (ER)-positive breast cancer cell lines with knockout of TSC2 were resistant to treatment with Piqray (alpelisib) in culture (PMID: 33685991). | 33685991 |
PIK3CA act mut TSC2 del | estrogen-receptor positive breast cancer | resistant | Taselisib | Preclinical - Cell culture | Actionable | In a preclinical study, PIK3CA-mutant, ESR1 (ER)-positive breast cancer cell lines with knockout of TSC2 were resistant to treatment with Taselisib (GDC-0032) in culture (PMID: 33685991). | 33685991 |
PIK3CA E542K | breast cancer | sensitive | Trametinib | Preclinical | Actionable | In a preclinical study, Mekinist (trametinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA E542K in culture (PMID: 26627007). | 26627007 |
PIK3CA E542K | breast cancer | sensitive | Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, a hormone breast cancer cell line harboring PIK3CA E542K was sensitive to Miransertib (ARQ092) in culture, demonstrating inhibition of cell growth (PMID: 26469692). | 26469692 |
PIK3CA E542K | stomach cancer | sensitive | Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, Miransertib (ARQ092) treatment induced cell death and inhibited proliferation of a gastric cancer cell line harboring PIK3CA E542K in culture (PMID: 32439931). | 32439931 |
PIK3CA E542K | gastrointestinal system cancer | sensitive | Capivasertib | Preclinical - Cell culture | Actionable | In a preclinical study, gastric cancer cells harboring PIK3CA E542K demonstrated sensitivity to the AKT inhibitor Truqap (capivasertib), resulting in decreased proliferation in culture (PMID: 24088382). | 24088382 |
PIK3CA E542K | stomach cancer | sensitive | Capivasertib | Case Reports/Case Series | Actionable | In a clinical case study, treatment with Truqap (capivasertib) in a patient with gastric cancer harboring PIK3CA E542K resulted in a partial response, and in preclinical studies, led to decreased cell proliferation in a gastric cancer cell line harboring PIK3CA E542K (PMID: 32070411). | 32070411 |
PIK3CA E542K | breast cancer | sensitive | Dactolisib | Preclinical | Actionable | In a preclinical study, BEZ235 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA E542K in culture (PMID: 26627007). | 26627007 |
PIK3CA E542K | breast cancer | resistant | Buparlisib | Preclinical - Cell culture | Actionable | In a preclinical study, breast cancer cells expressing PIK3CA E542K demonstrated resistance to treatment with Buparlisib (BKM120) in culture (PMID: 29636477). | 29636477 |
PIK3CA E542K | breast cancer | sensitive | Alpelisib | Preclinical - Cell culture | Actionable | In a preclinical study, Alpelisib (BYL719) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA E542K in culture (PMID: 26627007). | 26627007 |
PIK3CA E542K | Her2-receptor negative breast cancer | no benefit | Everolimus | Phase III | Actionable | In a retrospective analysis of a Phase III trial (BOLERO-2), Afinitor (everolimus) demonstrated comparable progression-free survival benefit in patients with hormone receptor-positive, Erbb2 (Her2)-negative breast cancer harboring wild-type (HR=0.43) or mutant (HR=0.37) PIK3CA, similar benefit was observed in subgroups harboring PIK3CA H1047R (HR=0.37) and PIK3CA E545K/E542K (HR=0.30) (PMID: 28183140; NCT00863655). | 28183140 |
PIK3CA E542K | stomach cancer | predicted - sensitive | Ipatasertib | Preclinical - Cell culture | Actionable | In a preclinical study, Ipatasertib (GDC-0068) treatment did not increase cell death but inhibited proliferation of a gastric cancer cell line harboring PIK3CA E542K in culture (PMID: 32439931). | 32439931 |
PIK3CA E542K | head and neck squamous cell carcinoma | predicted - sensitive | Apitolisib | Case Reports/Case Series | Actionable | In a Phase I trial, Apitolisib (GDC-0980) treatment resulted in a partial response in a patient with head and neck squamous cell carcinoma harboring a PIK3CA E542K mutation (PMID: 26787751; NCT00854152). | 26787751 |
PIK3CA E542K | breast cancer | sensitive | Lapatinib | Preclinical | Actionable | In a preclinical study, Tykerb (lapatinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA E542K in culture (PMID: 26627007). | 26627007 |
PIK3CA E542K | breast cancer | sensitive | MK2206 | Preclinical | Actionable | In a preclinical study, MK2206 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA E542K in culture (PMID: 26627007). | 26627007 |
PIK3CA E542K | papillary thyroid carcinoma | sensitive | MK2206 | Preclinical - Cell culture | Actionable | In a preclinical study, MK2206 inhibited AKT activation, proliferation, and growth of thyroid cancer cell lines with PI3K/AKT pathway alterations in culture, including a papillary thyroid cancer cell line harboring PIK3CA E542K (PMID: 21289267). | 21289267 |
PIK3CA E542K | stomach cancer | sensitive | MK2206 | Preclinical - Cell culture | Actionable | In a preclinical study, MK2206 treatment induced cell death and inhibited proliferation of a gastric cancer cell line harboring PIK3CA E542K in culture (PMID: 32439931). | 32439931 |
PIK3CA E542K | breast cancer | sensitive | Neratinib | Preclinical | Actionable | In a preclinical study, Nerlynx (neratinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA E542K in culture (PMID: 26627007). | 26627007 |
PIK3CA E542K | Advanced Solid Tumor | sensitive | Sirolimus | Preclinical | Actionable | In a preclinical study, Rapamune (sirolimus) demonstrated efficacy in inhibiting transformation of cultured cells containing PIK3CA E542K mutations (PMID: 15647370). | 15647370 |
PIK3CA E542K | colon adenocarcinoma | sensitive | VS-5584 | Preclinical | Actionable | In preclinical studies, VS-5584 demonstrated efficacy in a variety of cancer cell lines, particularly those harboring PIK3CA mutations (PMID: 23270925). | 23270925 |
PIK3CA E542K | endometrial adenocarcinoma | no benefit | Copanlisib | Case Reports/Case Series | Actionable | In a Phase II (NRG-GY008) trial, Aliqopa (copanlisib) was well tolerated but demonstrated limited efficacy, resulted in stable disease in 2 patients with serous endometrial adenocarcinoma harboring PIK3CA E542K (PMID: 31934607). | 31934607 |
PIK3CA E542K | endometrial serous adenocarcinoma | predicted - sensitive | Copanlisib | Case Reports/Case Series | Actionable | In a Phase II trial (NCI MATCH EAY131-Z1F), Aliqopa (copanlisib) treatment resulted in a partial response and progression-free survival of 5.4 months and an overall survival of 8.2 months in a patient with endometrial serous adenocarcinoma harboring PIK3CA E542K (PMID: 35133871; NCT02465060). | 35133871 |
PIK3CA E542K | lung squamous cell carcinoma | no benefit | Taselisib | Case Reports/Case Series | Actionable | In a Phase I (SWOG S1400B) trial, Taselisib (GDC-0032) treatment did not meet its primary endpoint for response rate in patients with lung squamous cell carcinoma harboring PIK3CA mutations, resulting in no responses in patients harboring PIK3CA E542K (n=6) (PMID: 31158500; NCT02785913). | 31158500 |
PIK3CA E542K | colorectal cancer | sensitive | PD-0325901 + Pictilisib | Preclinical - Cell line xenograft | Actionable | In preclinical studies, the combination of GDC-0941 and PD-0325901 (PI3K and MEK inhibitors, respectively) inhibited tumor growth in colorectal cancer cell line xenograft models (PMID: 24339963). | 24339963 |
PIK3CA E542K | colorectal cancer | predicted - sensitive | Cetuximab + Irinotecan | Case Reports/Case Series | Actionable | In a retrospective analysis, treatment with the combination of Erbitux (cetuximab) and Camptosar (irinotecan) resulted in a partial response in 50% (1/2) and stable disease in 50% (1/2) of colorectal carcinoma patients harboring a PIK3CA E542K mutation (PMID: 25714871). | 25714871 |
PIK3CA E542K | colorectal cancer | resistant | Cetuximab + Fluorouracil | Preclinical - Cell culture | Actionable | In a preclinical study, colorectal cancer cells over expressing PIK3CA E542K were resistant to Erbitux (cetuximab) and Fluorouracil combination treatment in culture (PMID: 28424201). | 28424201 |
PIK3CA E542K | breast cancer | sensitive | MEN1611 | Preclinical | Actionable | In a preclinical study, MEN1611 (CH5132799) inhibited proliferation of a breast cancer cell line harboring PIK3CA E542K in culture (PMID: 21558396). | 21558396 |
PIK3CA E542K | stomach cancer | predicted - sensitive | GSK690693 | Preclinical - Cell culture | Actionable | In a preclinical study, GSK690693 treatment did not increase cell death but inhibited proliferation of a gastric cancer cell line harboring PIK3CA E542K in culture (PMID: 32439931). | 32439931 |
PIK3CA E542K | stomach cancer | sensitive | ARQ 751 | Preclinical - Cell culture | Actionable | In a preclinical study, ARQ 751 treatment induced cell death and inhibited proliferation of a gastric cancer cell line harboring PIK3CA E542K in culture (PMID: 32439931). | 32439931 |
PIK3CA E542K | high grade glioma | sensitive | Buparlisib + Selumetinib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination therapy of Buparlisib (BKM120) and Koselugo (selumetinib) led to a synergistic effect, resulting in greater growth inhibition of astrocytoma cells expressing PIK3CA E542K than cells with wild-type PIK3CA in culture (PMID: 29975751). | 29975751 |
PIK3CA E542K | papillary thyroid carcinoma | sensitive | MK2206 + Temsirolimus | Preclinical - Cell culture | Actionable | In a preclinical study, MK2206 suppressed activation of AKT induced by Torisel (temsirolimus), and MK2206 and Torisel (temsirolimus) demonstrated synergy in inhibiting growth of a papillary thyroid cancer cell line harboring PIK3CA E542K in culture (PMID: 21289267). | 21289267 |
PIK3CA E542K | cervical squamous cell carcinoma | sensitive | Gemcitabine + LY2780301 | Phase Ib/II | Actionable | In a Phase Ib trial, a patient with cervical squamous cell carcinoma harboring PIK3CA E542K demonstrated a partial response when treated with a combination of LY2780301 and Gemzar (gemcitabine) (PMID: 28750271). | 28750271 |
PIK3CA E542K | head and neck squamous cell carcinoma | predicted - sensitive | Alpelisib + Cetuximab + Radiotherapy | Case Reports/Case Series | Actionable | In a Phase Ib trial, 11 of 11 patients with metastatic head and neck squamous cell carcinoma demonstrated no evidence of disease at 3 to 4 months following treatment with Piqray (alpelisb) in combination with Erbitux (cetuximab) and intensity modulated radiation therapy (IMRT), and PIK3CA E542K was identified in one patient with oropharyngeal squamous cell carcinoma who had a near complete radiologic response within 8 days of starting IMRT (PMID: 31678634). | 31678634 |
PIK3CA E542K | estrogen-receptor positive breast cancer | predicted - sensitive | RLY-2608 | Case Reports/Case Series | Actionable | In a clinical case study, treatment with RLY-2608 resulted in a partial response with disappearance of the soft tissue target lesion, which was ongoing at day 141, in a patient with ESR1/PGR-positive, ERBB2 (HER2)-negative breast cancer harboring PIK3CA E542K (PMID: 37916956; NCT05216432). | 37916956 |
PIK3CA E542K | Her2-receptor positive breast cancer | sensitive | STX-478 | Preclinical - Pdx | Actionable | In a preclinical study, STX-478 inhibited tumor growth of a ERBB2 (HER2)-positive breast cancer patient-derived xenograft (PDX) model harboring PIK3CA E542K (PMID: 37623743). | 37623743 |
PIK3CA E542K | Her2-receptor negative breast cancer | predicted - sensitive | HS-10352 | Case Reports/Case Series | Actionable | In a Phase I trial, HS-10352 treatment resulted in an objective response rate (ORR) of 27.8% (5/18, all partial responses), disease control rate (DCR) of 55.6%, and median progression-free survival (mPFS) of 3.9 mo in HR-positive, ERBB2 (HER2)-negative advanced breast cancer patients overall, and in the 6mg group led to an ORR of 66.7% and DCR of 83.3%, with an ORR of 75.0% (3/4) and DCR of 100% in patients with PIK3CA mutations (E542K, E545K, E545D, H1047L, H1047R) (PMID: 38037839; NCT04631835). | 38037839 |
PIK3CA E542K PTEN loss | lung squamous cell carcinoma | sensitive | Buparlisib | Preclinical - Pdx | Actionable | In a preclinical study, Buparlisib (BKM120) treatment resulted in inhibition of AKT and S6 phosphorylation and durable response in a lung squamous cell carcinoma patient-derived xenograft (PDX) model harboring PIK3CA E542K and PTEN loss (PMID: 30093452). | 30093452 |
PIK3CA E542K PTEN loss | lung squamous cell carcinoma | sensitive | Alpelisib | Preclinical - Pdx | Actionable | In a preclinical study, Alpelisib (BYL719) treatment resulted in response in a lung squamous cell carcinoma patient-derived xenograft (PDX) model harboring PIK3CA E542K and PTEN loss (PMID: 30093452). | 30093452 |
PIK3CA E542K PTEN loss | stomach cancer | unknown | Sirolimus | Phase 0 | Actionable | In a pilot clinical trial, Rapamune (sirolimus) demonstrated modest clinical activity in patients with PIK3CA-mutant gastric cancer (n=3) or hilar cholangiocarcinoma (n=1), including a gastric cancer patient harboring PIK3CA E542K and PTEN loss, with a 0% response rate, median progression-free survival of 1.9 months, and median overall survival of 3.6 months (PMID: 28685070). | 28685070 |
PIK3CA E542K PTEN loss | breast cancer | sensitive | Taselisib | Preclinical - Cell culture | Actionable | In a preclinical study, a breast cancer cell line harboring PIK3CA E542K was sensitive to treatment with Taselisib (GDC-0032) in culture, demonstrating decreased cell viability (PMID: 31534012). | 31534012 |
PIK3CA E542K PTEN loss | breast cancer | predicted - sensitive | Dactolisib + WEHI-539 | Preclinical - Cell culture | Actionable | In a preclinical study, inhibition of Pi3k signaling by BEZ235 sensitized breast cancer cell lines harboring PIK3CA E542K and PTEN loss to WEHI-539 in culture (PMID: 27974663). | 27974663 |
PIK3CA E542K PTEN loss | breast cancer | predicted - sensitive | CYH33 | Preclinical - Cell culture | Actionable | In a preclinical study, CYH33 inhibited proliferation of a breast cancer cell line harboring PIK3CA E542K and PTEN loss in culture (PMID: 30003928). | 30003928 |
PIK3CA E542K PIK3CA amp | lung squamous cell carcinoma | sensitive | Buparlisib | Preclinical - Pdx | Actionable | In a preclinical study, Buparlisib (BKM120) treatment resulted in inhibition of AKT and S6 phosphorylation and durable response in a lung squamous cell carcinoma patient-derived xenograft (PDX) model harboring PIK3CA E542K and PIK3CA amplification (PMID: 30093452). | 30093452 |
PIK3CA E542K PIK3CA amp | lung squamous cell carcinoma | sensitive | Alpelisib | Preclinical - Pdx | Actionable | In a preclinical study, Alpelisib (BYL719) treatment resulted in response in a lung squamous cell carcinoma patient-derived xenograft (PDX) model harboring PIK3CA E542K and PIK3CA amplification (PMID: 30093452). | 30093452 |
CDKN2A loss PIK3CA E542K PTEN loss | lung squamous cell carcinoma | sensitive | Buparlisib + Palbociclib | Preclinical - Pdx | Actionable | In a preclinical study, treatment with the combination of Buparlisib (BYL719) and Ibrance (palbociclib) resulted in increased tumor growth inhibition compared to either agent alone in a patient-derived xenograft (PDX) model of lung squamous cell carcinoma harboring PIK3CA E542K and PTEN loss, with p16 (CDKN2A) loss (PMID: 30093452). | 30093452 |
CDKN2A loss PIK3CA E542K PIK3CA amp | lung squamous cell carcinoma | sensitive | Buparlisib + Palbociclib | Preclinical - Pdx | Actionable | In a preclinical study, treatment with the combination of Buparlisib (BYL719) and Ibrance (palbociclib) resulted in increased tumor growth inhibition compared to either agent alone in a patient-derived xenograft (PDX) model of lung squamous cell carcinoma harboring PIK3CA E542K and PIK3CA amplification, with p16 (CDKN2A) loss (PMID: 30093452). | 30093452 |
HRAS mut PIK3CA E542K | high grade glioma | sensitive | Buparlisib + Selumetinib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination therapy of Buparlisib (BKM120) and Koselugo (selumetinib) led to a synergistic effect, resulting in growth inhibition of astrocytoma cells with an HRAS mutation expressing PIK3CA E542K in culture, but at a higher drug concentration compared to cells without mutant HRAS (PMID: 29975751). | 29975751 |
PIK3CA E542K PIK3CA F744L | head and neck squamous cell carcinoma | sensitive | Sulindac | Preclinical - Pdx | Actionable | In a preclinical study, Clinoril (sulindac) treatment reduced tumor growth rate in patient-derived xenograft (PDX) models of head and neck squamous cell carcinoma harboring PIK3CA mutations, including a model harboring PIK3CA E542K and PIK3CA F744L (PMID: 30683736). | 30683736 |
PIK3CA E542K TSC1 LOH | transitional cell carcinoma | no benefit | Buparlisib | Case Reports/Case Series | Actionable | In a Phase II trial, Buparlisib (BKM120) treatment resulted in progressive disease in a patient with metastatic urothelial carcinoma harboring PIK3CA E542K and TSC1 loss of heterozygosity (PMID: 32767682; NCT01551030). | 32767682 |
PIK3CA E542K PIK3CA E674Q | urinary bladder cancer | sensitive | MK2206 | Preclinical - Cell culture | Actionable | In a preclinical study, MK2206 increased apoptosis and inhibited viability in a bladder cancer cell line harboring PIK3CA E542K and E674Q in culture (PMID: 25349966). | 25349966 |
PIK3CA E542K PIK3CA H1065L | breast cancer | sensitive | STX-478 | Preclinical - Pdx | Actionable | In a preclinical study, STX-478 inhibited tumor growth of a breast cancer patient-derived xenograft (PDX) model harboring PIK3CA E542K and H1065L (PMID: 37623743). | 37623743 |
BRAF V600E PIK3CA E542K | anaplastic thyroid carcinoma | resistant | Dasatinib + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, an anaplastic thyroid cancer cell line harboring BRAF V600E and PIK3CA E542K was resistant to the combination of Sprycel (dasatinib) and Mekinist (trametinib) in culture (PMID: 37713162). | 37713162 |
BRAF V600E PIK3CA E542K | anaplastic thyroid carcinoma | sensitive | GSK2334470 + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, the addition of GSK2334470 sensitized an anaplastic thyroid cancer cell line harboring BRAF V600E and PIK3CA E542K to Mekinist (trametinib) treatment as demonstrated by a reduction in viability in culture (PMID: 37713162). | 37713162 |
BRAF V600E PIK3CA E542K | anaplastic thyroid carcinoma | resistant | Dasatinib + MK2206 + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, the addition of MK2206 did not sensitize an anaplastic thyroid cancer cell line harboring BRAF V600E and PIK3CA E542k to Sprycel (dasatinib) and Mekinist (trametinib) combination treatment in culture (PMID: 37713162). | 37713162 |
BRAF V600E PIK3CA W11C PIK3CA E542K | papillary thyroid carcinoma | sensitive | Dasatinib + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Sprycel (dasatinib) and Mekinist (trametinib) inhibited viability of a papillary thyroid cancer cell line harboring BRAF V600E and PIK3CA E542K and W11C in culture (PMID: 37713162). | 37713162 |
PIK3CA amp | lung squamous cell carcinoma | no benefit | Capivasertib | Case Reports/Case Series | Actionable | In a Phase II trial (NLMT), Truqap (capivasertib) treatment resulted in no confirmed responses (0/12) and durable clinical benefit in 9% (1/11) of patients with squamous cell lung cancer harboring PIK3CA amplification, thus the cohort was closed due to futility (PMID: 32669708, NCT02664935). | 32669708 |
PIK3CA amp | head and neck squamous cell carcinoma | sensitive | Dactolisib | Preclinical - Cell culture | Actionable | In a preclinical study, BEZ235 resulted in antiproliferative activity in head and neck squamous cell carcinoma cells harboring PIK3CA amplification in culture (PMID: 28446642). | 28446642 |
PIK3CA amp | lung squamous cell carcinoma | no benefit | Buparlisib | Preclinical - Pdx | Actionable | In a preclinical study, lung squamous cell carcinoma a patient-derived xenograft (PDX) model harboring PIK3CA amplification, without additional PIK3CA mutations, did not respond to Buparlisib (BKM120) treatment (PMID: 30093452). | 30093452 |
PIK3CA amp | nasopharynx carcinoma | sensitive | MK2206 | Phase II | Actionable | In a Phase II study, MK2206 increased stable disease to 12 months in a nasopharyngeal carcinoma patient with Pik3ca amplification (PMID: 26084990). | 26084990 |
PIK3CA amp | ovarian cancer | sensitive | Panulisib | Preclinical | Actionable | In a preclinical study, Panulisib (P7170) downregulated mTOR pathway signaling in ovarian cancer cells with amplified PIK3CA (PMID: 25700704). | 25700704 |
PIK3CA amp | head and neck squamous cell carcinoma | predicted - sensitive | Rigosertib Sodium | Case Reports/Case Series | Actionable | In a Phase I trial, Rigosertib (ON 01910.Na) treatment resulted in a complete response with disappearance of mediastinal and lung disease in a patients with head and neck squamous cell carcinoma harboring PIK3CA amplification (Cancer Res April 15 2013 (73) (8 Supplement) LB-198). | detail... |
PIK3CA amp | ovarian cancer | sensitive | XL147 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, XL147 inhibited PI3K signaling and proliferation of a PIK3CA amplified human ovarian cancer cell line in culture, and inhibited tumor growth in xenograft models (PMID: 25637314). | 25637314 |
PIK3CA amp | ovarian cancer | sensitive | Voxtalisib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, an ovarian cancer cell line harboring PIK3CA E545K was sensitive to XL765 (SAR245409), demonstrating inhibition of cell proliferation in culture, and inhibition of tumor growth in cell line xenograft models (PMID: 24634413). | 24634413 |
PIK3CA amp | head and neck squamous cell carcinoma | predicted - sensitive | AZD8055 | Preclinical - Cell culture | Actionable | In a preclinical study, treatment with AZD8055 resulted in antiproliferative activity in head and neck squamous cell carcinoma cells harboring PIK3CA amplification in culture (PMID: 28446642). | 28446642 |
PIK3CA amp | lung non-small cell carcinoma | predicted - sensitive | Sulindac | Preclinical - Cell culture | Actionable | In a preclinical study, non-small cell lung cancer cell lines harboring either a PIK3CA mutation or PIK3CA amplification demonstrated increased sensitivity to Clinoril (sulindac) compared to cell lines with wild-type PIK3CA, resulting in decreased proliferation in culture (PMID: 30683736). | 30683736 |
PIK3CA amp | head and neck squamous cell carcinoma | sensitive | Radiotherapy + Taselisib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Taselisib (GDC-0032) enhanced the effects of radiation induced apoptosis in HNSCC cell lines and cell line xenograft models with PIK3CA amplification (PMID: 26589432). | 26589432 |
PIK3CA amp | triple-receptor negative breast cancer | sensitive | NVP-AEW541 + Pictilisib | Preclinical - Cell culture | Actionable | In a preclinical study, NVP-AEW541 enhanced sensitivity of PIK3CA amplified triple-receptor negative breast cancer cells to Pictilisib (GDC-0941) in culture (PMID: 27196766). | 27196766 |
PIK3CA amp | triple-receptor negative breast cancer | sensitive | Linsitinib + Pictilisib | Preclinical - Cell culture | Actionable | In a preclinical study, Linsitinib (OSI-906) enhanced sensitivity of PIK3CA amplified triple-receptor negative breast cancer cells to Pictilisib (GDC-0941) in culture (PMID: 27196766). | 27196766 |
PIK3CA amp | urinary bladder cancer | sensitive | Gemcitabine + Pictilisib | Preclinical - Pdx | Actionable | In a preclinical study, Pictilisib (GDC-0941) and Gemzar (gemcitabine) combination treatment resulted in inhibition of Akt phosphorylation and improved tumor growth inhibition and survival compared to single agent therapy in patient-derived xenograft (PDX) models of PIK3CA amplified bladder cancer (PMID: 28808038). | 28808038 |
PIK3CA amp | head and neck squamous cell carcinoma | sensitive | Alpelisib + Tipifarnib | Preclinical - Pdx | Actionable | In a preclinical study, the combination of Piqray (alpelisib) and Zarnestra (tipifarnib) inhibited tumor growth in patient-derived xenograft (PDX) models of PIK3CA-amplified head and neck squamous cell carcinoma (PMID: 37339176). | 37339176 |
PIK3CA amp | cervical cancer | sensitive | Copanlisib + Neratinib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Aliqopa (copanlisib) and Nerlynx (neratinib) synergistically inhibited viability of an PIK3CA-amplified cervical cancer cell line in culture (PMID: 31624127). | 31624127 |
PIK3CA E545K PIK3CA amp | lung squamous cell carcinoma | predicted - sensitive | Buparlisib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Buparlisib (BKM120) treatment resulted in inhibition of AKT and S6 phosphorylation and durable responses in 2 of 3 lung squamous cell carcinoma patient-derived xenograft (PDX) models harboring PIK3CA E545K and PIK3CA amplification (PMID: 30093452). | 30093452 |
PIK3CA E545K PIK3CA amp | cervical cancer | sensitive | Copanlisib + Neratinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination of Aliqopa (copanlisib) and Nerlynx (neratinib) synergistically inhibited viability of a cervical cancer cell line harboring PIK3CA E545K with PIK3CA amplification in culture and inhibited tumor growth and increased survival in a cell line xenograft model (PMID: 31624127). | 31624127 |
CDKN2A loss PIK3CA E545K PIK3CA amp | lung squamous cell carcinoma | sensitive | Buparlisib + Palbociclib | Preclinical - Pdx | Actionable | In a preclinical study, treatment with the combination of Buparlisib (BYL719) and Ibrance (palbociclib) resulted in increased tumor growth inhibition compared to either agent alone in patient-derived xenograft (PDX) models of lung squamous cell carcinoma harboring PIK3CA E545K and PIK3CA amplification, with p16 (CDKN2A) loss (PMID: 30093452). | 30093452 |
PIK3CA amp TSC1 LOH | transitional cell carcinoma | predicted - sensitive | Buparlisib | Case Reports/Case Series | Actionable | In a Phase II trial, Buparlisib (BKM120) treatment resulted in a partial response in a patient with metastatic urothelial carcinoma harboring PIK3CA amplification and TSC1 loss of heterozygosity (PMID: 32767682; NCT01551030). | 32767682 |
PIK3CA M1043I PIK3CA amp | bladder urothelial carcinoma | predicted - sensitive | Everolimus | Case Reports/Case Series | Actionable | In a clinical case study, a patient with metastatic urothelial bladder cancer harboring PIK3CA M1043I and PIK3CA amplification (copy number >20), as well as amplification of CCND1 and loss of CDKN2A and CDKN2B, was treated with Afinitor (everolimus) and achieved a complete response including remission of lymph node metastases, and remained progression-free at 6 months (PMID: 33745098). | 33745098 |
MAP2K1 E203K PIK3CA amp | skin squamous cell carcinoma | predicted - sensitive | Metformin + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, a combination of Glucophage (metformin) and Mekinist (trametinib) resulted in a complete clinical response and continued remission for over two years in a patient with cutaneous squamous cell carcinoma with amplification of PIK3CA and harboring MAP2K1 E203K (PMID: 35005996). | 35005996 |
PIK3CA amp PTEN H123P | triple-receptor negative breast cancer | predicted - sensitive | Alpelisib + Everolimus | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, combination treatment with Piqray (albelisib) and Afinitor (everolimus) synergistically inhibited cell viability of patient-derived triple-negative breast cancer cells harboring PIK3CA amplification and PTEN H123P in culture, and led to inhibition of tumor growth in a patient-derived xenograft (PDX) model (PMID: 36900375). | 36900375 |
PIK3CA amp PTEN H123P | triple-receptor negative breast cancer | predicted - sensitive | Afatinib + Alpelisib | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, combination treatment with Piqray (albelisib) and Gilotrif (afatinib) synergistically inhibited cell viability of patient-derived triple-negative breast cancer cells harboring PIK3CA amplification and PTEN H123P in culture, and led to inhibition of tumor growth in a patient-derived xenograft (PDX) model (PMID: 36900375). | 36900375 |
PIK3CA H1047L PIK3CA amp | head and neck squamous cell carcinoma | sensitive | Alpelisib + Tipifarnib | Preclinical - Pdx | Actionable | In a preclinical study, the combination of Piqray (alpelisib) and Zarnestra (tipifarnib) inhibited tumor growth in a patient-derived xenograft (PDX) model of PIK3CA-amplified head and neck squamous cell carcinoma harboring PIK3CA H1047L (PMID: 37339176). | 37339176 |
PIK3CA E545K | breast cancer | sensitive | Trametinib | Preclinical | Actionable | In a preclinical study, Mekinist (trametinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA E545K in culture (PMID: 26627007). | 26627007 |
PIK3CA E545K | diffuse midline glioma, H3 K27M-mutant | sensitive | Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mekinist (trametinib) inhibited viability of mouse glioma cells expressing H3.1 K28M (reported as H3.1 K27M), ACVR1 G328V, and PIK3CA E545K in culture (PMID: 37011011). | 37011011 |
PIK3CA E545K | Advanced Solid Tumor | sensitive | Trametinib | Preclinical | Actionable | In a preclinical study, Mekinist (trametinib) inhibited survival of transformed cell lines overexpressing PIK3CA E545K in culture (PMID: 26627007). | 26627007 |
PIK3CA E545K | Advanced Solid Tumor | resistant | A66 | Preclinical | Actionable | In a preclinical study, cancer cell lines harboring PIK3CA E545K did not demonstrate sensitivity to A66 in culture, in contrast with cells harboring PIK3CA H1047R (PMID: 21668414). | 21668414 |
PIK3CA E545K | breast cancer | sensitive | Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, Miransertib (ARQ092) treatment inhibited Akt signaling, induced cell death, and inhibited proliferation of breast cancer cell lines harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, treatment with Miransertib (ARQ092) resulted in growth inhibition in hormone receptor positive breast cancer cells harboring PIK3CA E545K in culture (PMID: 26469692). | 26469692 |
PIK3CA E545K | gastrointestinal system cancer | sensitive | Capivasertib | Preclinical - Cell culture | Actionable | In a preclinical study, gastric cancer cells harboring PIK3CA E545K demonstrated sensitivity to the AKT inhibitor Truqap (capivasertib), resulting in decreased proliferation in culture (PMID: 24088382). | 24088382 |
PIK3CA E545K | stomach cancer | sensitive | Capivasertib | Preclinical - Cell culture | Actionable | In a preclinical study, a gastric cancer cell line harboring PIK3CA E545K was sensitive to treatment with Truqap (capivasertib), demonstrating decreased cell proliferation in culture (PMID: 32070411). | 32070411 |
PIK3CA E545K | breast cancer | sensitive | Dactolisib | Preclinical | Actionable | In a preclinical study, BEZ235 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA E545K in culture (PMID: 26627007). | 26627007 |
PIK3CA E545K | lung squamous cell carcinoma | sensitive | Dactolisib | Preclinical - Cell culture | Actionable | In a preclinical study, BEZ235 induced apoptosis, inhibited cell proliferation, migration, and invasion of lung squamous cell carcinoma cells over expressing PIK3CA E545K in culture (PMID: 26013318). | 26013318 |
PIK3CA E545K | colorectal cancer | sensitive | Dactolisib | Preclinical | Actionable | In a preclinical study, BEZ235 decreased cell proliferation in colorectal cancer cells harboring a PIK3CA E545K mutation in cell culture (PMID: 21966435). | 21966435 |
PIK3CA E545K | breast cancer | resistant | Buparlisib | Preclinical - Cell culture | Actionable | In a preclinical study, breast cancer cells expressing PIK3CA E545K demonstrated resistance to treatment with Buparlisib (BKM120) in culture (PMID: 29636477). | 29636477 |
PIK3CA E545K | lung squamous cell carcinoma | sensitive | Buparlisib | Preclinical - Cell culture | Actionable | In a preclinical study, Buparlisib (BKM120) induced apoptosis, inhibited cell proliferation, migration, and invasion of lung squamous cell carcinoma cells over expressing PIK3CA E545K in culture (PMID: 26013318). | 26013318 |
PIK3CA E545K | breast cancer | sensitive | Alpelisib | Preclinical - Cell culture | Actionable | In a preclinical study, Alpelisib (BYL719) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA E545K in culture (PMID: 26627007). | 26627007 |
PIK3CA E545K | lung squamous cell carcinoma | sensitive | Alpelisib | Preclinical - Cell culture | Actionable | In a preclinical study, Alpelisib (BYL719) induced apoptosis, inhibited cell proliferation, migration, and invasion of lung squamous cell carcinoma cells over expressing PIK3CA E545K in culture (PMID: 26013318). | 26013318 |
PIK3CA E545K | cervical cancer | predicted - sensitive | Alpelisib | Case Reports/Case Series | Actionable | In a Phase I trial, treatment with Piqray (alpelisib) resulted in an objective response rate of 33% (2/6; all partial responses), disease control rate of 100% (6/6), with stable disease in 5 patients, in cervical cancer patients harboring PIK3CA mutations, including PIK3CA E545K (PMID: 35311394). | 35311394 |
PIK3CA E545K | cervical cancer | predicted - sensitive | Alpelisib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Piqray (alpelisib) increased apoptosis and decreased colony formation in a cervical cancer cell line harboring PIK3CA E545K in culture and decreased tumor cell proliferation and increased CD8-positive T-cell differentiation and proliferation in a cell line xenograft model (PMID: 37469254). | 37469254 |
PIK3CA E545K | stomach cancer | sensitive | Alpelisib | Preclinical - Cell culture | Actionable | In a preclinical study, Piqray (alpelisib) inhibited growth and induced cell cycle arrest and inhibited phosphorylation of Akt and S6 in a gastric cancer cell line harboring PIK3CA E545K in culture (PMID: 37493631). | 37493631 |
PIK3CA E545K | Advanced Solid Tumor | sensitive | Alpelisib | Preclinical - Pdx | Actionable | In a preclinical study, Alpelisib (BYL719) inhibited PIK3CA E545K and showed anti-tumor activity in patient-derived xenograft models harboring a PIK3CA E545K mutation (PMID: 24608574). | 24608574 |
PIK3CA E545K | breast cancer | sensitive | Everolimus | Preclinical | Actionable | In a preclinical study, breast cancer cell lines harboring a PIK3CA E545K mutation had increased sensitivity to Afinitor (everolimus) in culture (PMID: 20664172). | 20664172 |
PIK3CA E545K | Her2-receptor negative breast cancer | no benefit | Everolimus | Phase III | Actionable | In a retrospective analysis of a Phase III trial (BOLERO-2), Afinitor (everolimus) demonstrated comparable progression-free survival benefit in patients with hormone receptor-positive, Erbb2 (Her2)-negative breast cancer harboring wild-type (HR=0.43) or mutant (HR=0.37) PIK3CA, similar benefit was observed in subgroups harboring PIK3CA H1047R (HR=0.37) and PIK3CA E545K/E542K (HR=0.30) (PMID: 28183140; NCT00863655). | 28183140 |
PIK3CA E545K | breast cancer | sensitive | Ipatasertib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Ipatasertib (GDC-0068) reduced tumor growth in a cell line xenograft model of hormone-receptor positive breast cancer harboring PIK3CA E545K (PMID: 32205017). | 32205017 |
PIK3CA E545K | breast cancer | sensitive | Ipatasertib | Preclinical - Cell culture | Actionable | In a preclinical study, Ipatasertib (GDC-0068) treatment inhibited Akt signaling, induced cell death, and inhibited proliferation of breast cancer cell lines harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | colon cancer | no benefit | Pictilisib | Preclinical - Cell culture | Actionable | In a preclinical study, Pictilisib (GDC-0941) treatment did not affect cell viability in a colon cancer cell line expressing PIK3CA E545K in culture (PMID: 34544753). | 34544753 |
PIK3CA E545K | urinary bladder cancer | sensitive | Pictilisib | Preclinical - Cell culture | Actionable | In a preclinical study, Pictilisib (GDC-0941) inhibited Akt phosphorylation, resulted in growth inhibition in bladder cancer cells harboring PIK3CA E545K in culture (PMID: 28808038). | 28808038 |
PIK3CA E545K | head and neck squamous cell carcinoma | predicted - sensitive | Apitolisib | Case Reports/Case Series | Actionable | In a Phase I trial, Apitolisib (GDC-0980) treatment resulted in an unconfirmed partial response in a patient with head and neck squamous cell carcinoma harboring PIK3CA E545K (PMID: 26787751; NCT00854152). | 26787751 |
PIK3CA E545K | ovarian clear cell carcinoma | predicted - sensitive | Apitolisib | Case Reports/Case Series | Actionable | In a Phase I trial, Apitolisib (GDC-0980) treatment resulted in tumor regression by 48.3% in a patient with ovarian clear cell carcinoma harboring PIK3CA E545K, who remained on treatment for 282 days (PMID: 26787751; NCT00854152). | 26787751 |
PIK3CA E545K | breast cancer | sensitive | Lapatinib | Preclinical | Actionable | In a preclinical study, Tykerb (lapatinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA E545K in culture (PMID: 26627007). | 26627007 |
PIK3CA E545K | colon cancer | predicted - sensitive | LY2780301 | Case Reports/Case Series | Actionable | In a Phase I trial, a colon cancer patient harboring PIK3CA E545K was sensitive to LY2780301, demonstrating stable disease for approximately 125 days (PMID: 25902900). | 25902900 |
PIK3CA E545K | breast cancer | sensitive | MK2206 | Preclinical | Actionable | In a preclinical study, MK2206 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA E545K in culture (PMID: 26627007). | 26627007 |
PIK3CA E545K | breast cancer | sensitive | MK2206 | Preclinical - Cell culture | Actionable | In a preclinical study, MK2206 treatment inhibited Akt signaling, induced cell death, and inhibited proliferation of breast cancer cell lines harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | thyroid cancer | sensitive | MK2206 | Preclinical - Cell culture | Actionable | In a preclinical study, expression of PIK3CA E545K in a thyroid cancer cell line resulted in increased sensitivity to MK2206 in culture (PMID: 21289267). | 21289267 |
PIK3CA E545K | urinary bladder cancer | sensitive | MK2206 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, MK2206 increased apoptosis and inhibited viability in bladder cancer cell lines harboring PIK3CA E545K in culture and inhibited tumor growth in cell line xenograft models (PMID: 25349966). | 25349966 |
PIK3CA E545K | breast cancer | sensitive | Neratinib | Preclinical | Actionable | In a preclinical study, Nerlynx (neratinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA E545K in culture (PMID: 26627007). | 26627007 |
PIK3CA E545K | breast cancer | sensitive | Sirolimus | Preclinical - Cell culture | Actionable | In a preclinical study, a breast cancer cell line harboring PIK3CA E545K demonstrated hypersensitivity to Rapamune (sirolimus)-induced growth inhibition in culture (PMID: 24631838). | 24631838 |
PIK3CA E545K | Klatskin's tumor | unknown | Sirolimus | Phase 0 | Actionable | In a pilot clinical trial, Rapamune (sirolimus) demonstrated modest clinical activity in patients with PIK3CA-mutant gastric cancer (n=3) or hilar cholangiocarcinoma (n=1; harboring PIK3CA E545K), with a 0% response rate, median progression-free survival of 1.9 months, and median overall survival of 3.6 months (PMID: 28685070). | 28685070 |
PIK3CA E545K | Advanced Solid Tumor | sensitive | Sirolimus | Preclinical | Actionable | In a preclinical study, Rapamune (sirolimus) demonstrated efficacy in inhibiting transformation of cultured cells containing PIK3CA E545K mutations (PMID: 15647370). | 15647370 |
PIK3CA E545K | breast cancer | sensitive | BAY1125976 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, BAY1125976 inhibited proliferation of a breast cancer cell line harboring PIK3CA E545K in culture, and inhibited AKT signaling and tumor growth in xenograft models (PMID: 27699769). | 27699769 |
PIK3CA E545K | clear cell adenocarcinoma | predicted - sensitive | Copanlisib | Case Reports/Case Series | Actionable | In a Phase II trial (NCI MATCH EAY131-Z1F), Aliqopa (copanlisib) treatment resulted in a partial response and progression-free survival of 7.3 months and an overall survival of 19.8 months in a patient with clear cell carcinoma of anterior abdominal wall harboring PIK3CA E545K (PMID: 35133871; NCT02465060). | 35133871 |
PIK3CA E545K | colon cancer | sensitive | Taselisib | Preclinical - Cell culture | Actionable | In a preclinical study, Taselisib (GDC-0032) treatment led to decreased cell viability in a colon cancer cell line expressing PIK3CA E545K in culture (PMID: 34544753). | 34544753 |
PIK3CA E545K | lung squamous cell carcinoma | no benefit | Taselisib | Case Reports/Case Series | Actionable | In a Phase I (SWOG S1400B) trial, Taselisib (GDC-0032) treatment did not meet its primary endpoint for response rate in patients with lung squamous cell carcinoma harboring PIK3CA mutations, resulting in only 1 response of 11 patients harboring PIK3CA E545K (PMID: 31158500; NCT02785913). | 31158500 |
PIK3CA E545K | breast cancer | sensitive | Gedatolisib | Preclinical | Actionable | In a preclinical study, Gedatolisib (PKI-587) inhibited growth of human breast cancer cells harboring PIK3CA E545K in culture (PMID: 21325073, PMID: 17314276). | 17314276 21325073 |
PIK3CA E545K | head and neck squamous cell carcinoma | sensitive | Rigosertib Sodium | Preclinical - Pdx | Actionable | In a preclinical study, head and neck squamous cell carcinoma patient-derived xenograft models harboring a PIK3CA E545K mutation demonstrated increased sensitivity to Rigosertib (ON 01910.Na) (PMID: 23873848). | 23873848 |
PIK3CA E545K | Advanced Solid Tumor | sensitive | Rigosertib Sodium | Preclinical - Cell culture | Actionable | In a preclinical study, Rigosertib (ON 01910.Na) inhibited oncogenic transformation in fibroblast cells over-expressing PIK3CA E545K in culture (PMID: 27104980). | 27104980 |
PIK3CA E545K | breast carcinoma | sensitive | XL147 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, XL147 inhibited PI3K signaling and proliferation of a human breast carcinoma cell line harboring PIK3CA E545K in culture and inhibited tumor growth in xenograft models (PMID: 25637314). | 25637314 |
PIK3CA E545K | breast cancer | sensitive | Voxtalisib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, a breast cancer cell line harboring PIK3CA E545K was sensitive to XL765 (SAR245409), demonstrating inhibition of cell proliferation and colony formation in culture, and inhibition of tumor growth in cell line xenograft models (PMID: 24634413). | 24634413 |
PIK3CA E545K | esophagus squamous cell carcinoma | sensitive | LY294002 | Preclinical | Actionable | In a preclinical study, LY294002 inhibited cell proliferation of esophagus squamous cell carcinoma cells expressing PIK3CA E545K (PMID: 18262558). | 18262558 |
PIK3CA E545K | leukemia | sensitive | LY3023414 | Preclinical | Actionable | In a preclinical study, LY3023414 inhibited tumor growth in a transgenic animal model of leukemia driven by PIK3CA E545K (PMID: 27439478). | 27439478 |
PIK3CA E545K | lung non-small cell carcinoma | sensitive | Copanlisib + Paclitaxel | Preclinical - Pdx | Actionable | In a preclinical study, Aliqopa (copanlisib), in combination with Taxol (paclitaxel), induced tumor regression in PIK3CA E545K-mutant patient-derived non-small cell lung cancer xenografts (PMID: 24170767). | 24170767 |
PIK3CA E545K | estrogen-receptor positive breast cancer | predicted - sensitive | Alpelisib + Everolimus | Preclinical - Patient cell culture | Actionable | In a preclinical study, combination treatment with Piqray (albelisib) and Afinitor (everolimus) inhibited cell viability of patient-derived ESR1 (ER)-positive breast cancer cells harboring PIK3CA E545K in culture (PMID: 36900375). | 36900375 |
PIK3CA E545K | cervical cancer | predicted - sensitive | Pembrolizumab | Case Reports/Case Series | Actionable | In a clinical case study, Keytruda (pembrolizumab) treatment resulted in complete remission in a patient with metastatic cervical cancer harboring PIK3CA E545K and moderate tumor mutational burden (TMB) (9.2 mut/Mb) (PMID: 37469254). | 37469254 |
PIK3CA E545K | urinary bladder cancer | sensitive | Cisplatin + Pictilisib | Preclinical - Cell culture | Actionable | In a preclinical study, Pictilisib (GDC-0941) and Platinol (cisplatin) synergistically inhibited Akt phosphorylation and growth of bladder cancer cells harboring PIK3CA E545K in culture (PMID: 28808038). | 28808038 |
PIK3CA E545K | breast cancer | sensitive | Ipatasertib + Paclitaxel | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination of Ipatasertib (GDC-0068) and Taxol (paclitaxel) inhibited tumor growth in a cell line xenograft model of hormone-receptor positive breast cancer harboring PIK3CA E545K, and demonstrated increased activity over either agent alone (PMID: 32205017). | 32205017 |
PIK3CA E545K | colorectal cancer | sensitive | Cetuximab + Irinotecan | Case Reports/Case Series | Actionable | In a retrospective analysis, treatment with the combination of Erbitux (cetuximab) and Camptosar (irinotecan) resulted in stable disease in 50% (1/2) and 14 months without evidence of disease in 50% (1/2) of colorectal carcinoma patients harboring a PIK3CA E545K mutation (PMID: 25714871). | 25714871 |
PIK3CA E545K | colorectal cancer | resistant | Cetuximab + Fluorouracil | Preclinical - Cell culture | Actionable | In a preclinical study, colorectal cancer cells over expressing PIK3CA E545K were resistant to Erbitux (cetuximab) and Fluorouracil combination treatment in culture (PMID: 28424201). | 28424201 |
PIK3CA E545K | estrogen-receptor positive breast cancer | sensitive | AZD8835 | Preclinical | Actionable | In a preclinical study, AZD8835 inhibited proliferation of estrogen receptor (ER)-positive breast cancer cells harboring PIK3CA E545K in culture and suppressed tumor growth in xenograft models (PMID: 26839307). | 26839307 |
PIK3CA E545K | breast cancer | sensitive | MEN1611 | Preclinical | Actionable | In a preclinical study, MEN1611 (CH5132799) inhibited proliferation of breast cancer cells expressing PIK3CA E545K (PMID: 21558396). | 21558396 |
PIK3CA E545K | ovarian cancer | sensitive | MEN1611 | Preclinical | Actionable | In a preclinical study, MEN1611 (CH5132799) inhibited proliferation of ovarian cancer cells harboring PIK3CA E545K in culture (PMID: 21558396). | 21558396 |
PIK3CA E545K | breast cancer | sensitive | WYE-125132 | Preclinical | Actionable | In a preclinical study, WYE-125132 inhibited proliferation of breast cancer cells with a PIK3CA E545K mutation (PMID: 20068177). | 20068177 |
PIK3CA E545K | cervical cancer | sensitive | PW12 | Preclinical | Actionable | In a preclinical study, PW12 inhibited proliferation of cervical cancer cells with a PIK3CA E545K mutation (PMID: 22391131). | 22391131 |
PIK3CA E545K | breast cancer | sensitive | GSK690693 | Preclinical - Cell culture | Actionable | In a preclinical study, GSK690693 treatment inhibited Akt signaling, induced cell death, and inhibited proliferation of breast cancer cell lines harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | PKI-402 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, treatment with PKI-402 resulted in decreased Akt phosphorylation and tumor regression in ERBB2 (HER2)-positive breast cancer cell line xenograft models harboring PIK3CA E545K (PMID: 20371716). | 20371716 |
PIK3CA E545K | breast cancer | sensitive | ARQ 751 | Preclinical - Cell culture | Actionable | In a preclinical study, a breast cancer cell line harboring PIK3CA E545K was sensitive to ARQ 751 in culture, demonstrating inhibition of cell growth (PMID: 26469692). | 26469692 |
PIK3CA E545K | breast cancer | sensitive | ARQ 751 | Preclinical - Cell culture | Actionable | In a preclinical study, ARQ 751 treatment inhibited Akt signaling, induced cell death, and inhibited proliferation of breast cancer cell lines harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | colon cancer | sensitive | Inavolisib | Preclinical - Cell culture | Actionable | In a preclinical study, Itovebi (inavolisib) treatment led to decreased cell viability in a colon cancer cell line expressing PIK3CA E545K in culture (PMID: 34544753). | 34544753 |
PIK3CA E545K | breast cancer | sensitive | Inavolisib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Itovebi (inavolisib) treatment led to tumor regression in an ESR1 (ER)-positive breast cancer cell line xenograft model harboring PIK3CA E545K (PMID: 34544753). | 34544753 |
PIK3CA E545K | breast cancer | no benefit | Dactolisib + Venetoclax | Preclinical - Cell culture | Actionable | In a preclinical study, inhibition of Pi3k signaling by BEZ235 did not sensitize breast cancer cell lines harboring PIK3CA E545K to Venclexta (venetoclax) in culture (PMID: 27974663). | 27974663 |
PIK3CA E545K | breast cancer | predicted - sensitive | Dactolisib + WEHI-539 | Preclinical - Cell culture | Actionable | In a preclinical study, inhibition of Pi3k signaling by BEZ235 sensitized breast cancer cell lines harboring PIK3CA E545K to WEHI-539 in culture (PMID: 27974663). | 27974663 |
PIK3CA E545K | breast cancer | sensitive | DHM25 | Preclinical - Cell culture | Actionable | In a preclinical study, DHM25 increased cell death in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 26237138). | 26237138 |
PIK3CA E545K | head and neck squamous cell carcinoma | predicted - sensitive | Carboplatin + Paclitaxel + Temsirolimus | Case Reports/Case Series | Actionable | In a Phase II trial, a patient with head and neck squamous cell carcinoma harboring PIK3CA E545K demonstrated a partial response when treated with the combination of Torisel (temsirolimus), Paraplatin (carboplatin), and Taxol (paclitaxel) (PMID: 28961834). | 28961834 |
PIK3CA E545K | urinary bladder cancer | sensitive | Gemcitabine + Pictilisib | Preclinical - Cell culture | Actionable | In a preclinical study, Pictilisib (GDC-0941) and Gemzar (gemcitabine) synergistically inhibited Akt phosphorylation and growth of bladder cancer cells harboring PIK3CA E545K in culture (PMID: 28808038). | 28808038 |
PIK3CA E545K | urinary bladder cancer | sensitive | Pictilisib + Sorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Pictilisib (GDC-0941) and Nexavar (sorafenib) synergistically decreased Erk and Akt phosphorylation, inhibited survival of bladder cancer cells harboring PIK3CA E545K in culture (PMID: 28808038). | 28808038 |
PIK3CA E545K | breast cancer | sensitive | Ipatasertib + Sirolimus | Preclinical - Cell culture | Actionable | In a preclinical study, Rapamune (sirolimus) and Ipatasertib (GDC0068) combination treatment increased cell death compared to Ipatasertib (GDC0068) alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | GSK2334470 + Ipatasertib | Preclinical - Cell culture | Actionable | In a preclinical study, GSK2334470 and Ipatasertib (GDC0068) combination treatment increased cell death compared to Ipatasertib (GDC0068) alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | predicted - sensitive | CYH33 | Preclinical - Cell culture | Actionable | In a preclinical study, CYH33 inhibited proliferation of a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 30003928). | 30003928 |
PIK3CA E545K | breast cancer | sensitive | Borussertib | Preclinical - Cell culture | Actionable | In a preclinical study, borussertib inhibited AKT signaling and proliferation of a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 30858154). | 30858154 |
PIK3CA E545K | head and neck squamous cell carcinoma | sensitive | Alpelisib + Tipifarnib | Preclinical - Pdx | Actionable | In a preclinical study, the combination of Piqray (alpelisib) and Zarnestra (tipifarnib) inhibited tumor growth in a patient-derived xenograft (PDX) model of head and neck squamous cell carcinoma harboring PIK3CA E545K (PMID: 37339176). | 37339176 |
PIK3CA E545K | lung non-small cell carcinoma | sensitive | T-2143 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, T-2143 treatment reduced proliferation of non-small cell lung cancer cells harboring PIK3CA E545K in culture, and inhibited tumor growth in a cell line xenograft model (PMID: 32499300). | 32499300 |
PIK3CA E545K | ovarian cancer | predicted - sensitive | TAS-117 | Case Reports/Case Series | Actionable | In a Phase II trial, TAS-117 treatment in an ovarian cancer patient harboring PIK3CA E545K led to a partial response at 6 weeks after treatment and a 39% decrease in tumor size, but subsequently progression was observed at 12 weeks in non-target lesions and an increase in tumor markers at 18 weeks, and TAS-117 treatment was discontinued (PMID: 33723724; NCT03017521). | 33723724 |
PIK3CA E545K | breast cancer | sensitive | AZD0156 + MK2206 | Preclinical - Cell culture | Actionable | In a preclinical study, AZD0156 and MK2206 combination treatment increased cell death compared to MK2206 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | ARQ 751 + AZD0156 | Preclinical - Cell culture | Actionable | In a preclinical study, AZD0156 and ARQ 751 combination treatment increased cell death compared to ARQ 751 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | AZD0156 + Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, AZD0156 and Miransertib (ARQ092) combination treatment increased cell death compared to Miransertib (ARQ092) alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | AZD0156 + GSK690693 | Preclinical - Cell culture | Actionable | In a preclinical study, AZD0156 and GSK690693 combination treatment increased cell death compared to GSK690693 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | AZD0156 + Ipatasertib | Preclinical - Cell culture | Actionable | In a preclinical study, AZD0156 and Ipatasertib (GDC-0068) combination treatment increased cell death compared to Ipatasertib (GDC-0068) alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | KU-57788 + MK2206 | Preclinical - Cell culture | Actionable | In a preclinical study, KU-57788 and MK2206 combination treatment increased cell death compared to MK2206 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | ARQ 751 + KU-57788 | Preclinical - Cell culture | Actionable | In a preclinical study, KU-57788 and ARQ 751 combination treatment increased cell death compared to ARQ 751 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | KU-57788 + Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, KU-57788 and Miransertib (ARQ092) combination treatment increased cell death compared to Miransertib (ARQ092) alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | Ipatasertib + KU-57788 | Preclinical - Cell culture | Actionable | In a preclinical study, KU-57788 and Ipatasertib (GDC-0068) combination treatment increased cell death compared to Ipatasertib (GDC-0068) alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | GSK690693 + KU-57788 | Preclinical - Cell culture | Actionable | In a preclinical study, KU-57788 and GSK690693 combination treatment increased cell death compared to GSK690693 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | GSK2334470 + MK2206 | Preclinical - Cell culture | Actionable | In a preclinical study, GSK2334470 and MK2206 combination treatment increased cell death compared to MK2206 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | ARQ 751 + GSK2334470 | Preclinical - Cell culture | Actionable | In a preclinical study, GSK2334470 and ARQ 751 combination treatment increased cell death compared to ARQ 751 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | GSK2334470 + GSK690693 | Preclinical - Cell culture | Actionable | In a preclinical study, GSK2334470 and GSK690693 combination treatment increased cell death compared to GSK690693 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | MK2206 + OSU-T315 | Preclinical - Cell culture | Actionable | In a preclinical study, OSU-T315 and MK2206 combination treatment increased cell death compared to MK2206 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | ARQ 751 + OSU-T315 | Preclinical - Cell culture | Actionable | In a preclinical study, OSU-T315 and ARQ 751combination treatment increased cell death compared to ARQ 751 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | Miransertib + OSU-T315 | Preclinical - Cell culture | Actionable | In a preclinical study, OSU-T315 and Miransertib (ARQ092) combination treatment increased cell death compared to Miransertib (ARQ092) alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | GSK690693 + OSU-T315 | Preclinical - Cell culture | Actionable | In a preclinical study, OSU-T315 and GSK690693 combination treatment increased cell death compared to GSK690693 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | Ipatasertib + OSU-T315 | Preclinical - Cell culture | Actionable | In a preclinical study, OSU-T315 and Ipatasertib (GDC0068) combination treatment increased cell death compared to Ipatasertib (GDC0068) alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | GSK2334470 + Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, GSK2334470 and Miransertib (ARQ092) combination treatment increased cell death compared to Miransertib (ARQ092) alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | decreased response | LAM-002A + MK2206 | Preclinical - Cell culture | Actionable | In a preclinical study, LAM-002A (Apilimod dimesylate) and MK2206 combination treatment resulted in less cell death compared to MK2206 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | decreased response | ARQ 751 + LAM-002A | Preclinical - Cell culture | Actionable | In a preclinical study, LAM-002A (Apilimod dimesylate) and ARQ 751 combination treatment resulted in less cell death compared to ARQ 751 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | MK2206 + Sirolimus | Preclinical - Cell culture | Actionable | In a preclinical study, Rapamune (sirolimus) and MK2206 combination treatment increased cell death compared to MK2206 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | ARQ 751 + Sirolimus | Preclinical - Cell culture | Actionable | In a preclinical study, Rapamune (sirolimus) and ARQ 751 combination treatment increased cell death compared to ARQ 751 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | Miransertib + Sirolimus | Preclinical - Cell culture | Actionable | In a preclinical study, Rapamune (sirolimus) and Miransertib (ARQ092) combination treatment increased cell death compared to Miransertib (ARQ092) alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | GSK690693 + Sirolimus | Preclinical - Cell culture | Actionable | In a preclinical study, Rapamune (sirolimus) and GSK690693 combination treatment increased cell death compared to GSK690693 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | MK2206 + Torin 1 | Preclinical - Cell culture | Actionable | In a preclinical study, Torin 1 and MK2206 combination treatment increased cell death compared to MK2206 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | ARQ 751 + Torin 1 | Preclinical - Cell culture | Actionable | In a preclinical study, Torin 1 and ARQ 751 combination treatment increased cell death compared to ARQ 751 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | Miransertib + Torin 1 | Preclinical - Cell culture | Actionable | In a preclinical study, Torin 1 and Miransertib (ARQ092) combination treatment increased cell death compared to Miransertib (ARQ092) alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | GSK690693 + Torin 1 | Preclinical - Cell culture | Actionable | In a preclinical study, Torin 1 and GSK690693 combination treatment increased cell death compared to GSK690693 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | Ipatasertib + Torin 1 | Preclinical - Cell culture | Actionable | In a preclinical study, Torin 1 and Ipatasertib (GDC0068) combination treatment increased cell death compared to Ipatasertib (GDC0068) alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | RLY-2608 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, RLY-2608 inhibited proliferation of hormone receptor-positive breast cancer cells harboring PIK3CA E545K in culture, and led to tumor regression in a cell line xenograft model (PMID: 37916956). | 37916956 |
PIK3CA E545K | estrogen-receptor positive breast cancer | predicted - sensitive | Afatinib + Alpelisib | Preclinical - Patient cell culture | Actionable | In a preclinical study, combination treatment with Piqray (albelisib) and Gilotrif (afatinib) synergistically inhibited cell viability of patient-derived ESR1 (ER)-positive breast cancer cells harboring PIK3CA E545K in culture (PMID: 36900375). | 36900375 |
PIK3CA E545K | head and neck squamous cell carcinoma | sensitive | STX-478 | Preclinical - Pdx | Actionable | In a preclinical study, STX-478 inhibited tumor growth of a head and neck squamous cell cancer patient-derived xenograft (PDX) model harboring PIK3CA E545K (PMID: 37623743). | 37623743 |
PIK3CA E545K | cervical cancer | sensitive | Alpelisib + Toripalimab-tpzi | Preclinical - Pdx | Actionable | In a preclinical study, the combination of Piqray (alpelisib) and Loqtorz (toripalimab-tpzi) inhibited proliferation in cell line xenograft models of cervical cancer harboring PIK3CA E545K and in a patient-derived xenograft (PDX) model (PMID: 37469254). | 37469254 |
PIK3CA E545K | stomach cancer | sensitive | A-1331852 + Alpelisib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Piqray (alpelisib) and A-1331852 synergistically inhibited viability in a gastric cancer cell line harboring PIK3CA E545K in culture (PMID: 37493631). | 37493631 |
PIK3CA E545K | Her2-receptor negative breast cancer | predicted - sensitive | HS-10352 | Case Reports/Case Series | Actionable | In a Phase I trial, HS-10352 treatment resulted in an objective response rate (ORR) of 27.8% (5/18, all partial responses), disease control rate (DCR) of 55.6%, and median progression-free survival (mPFS) of 3.9 mo in HR-positive, ERBB2 (HER2)-negative advanced breast cancer patients overall, and in the 6mg group led to an ORR of 66.7% and DCR of 83.3%, with an ORR of 75.0% (3/4) and DCR of 100% in patients with PIK3CA mutations (E542K, E545K, E545D, H1047L, H1047R) (PMID: 38037839; NCT04631835). | 38037839 |
PIK3CA E545K | breast cancer | sensitive | ZM-PI05 | Preclinical - Cell culture | Actionable | In a preclinical study, ZM-PI05 decreased viability of a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 38986734). | 38986734 |
BRAF G596R PIK3CA E545K | colorectal cancer | resistant | Vemurafenib | Preclinical - Cell culture | Actionable | In a preclinical study, colorectal cancer cells harboring BRAF G596R and PIK3CA E545K did not demonstrate sensitivity to Zelboraf (vemurafenib) treatment in culture (PMID: 22180495). | 22180495 |
BRAF G596R PIK3CA E545K | colorectal cancer | sensitive | Neratinib | Preclinical | Actionable | In a preclinical study, Nerlynx (neratinib) inhibited growth of colorectal cancer cells harboring both BRAF G596R and PIK3CA E545K in culture (PMID: 26243863). | 26243863 |
PIK3CA E545K PTEN loss | stomach cancer | unknown | Sirolimus | Phase 0 | Actionable | In a pilot clinical trial, Rapamune (sirolimus) demonstrated modest clinical activity in patients with PIK3CA-mutant gastric cancer (n=3) or hilar cholangiocarcinoma (n=1), including 2 gastric cancer patients harboring PIK3CA E545K and PTEN loss, with a 0% response rate, median progression-free survival of 1.9 months, and median overall survival of 3.6 months (PMID: 28685070). | 28685070 |
NRAS mut PIK3CA E545K | melanoma | predicted - resistant | Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, NRAS-mutant melanoma cell lines expressing PIK3CA E545K demonstrated resistance to treatment with Mekinist (trametinib) in culture (PMID: 30819666). | 30819666 |
NRAS mut PIK3CA E545K | melanoma | predicted - resistant | Palbociclib | Preclinical - Cell culture | Actionable | In a preclinical study, two of two NRAS-mutant melanoma cell lines expressing PIK3CA E545K demonstrated resistance to treatment with Ibrance (palbociclib) in culture (PMID: 30819666). | 30819666 |
NRAS mut PIK3CA E545K | melanoma | predicted - resistant | Palbociclib + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, four of four NRAS-mutant melanoma cell lines expressing PIK3CA E545K were resistant to the combination treatment of Ibrance (palbociclib) and Mekinist (trametinib) in culture (PMID: 30819666). | 30819666 |
ROS1 rearrange PIK3CA E545K | lung non-small cell carcinoma | predicted - resistant | Crizotinib | Case Reports/Case Series | Actionable | In a Phase II clinical trial, a patient with non-small cell lung cancer harboring a ROS1 rearrangement demonstrated progression while being treated with Xalkori (crizotinib), and was found to have acquired a PIK3CA E545K mutation (PMID: 30978502; NCT02183870). | 30978502 |
PIK3CA E545K PIK3CA E726K | breast cancer | sensitive | Alpelisib | Preclinical - Cell culture | Actionable | In a preclinical study, breast epithelial cells expressing PIK3CA E545K and PIK3CA E726K in cis demonstrated increased sensitivity to growth inhibition by Piqray (Alpelisib) treatment compared to cells expressing individual PIK3CA mutations in culture (PMID: 31699932). | 31699932 |
PIK3CA E545K PIK3CA E726K | breast cancer | sensitive | Alpelisib | Preclinical - Cell culture | Actionable | In a preclinical study, Piqray (alpelisib) decreased viability of a breast cancer cell line harboring PIK3CA E545K and expressing PIK3CA E726K in culture (PMID: 37916958). | 37916958 |
PIK3CA E545K PIK3CA E726K | breast cancer | sensitive | Everolimus | Preclinical - Cell culture | Actionable | In a preclinical study, breast epithelial cells expressing PIK3CA E545K and PIK3CA E726K in cis demonstrated increased sensitivity to growth inhibition by Afinitor (everolimus) treatment compared to cells expressing individual PIK3CA mutations in culture (PMID: 31699932). | 31699932 |
PIK3CA E545K PIK3CA E726K | breast cancer | sensitive | Ipatasertib | Preclinical - Cell culture | Actionable | In a preclinical study, Ipatasertib (GDC-0068) decreased viability of a breast cancer cell line harboring PIK3CA E545K and expressing PIK3CA E726K in culture (PMID: 37916958). | 37916958 |
PIK3CA E545K PIK3CA E726K | breast cancer | sensitive | Pictilisib | Preclinical - Cell culture | Actionable | In a preclinical study, Pictilisib (GDC-0941) decreased viability of a breast cancer cell line harboring PIK3CA E545K and expressing PIK3CA E726K in culture (PMID: 37916958). | 37916958 |
PIK3CA E545K PIK3CA E726K | breast cancer | sensitive | Taselisib | Preclinical - Cell culture | Actionable | In a preclinical study, Taselisib (GDC-0032) decreased viability of a breast cancer cell line harboring PIK3CA E545K and expressing PIK3CA E726K in culture (PMID: 37916958). | 37916958 |
PIK3CA E545K PIK3CA E726K | breast cancer | sensitive | Inavolisib | Preclinical - Cell culture | Actionable | In a preclinical study, breast epithelial cells expressing PIK3CA E545K and PIK3CA E726K in cis demonstrated increased sensitivity to growth inhibition by Itovebi (inavolisib) treatment compared to cells expressing individual PIK3CA mutations in culture (PMID: 31699932). | 31699932 |
PIK3CA E545K PIK3CA E726K | breast cancer | sensitive | Inavolisib | Preclinical - Cell culture | Actionable | In a preclinical study, Itovebi (inavolisib) decreased viability of a breast cancer cell line harboring PIK3CA E545K and expressing PIK3CA E726K in culture (PMID: 37916958). | 37916958 |
PIK3CA E545K PIK3CA M1043L | breast cancer | sensitive | Alpelisib | Preclinical - Cell culture | Actionable | In a preclinical study, breast epithelial cells expressing PIK3CA E545K and PIK3CA M1043L in cis demonstrated increased sensitivity to growth inhibition by Piqray (Alpelisib) treatment compared to cells expressing individual PIK3CA mutations in culture (PMID: 31699932). | 31699932 |
PIK3CA E545K PIK3CA M1043L | breast cancer | sensitive | Everolimus | Preclinical - Cell culture | Actionable | In a preclinical study, breast epithelial cells expressing PIK3CA E545K and PIK3CA M1043L in cis demonstrated increased sensitivity to growth inhibition by Afinitor (everolimus) treatment compared to cells expressing individual PIK3CA mutations in culture (PMID: 31699932). | 31699932 |
PIK3CA E545K PIK3CA M1043L | breast cancer | sensitive | Inavolisib | Preclinical - Cell culture | Actionable | In a preclinical study, breast epithelial cells expressing PIK3CA E545K and PIK3CA M1043L in cis demonstrated increased sensitivity to growth inhibition by Itovebi (inavolisib) treatment compared to cells expressing individual PIK3CA mutations in culture (PMID: 31699932). | 31699932 |
BRAF V600E PIK3CA E545K | lung non-small cell carcinoma | predicted - sensitive | Vemurafenib | Case Reports/Case Series | Actionable | In a clinical study, Zelboraf (vemurafenib) treatment resulted in stable disease for 6.4 months in a non-small cell lung cancer patient harboring BRAF V600E, tested in tissue and plasma, and PIK3CA E545K, tested in plasma only (PMID: 32859654). | 32859654 |
PIK3CA L10_P18del PIK3CA E545K | gastrointestinal stromal tumor | predicted - sensitive | Alpelisib | Case Reports/Case Series | Actionable | In a clinical case study, Piqray (alpelisib) treatment resulted in symptom improvement and stable disease maintained for more than 12 months in an adolescent patient with SDH-deficient gastrointestinal stromal tumor (GIST) harboring PIK3CA E545K and PIK3CA L10_P18del (PMID: 35917491). | 35917491 |
NRAS G13R PIK3CA E545K | melanoma | predicted - resistant | Binimetinib + Ribociclib | Case Reports/Case Series | Actionable | In a Phase Ib/II trial, a patient with melanoma harboring NRAS G13R experienced disease progression on combination treatment with Mektovi (binimetinib) and Kisqali (ribociclib), likely due to the acquisition of PIK3CA E545K (PMID: 29496665; NCT01781572). | 29496665 |
NRAS Q61K PIK3CA E545K | melanoma | predicted - resistant | Binimetinib + Ribociclib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, a melanoma cell line harboring NRAS Q61K and expressing PIK3CA E545K was resistant to combination treatment with Mektovi (binimetinib) and Kisqali (ribociclib) in culture and in a cell line xenograft model, demonstrating lack of tumor regression and continued tumor growth (PMID: 29496665). | 29496665 |
NRAS Q61K PIK3CA E545K | melanoma | predicted - sensitive | Ribociclib | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring NRAS Q61K and expressing PIK3CA E545K was resistant to treatment with Kisqali (ribociclib) in culture (PMID: 29496665). | 29496665 |
NRAS Q61K PIK3CA E545K | melanoma | predicted - resistant | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring NRAS Q61K and expressing PIK3CA E545K was resistant to treatment with Mektovi (binimetinib) in culture (PMID: 29496665). | 29496665 |
NRAS Q61K PIK3CA E545K | melanoma | predicted - sensitive | Binimetinib + Ribociclib + Sirolimus | Preclinical - Cell culture | Actionable | In a preclinical study, the addition of Sirolimus (rapamycin) resensitized a melanoma cell line harboring NRAS Q61K and expressing PIK3CA E545K to combination treatment with Mektovi (binimetinib) and Kisqali (ribociclib) in culture, resulting in inhibition of cell growth (PMID: 29496665). | 29496665 |
NRAS Q61K PIK3CA E545K | melanoma | predicted - sensitive | Binimetinib + PF-4708671 + Ribociclib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the addition of PF-4708671 resensitized a melanoma cell line harboring NRAS Q61K and expressing PIK3CA E545K to combination treatment with Mektovi (binimetinib) and Kisqali (ribociclib) in culture, resulting in inhibition of cell growth, and resulted in tumor regression and complete responses in cell line xenograft models (PMID: 29496665). | 29496665 |
NRAS Q61L PIK3CA E545K | melanoma | predicted - resistant | Binimetinib + Ribociclib | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring NRAS Q61L and expressing PIK3CA E545K was resistant to combination treatment with Mektovi (binimetinib) and Kisqali (ribociclib) in culture (PMID: 29496665). | 29496665 |
NRAS Q61L PIK3CA E545K | melanoma | predicted - resistant | Ribociclib | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring NRAS Q61L and expressing PIK3CA E545K was resistant to treatment with Kisqali (ribociclib) in culture (PMID: 29496665). | 29496665 |
NRAS Q61L PIK3CA E545K | melanoma | predicted - resistant | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring NRAS Q61L and expressing PIK3CA E545K was resistant to treatment with Mektovi (binimetinib) in culture (PMID: 29496665). | 29496665 |
NRAS Q61L PIK3CA E545K | melanoma | predicted - sensitive | Binimetinib + Ribociclib + Sirolimus | Preclinical - Cell culture | Actionable | In a preclinical study, the addition of Sirolimus (rapamycin) resensitized a melanoma cell line harboring NRAS Q61L and expressing PIK3CA E545K to combination treatment with Mektovi (binimetinib) and Kisqali (ribociclib) in culture, resulting in inhibition of cell growth (PMID: 29496665). | 29496665 |
NRAS Q61L PIK3CA E545K | melanoma | predicted - sensitive | Binimetinib + PF-4708671 + Ribociclib | Preclinical - Cell culture | Actionable | In a preclinical study, the addition of PF-4708671 resensitized a melanoma cell line harboring NRAS Q61L and expressing PIK3CA E545K to combination treatment with Mektovi (binimetinib) and Kisqali (ribociclib) in culture, resulting in inhibition of cell growth (PMID: 29496665). | 29496665 |
FGFR3 S249C PIK3CA E545K | bladder urothelial carcinoma | predicted - resistant | Erdafitinib | Case Reports/Case Series | Actionable | In a clinical case study, PIK3CA E545K was identified in the post-progression biopsy of a patient with bladder urothelial cancer harboring FGFR3 S249C who progressed on treatment with Balversa (erdafitinib) (PMID: 37377403). | 37377403 |
FGFR3 S249C PIK3CA E545K | bladder urothelial carcinoma | predicted - resistant | Futibatinib | Case Reports/Case Series | Actionable | In a clinical case study, a patient with bladder urothelial cancer harboring FGFR3 S249C and an acquired PIK3CA E545K experienced primary resistance to treatment with Lytgobi (futibatinib) (PMID: 37377403). | 37377403 |
FGFR3 S249C PIK3CA E545K | transitional cell carcinoma | sensitive | Erdafitinib + Pictilisib | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, combination treatment with Balversa (erdafitinib) and Pictilisib (GDC-0941) resulted in synergistic inhibition of tumor growth in a patient-derived xenograft (PDX) model of urothelial cancer harboring FGFR3 S249C and PIK3CA E545K (PMID: 37377403). | 37377403 |
FGFR3 S249C FGFR3 N540K PIK3CA E545K | transitional cell carcinoma | predicted - resistant | Erdafitinib | Case Reports/Case Series | Actionable | In a clinical case study, FGFR3 N540K was identified in the post-progression biopsy of a patient with upper tract urothelial carcinoma harboring FGFR3 S249C and PIK3CA E545K who previously responded to Balversa (erdafitinib) treatment (PMID: 37377403). | 37377403 |
HRAS G13V PIK3CA E545K | salivary gland carcinoma | predicted - sensitive | Tipifarnib | Case Reports/Case Series | Actionable | In a clinical case study, Zarnestra (tipifarnib) treatment resulted in a partial response and progression-free survival lasting more than 5 months in a patient with androgen-receptor (AR)-positive salivary duct carcinoma harboring HRAS G13V and PIK3CA E545K (PMID: 37427101). | 37427101 |
PIK3CA E545K PIK3CA W780R | breast cancer | sensitive | Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, Miransertib (ARQ092) decreased viability of a breast cancer cell line harboring PIK3CA E545K and expressing PIK3CA W780R in culture (PMID: 37916958). | 37916958 |
PIK3CA E545K PIK3CA W780R | breast cancer | resistant | Alpelisib | Preclinical - Cell culture | Actionable | In a preclinical study, a breast cancer cell line harboring PIK3CA E545K and expressing PIK3CA W780R was resistant to Piqray (alpelisib) in culture (PMID: 37916958). | 37916958 |
PIK3CA E545K PIK3CA W780R | breast cancer | sensitive | Ipatasertib | Preclinical - Cell culture | Actionable | In a preclinical study, Ipatasertib (GDC-0068) decreased viability of a breast cancer cell line harboring PIK3CA E545K and expressing PIK3CA W780R in culture (PMID: 37916958). | 37916958 |
PIK3CA E545K PIK3CA W780R | breast cancer | resistant | Pictilisib | Preclinical - Cell culture | Actionable | In a preclinical study, a breast cancer cell line harboring PIK3CA E545K and expressing PIK3CA W780R was resistant to Pictilisib (GDC-0941) in culture (PMID: 37916958). | 37916958 |
PIK3CA E545K PIK3CA W780R | breast cancer | resistant | Taselisib | Preclinical - Cell culture | Actionable | In a preclinical study, a breast cancer cell line harboring PIK3CA E545K and expressing PIK3CA W780R was resistant to Taselisib (GDC-0032) in culture (PMID: 37916958). | 37916958 |
PIK3CA E545K PIK3CA W780R | breast cancer | resistant | Inavolisib | Preclinical - Cell culture | Actionable | In a preclinical study, a breast cancer cell line harboring PIK3CA E545K and expressing PIK3CA W780R was resistant to Itovebi (inavolisib) in culture (PMID: 37916958). | 37916958 |
PIK3CA E545K PIK3CA Q859H | breast cancer | sensitive | Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, Miransertib (ARQ092) decreased viability of a breast cancer cell line harboring PIK3CA E545K and expressing PIK3CA Q859H in culture (PMID: 37916958). | 37916958 |
PIK3CA E545K PIK3CA Q859H | breast cancer | resistant | Alpelisib | Preclinical - Cell culture | Actionable | In a preclinical study, a breast cancer cell line harboring PIK3CA E545K and expressing PIK3CA Q859H was resistant to Piqray (alpelisib) in culture (PMID: 37916958). | 37916958 |
PIK3CA E545K PIK3CA Q859H | breast cancer | sensitive | Ipatasertib | Preclinical - Cell culture | Actionable | In a preclinical study, Ipatasertib (GDC-0068) decreased viability of a breast cancer cell line harboring PIK3CA E545K and expressing PIK3CA Q859H in culture (PMID: 37916958). | 37916958 |
PIK3CA E545K PIK3CA Q859H | breast cancer | sensitive | Pictilisib | Preclinical - Cell culture | Actionable | In a preclinical study, Pictilisib (GDC-0941) decreased viability of a breast cancer cell line harboring PIK3CA E545K and expressing PIK3CA Q859H in culture (PMID: 37916958). | 37916958 |
PIK3CA E545K PIK3CA Q859H | breast cancer | sensitive | Taselisib | Preclinical - Cell culture | Actionable | In a preclinical study, Taselisib (GDC-0032) decreased viability of a breast cancer cell line harboring PIK3CA E545K and expressing PIK3CA Q859H in culture (PMID: 37916958). | 37916958 |
PIK3CA E545K PIK3CA Q859H | breast cancer | resistant | Inavolisib | Preclinical - Cell culture | Actionable | In a preclinical study, a breast cancer cell line harboring PIK3CA E545K and expressing PIK3CA Q859H was resistant to Itovebi (inavolisib) in culture (PMID: 37916958). | 37916958 |
PIK3CA E545K PIK3CA I817F | breast cancer | sensitive | Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, Miransertib (ARQ092) decreased viability of a breast cancer cell line harboring PIK3CA E545K and expressing PIK3CA I817F in culture (PMID: 37916958). | 37916958 |
PIK3CA E545K PIK3CA I817F | breast cancer | sensitive | Alpelisib | Preclinical - Cell culture | Actionable | In a preclinical study, Piqray (alpelisib) decreased viability of a breast cancer cell line harboring PIK3CA E545K and expressing PIK3CA I817F in culture (PMID: 37916958). | 37916958 |
PIK3CA E545K PIK3CA I817F | breast cancer | sensitive | Ipatasertib | Preclinical - Cell culture | Actionable | In a preclinical study, Ipatasertib (GDC-0068) decreased viability of a breast cancer cell line harboring PIK3CA E545K and expressing PIK3CA I817F in culture (PMID: 37916958). | 37916958 |
PIK3CA E545K PIK3CA I817F | breast cancer | sensitive | Pictilisib | Preclinical - Cell culture | Actionable | In a preclinical study, Pictilisib (GDC-0941) decreased viability of a breast cancer cell line harboring PIK3CA E545K and expressing PIK3CA I817F in culture (PMID: 37916958). | 37916958 |
PIK3CA E545K PIK3CA I817F | breast cancer | sensitive | Taselisib | Preclinical - Cell culture | Actionable | In a preclinical study, Taselisib (GDC-0032) decreased viability of a breast cancer cell line harboring PIK3CA E545K and expressing PIK3CA I817F in culture (PMID: 37916958). | 37916958 |
PIK3CA E545K PIK3CA I817F | breast cancer | sensitive | Inavolisib | Preclinical - Cell culture | Actionable | In a preclinical study, Itovebi (inavolisib) decreased viability of a breast cancer cell line harboring PIK3CA E545K and expressing PIK3CA I817F in culture (PMID: 37916958). | 37916958 |
PIK3CA Q546R | prostate cancer | sensitive | MEN1611 | Preclinical | Actionable | In a preclinical study, MEN1611 (CH5132799) inhibited proliferation of prostate cancer cells harboring PIK3CA Q546R in culture (PMID: 21558396). | 21558396 |
PIK3CA C420R | breast cancer | sensitive | Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, Miransertib (ARQ092) treatment induced cell death and inhibited proliferation of a breast cancer cell line harboring PIK3CA C420R in culture (PMID: 32439931). | 32439931 |
PIK3CA C420R | ovarian clear cell adenocarcinoma | sensitive | DS-7423 | Preclinical - Cell culture | Actionable | In a preclinical study, an ovarian clear cell adenocarcinoma cell line harboring PIK3CA C420R was sensitive to DS-7423 in culture, demonstrating inhibition of cell proliferation (PMID: 24504419). | 24504419 |
PIK3CA C420R | breast cancer | predicted - sensitive | Ipatasertib | Preclinical - Cell culture | Actionable | In a preclinical study, Ipatasertib (GDC-0068) treatment did not increase cell death but inhibited proliferation of a breast cancer cell line harboring PIK3CA C420R in culture (PMID: 32439931). | 32439931 |
PIK3CA C420R | breast cancer | sensitive | MK2206 | Preclinical - Cell culture | Actionable | In a preclinical study, MK2206 treatment induced cell death and inhibited proliferation of a breast cancer cell line harboring PIK3CA C420R in culture (PMID: 32439931). | 32439931 |
PIK3CA C420R | Advanced Solid Tumor | sensitive | Sirolimus | Preclinical | Actionable | In a preclinical study, cells expressing PIK3CA C420R were sensitive to Rapamune (sirolimus) in culture (PMID: 17376864). | 17376864 |
PIK3CA C420R | breast cancer | predicted - sensitive | GSK690693 | Preclinical - Cell culture | Actionable | In a preclinical study, GSK690693 treatment did not increase cell death but inhibited proliferation of a breast cancer cell line harboring PIK3CA C420R in culture (PMID: 32439931). | 32439931 |
PIK3CA C420R | breast cancer | sensitive | ARQ 751 | Preclinical - Cell culture | Actionable | In a preclinical study, ARQ 751 treatment induced cell death and inhibited proliferation of a breast cancer cell line harboring PIK3CA C420R in culture (PMID: 32439931). | 32439931 |
PIK3CA C420R | Her2-receptor positive breast cancer | sensitive | ZM-PI05 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, ZM-PI05 induced cell cycle arrest and decreased viability of an ERBB2 (HER2)-positive breast cancer cell line harboring PIK3CA C420R in culture and inhibited tumor growth in a cell line xenograft model (PMID: 38986734). | 38986734 |
PIK3CA I391M | uterine cancer | predicted - sensitive | Sirolimus | Case Reports/Case Series | Actionable | In a clinical case study, a uterine cancer patient harboring PIK3CA I391M demonstrated stable disease when treated with Rapamune (sirolimus) (PMID: 28514312). | 28514312 |
BRAF V600E PIK3CA N1044S | anaplastic thyroid carcinoma | resistant | Dasatinib + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, an anaplastic thyroid cancer cell line harboring BRAF V600E and PIK3CA N1044S was resistant to the combination of Sprycel (dasatinib) and Mekinist (trametinib) in culture (PMID: 37713162). | 37713162 |
BRAF V600E PIK3CA N1044S | anaplastic thyroid carcinoma | sensitive | GSK2334470 + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, the addition of GSK2334470 sensitized an anaplastic thyroid cancer cell line harboring BRAF V600E and PIK3CA N1044S to Mekinist (trametinib) treatment as demonstrated by a reduction in viability in culture (PMID: 37713162). | 37713162 |
BRAF V600E PIK3CA N1044S | anaplastic thyroid carcinoma | resistant | Dasatinib + MK2206 + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, the addition of MK2206 did not sensitize an anaplastic thyroid cancer cell line harboring BRAF V600E and PIK3CA N1044S to Sprycel (dasatinib) and Mekinist (trametinib) combination treatment in culture (PMID: 37713162). | 37713162 |
PIK3CA P539R | breast cancer | sensitive | BAY1125976 | Preclinical - Cell culture | Actionable | In a preclinical study, BAY1125976 inhibited proliferation of a breast cancer cell line harboring PIK3CA P539R in culture (PMID: 27699769). | 27699769 |
PIK3CA P539R | breast cancer | predicted - sensitive | CYH33 | Preclinical - Cell culture | Actionable | In a preclinical study, CYH33 inhibited proliferation of a breast cancer cell line harboring PIK3CA P539R in culture (PMID: 30003928). | 30003928 |
FGFR2 N550K PIK3CA I20M PIK3CA P539R PTEN R130Q PTEN T321fs | endometrial cancer | sensitive | Alpelisib + Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Truseltiq (infigratinib) and Alpelisib (BYL719) resulted in a synergistic effect, demonstrating inhibition of cell proliferation and induced cell death in an endometrial cancer cell line harboring FGFR2 N550K, PIK3CA I20M and P539R, and PTEN R130Q and T321fs*23 in culture (PMID: 28119489). | 28119489 |
FGFR2 N550K PIK3CA I20M PIK3CA P539R PTEN R130Q PTEN T321fs | endometrial cancer | sensitive | Buparlisib + Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Truseltiq (infigratinib) and Buparlisib (BKM120) resulted in a synergistic effect, demonstrating inhibition of cell proliferation, decreased colony formation, and cell death in an endometrial cancer cell line harboring FGFR2 N550K, PIK3CA I20M and P539R, and PTEN R130Q and T321fs*23 in culture (PMID: 28119489). | 28119489 |
FGFR2 N550K PIK3CA I20M PIK3CA P539R PTEN R130Q PTEN T321fs | endometrial cancer | sensitive | Infigratinib + Pictilisib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Truseltiq (infigratinib) and Pictilisib (GDC-0941) resulted in a synergistic effect, demonstrating inhibition of cell proliferation, decreased colony formation, and cell death in an endometrial cancer cell line harboring FGFR2 N550K, PIK3CA I20M and P539R, and PTEN R130Q and T321fs*23 in culture (PMID: 28119489). | 28119489 |
PIK3CA Q546K | breast cancer | sensitive | Trametinib | Preclinical | Actionable | In a preclinical study, Mekinist (trametinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA Q546K in culture (PMID: 26627007). | 26627007 |
PIK3CA Q546K | Advanced Solid Tumor | sensitive | Trametinib | Preclinical | Actionable | In a preclinical study, Mekinist (trametinib) inhibited survival of transformed cell lines overexpressing PIK3CA Q546K in culture (PMID: 26627007). | 26627007 |
PIK3CA Q546K | breast cancer | sensitive | Dactolisib | Preclinical | Actionable | In a preclinical study, BEZ235 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA Q546K in culture (PMID: 26627007). | 26627007 |
PIK3CA Q546K | breast cancer | sensitive | Alpelisib | Preclinical - Cell culture | Actionable | In a preclinical study, Alpelisib (BYL719) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA Q546K in culture (PMID: 26627007). | 26627007 |
PIK3CA Q546K | breast cancer | sensitive | Lapatinib | Preclinical | Actionable | In a preclinical study, Tykerb (lapatinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA Q546K in culture (PMID: 26627007). | 26627007 |
PIK3CA Q546K | breast cancer | sensitive | MK2206 | Preclinical | Actionable | In a preclinical study, MK2206 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA Q546K in culture (PMID: 26627007). | 26627007 |
PIK3CA Q546K | breast cancer | sensitive | Neratinib | Preclinical | Actionable | In a preclinical study, Nerlynx (neratinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA Q546K in culture (PMID: 26627007). | 26627007 |
PIK3CA R88Q | malignant pleural mesothelioma | predicted - sensitive | Apitolisib | Case Reports/Case Series | Actionable | In a Phase I trial, treatment with Apitolisib (GDC-0980) resulted in a partial response in a patient with malignant pleural mesothelioma harboring PIK3CA R88Q (PMID: 26787751; NCT00854152). | 26787751 |
PIK3CA R88Q | colorectal cancer | predicted - sensitive | Cetuximab + Floxuridine + Fluorouracil + Irinotecan | Case Reports/Case Series | Actionable | In a retrospective analysis, treatment with the combination of Erbitux (cetuximab), Adrucil (fluorouracil), Camptosar (irinotecan), and Floxuridine resulted in at least 24 months without evidence of disease in a colorectal carcinoma patient harboring a PIK3CA R88Q mutation (PMID: 25714871). | 25714871 |
PIK3CA R88Q | high grade glioma | sensitive | Buparlisib + Selumetinib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination therapy of Buparlisib (BKM120) and Koselugo (selumetinib) led to a synergistic effect, resulting in greater growth inhibition of astrocytoma cells expressing PIK3CA R88Q than cells with wild-type PIK3CA in culture (PMID: 29975751). | 29975751 |
PIK3CA R88Q | tonsil squamous cell carcinoma | predicted - sensitive | Alpelisib + Tipifarnib | Case Reports/Case Series | Actionable | In a Phase I/II trial (KURRENT-HN), the combination of Piqray (alpelisib) and Zarnestra (tipifarnib) resulted in a partial response with an 84% reduction in the target lesions and a complete response in the lung in a patient with metastatic squamous cell carcinoma of the tonsil harboring PIK3CA R88Q, with response ongoing at 27 weeks (PMID: 37339176; NCT04997902). | 37339176 |
PIK3CA R88Q PTEN mut | endometrial cancer | sensitive | Dactolisib | Preclinical | Actionable | In a preclinical study, BEZ235 inhibited proliferation of endometrial cancer cells harboring PIK3CA R88Q and PTEN mutations in culture (PMID: 22662154). | 22662154 |
PIK3CA R88Q PTEN mut | endometrial cancer | sensitive | Everolimus | Preclinical | Actionable | In a preclinical study, Afinitor (everolimus) inhibited proliferation of endometrial cancer cells harboring PIK3CA R88Q and PTEN mutations in culture (PMID: 22662154). | 22662154 |
HRAS mut PIK3CA R88Q | high grade glioma | sensitive | Buparlisib + Selumetinib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination therapy of Buparlisib (BKM120) and Koselugo (selumetinib) led to a synergistic effect, resulting in growth inhibition of astrocytoma cells with an HRAS mutation and expressing PIK3CA R88Q in culture, but at a higher drug concentration compared to cells without mutant HRAS (PMID: 29975751). | 29975751 |
PIK3CA E453K | breast cancer | resistant | Buparlisib | Preclinical - Cell culture | Actionable | In a preclinical study, breast cancer cells expressing PIK3CA E453K demonstrated resistance to treatment with Buparlisib (BKM120) in culture (PMID: 29636477). | 29636477 |
PIK3CA E453K | lung squamous cell carcinoma | no benefit | Taselisib | Case Reports/Case Series | Actionable | In a Phase I (SWOG S1400B) trial, Taselisib (GDC-0032) treatment did not meet its primary endpoint for response rate in patients with lung squamous cell carcinoma harboring PIK3CA mutations, resulting in no response in a patient harboring PIK3CA E453K (PMID: 31158500; NCT02785913). | 31158500 |
PIK3CA E453K PIK3CA E545A | stomach cancer | sensitive | Alpelisib | Preclinical - Cell culture | Actionable | In a preclinical study, Piqray (alpelisib) inhibited growth and induced cell cycle arrest and inhibited phosphorylation of Akt and S6 in a gastric cancer cell line harboring PIK3CA E545A and E453K in culture (PMID: 37493631). | 37493631 |
PIK3CA E453K PIK3CA E545A | stomach cancer | sensitive | Alpelisib + Dasatinib | Preclinical - Cell culture | Actionable | In a preclinical study, the addition of Sprycel (dasatinib) to Piqray (alpelisib) treatment resulted in an increased inhibition of proliferation in a gastric cancer cell line harboring PIK3CA E545A and E453K in culture (PMID: 37493631). | 37493631 |
PIK3CA E453K PIK3CA E545A | stomach cancer | sensitive | A-1331852 + Alpelisib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Piqray (alpelisib) and A-1331852 synergistically inhibited viability in a gastric cancer cell line harboring PIK3CA E545A and E453K in culture (PMID: 37493631). | 37493631 |
FGFR2 T319I PIK3CA N345K PIK3CA E453K | Her2-receptor negative breast cancer | predicted - resistant | Inavolisib | Case Reports/Case Series | Actionable | In a clinical case study, FGFR2 T319I was identified in circulating tumor DNA at the time of progression on Itovebi (inavolisib) in a patient with ESR1-positive, ERBB2 (HER2)-negative breast cancer harboring PIK3CA N345K and E453K (PMID: 37916958). | 37916958 |
PIK3CA E542Q PIK3CA E674Q | urinary bladder cancer | sensitive | Alpelisib + Nintedanib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, combination treatment with Ofev (nintedanib) and Piqray (alpelisib) led to synergistic inhibition of growth in bladder cancer cell lines harboring PIK3CA E542Q and PIK3CA E674Q in culture, and led to inhibition of tumor growth in a cell line xenograft model (PMID: 36805958). | 36805958 |
PIK3CA E542Q PIK3CA E674Q | urinary bladder cancer | sensitive | Nintedanib + Pictilisib | Preclinical - Cell culture | Actionable | In a preclinical study, combination treatment with Ofev (nintedanib) and Pictilisib (GDC-0941) inhibited cell proliferation in a bladder cancer cell line harboring PIK3CA E542Q and PIK3CA E674Q in culture (PMID: 36805958). | 36805958 |
PIK3CA E542V | colorectal cancer | predicted - sensitive | Cetuximab | Case Reports/Case Series | Actionable | In a retrospective analysis, Erbitux (cetuximab) treatment resulted in stable disease in a colorectal carcinoma patient harboring a PIK3CA E542V mutation (PMID: 25714871). | 25714871 |
FGFR3 S249C PIK3CA E545A | transitional cell carcinoma | predicted - sensitive | Erdafitinib | Case Reports/Case Series | Actionable | In a clinical case study, Balversa (erdafitinib) treatment resulted in a partial response with a progression-free survival of 5.8 months in a patient with upper tract urothelial carcinoma harboring FGFR3 S249C and PIK3CA E545A (PMID: 37377403). | 37377403 |
PIK3CA E545D | Her2-receptor negative breast cancer | predicted - sensitive | HS-10352 | Case Reports/Case Series | Actionable | In a Phase I trial, HS-10352 treatment resulted in an objective response rate (ORR) of 27.8% (5/18, all partial responses), disease control rate (DCR) of 55.6%, and median progression-free survival (mPFS) of 3.9 mo in HR-positive, ERBB2 (HER2)-negative advanced breast cancer patients overall, and in the 6mg group led to an ORR of 66.7% and DCR of 83.3%, with an ORR of 75.0% (3/4) and DCR of 100% in patients with PIK3CA mutations (E542K, E545K, E545D, H1047L, H1047R) (PMID: 38037839; NCT04631835). | 38037839 |
PIK3CA E545G | urinary bladder cancer | sensitive | MK2206 | Preclinical - Cell culture | Actionable | In a preclinical study, MK2206 increased apoptosis and inhibited viability in a bladder cancer cell line harboring PIK3CA E545G in culture (PMID: 25349966). | 25349966 |
PIK3CA E545G | colorectal adenocarcinoma | sensitive | Palbociclib + PD-0325901 | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Ibrance (palbociclib) and PD-0325901 synergistically inhibited growth of a colorectal adenocarcinoma cell line harboring PIK3CA E545G in culture (PMID: 37326340). | 37326340 |
PIK3CA E545G | colorectal adenocarcinoma | sensitive | Gedatolisib + Palbociclib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Ibrance (palbociclib) and Gedatolisib (PF-05212384) synergistically inhibited growth of a colorectal adenocarcinoma cell line harboring PIK3CA E545G in culture (PMID: 37326340). | 37326340 |
PIK3CA E545V | ovarian clear cell adenocarcinoma | sensitive | DS-7423 | Preclinical - Cell culture | Actionable | In a preclinical study, an ovarian clear cell adenocarcinoma cell line harboring PIK3CA E545V was sensitive to DS-7423 in culture, demonstrating inhibition of cell proliferation (PMID: 24504419). | 24504419 |
PIK3CA G1049R | breast cancer | sensitive | Trametinib | Preclinical | Actionable | In a preclinical study, Mekinist (trametinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA G1049R in culture (PMID: 26627007). | 26627007 |
PIK3CA G1049R | Advanced Solid Tumor | sensitive | Trametinib | Preclinical | Actionable | In a preclinical study, Mekinist (trametinib) inhibited survival of transformed cell lines overexpressing PIK3CA G1049R in culture (PMID: 26627007). | 26627007 |
PIK3CA G1049R | breast cancer | sensitive | Dactolisib | Preclinical | Actionable | In a preclinical study, BEZ235 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA G1049R in culture (PMID: 26627007). | 26627007 |
PIK3CA G1049R | breast cancer | resistant | Buparlisib | Preclinical - Cell culture | Actionable | In a preclinical study, breast cancer cells expressing PIK3CA G1049R demonstrated resistance to treatment with Buparlisib (BKM120) in culture (PMID: 29636477). | 29636477 |
PIK3CA G1049R | breast cancer | sensitive | Alpelisib | Preclinical | Actionable | In a preclinical study, Alpelisib (BYL719) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA G1049R in culture (PMID: 26627007). | 26627007 |
PIK3CA G1049R | breast cancer | sensitive | Lapatinib | Preclinical | Actionable | In a preclinical study, Tykerb (lapatinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA G1049R in culture (PMID: 26627007). | 26627007 |
PIK3CA G1049R | breast cancer | sensitive | MK2206 | Preclinical | Actionable | In a preclinical study, MK2206 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA G1049R in culture (PMID: 26627007). | 26627007 |
PIK3CA G1049R | breast cancer | sensitive | Neratinib | Preclinical | Actionable | In a preclinical study, Nerlynx (neratinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA G1049R in culture (PMID: 26627007). | 26627007 |
PIK3CA G1049R | lung squamous cell carcinoma | no benefit | Taselisib | Case Reports/Case Series | Actionable | In a Phase I (SWOG S1400B) trial, Taselisib (GDC-0032) treatment did not meet its primary endpoint for response rate in patients with lung squamous cell carcinoma harboring PIK3CA mutations, resulting in no response in a patient harboring PIK3CA G1049R (PMID: 31158500; NCT02785913). | 31158500 |
PIK3CA G118D | lung non-small cell carcinoma | sensitive | LY3023414 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, LY3023414 inhibited proliferation of non-small cell lung cancer cells harboring PIK3CA G118D in culture, resulted in tumor growth inhibition in cell line xenograft models (PMID: 27439478). | 27439478 |
PIK3CA G118D | head and neck squamous cell carcinoma | sensitive | Alpelisib + Tipifarnib | Preclinical - Pdx | Actionable | In a preclinical study, the combination of Piqray (alpelisib) and Zarnestra (tipifarnib) inhibited tumor growth in a patient-derived xenograft (PDX) model of head and neck squamous cell carcinoma harboring PIK3CA G118D (PMID: 37339176). | 37339176 |
PIK3CA H1047L | breast cancer | sensitive | Trametinib | Preclinical | Actionable | In a preclinical study, Mekinist (trametinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA H1047L in culture (PMID: 26627007). | 26627007 |
PIK3CA H1047L | breast cancer | sensitive | Dactolisib | Preclinical | Actionable | In a preclinical study, BEZ235 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA H1047L in culture (PMID: 26627007). | 26627007 |
PIK3CA H1047L | breast cancer | sensitive | Alpelisib | Preclinical - Cell culture | Actionable | In a preclinical study, Alpelisib (BYL719) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA H1047L in culture (PMID: 26627007). | 26627007 |
PIK3CA H1047L | breast cancer | sensitive | Lapatinib | Preclinical | Actionable | In a preclinical study, Tykerb (lapatinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA H1047L in culture (PMID: 26627007). | 26627007 |
PIK3CA H1047L | breast cancer | sensitive | MK2206 | Preclinical | Actionable | In a preclinical study, MK2206 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA H1047L in culture (PMID: 26627007). | 26627007 |
PIK3CA H1047L | breast cancer | sensitive | Neratinib | Preclinical | Actionable | In a preclinical study, Nerlynx (neratinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA H1047L in culture (PMID: 26627007). | 26627007 |
PIK3CA H1047L | oral squamous cell carcinoma | decreased response | Palbociclib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, treatment with Ibrance (palbociclib) resulted in sustained tumor growth, but increasing tumor volume over time with treatment in oral squamous cell carcinoma cell line xenograft models harboring PIK3CA H1047L (PMID: 31516747). | 31516747 |
PIK3CA H1047L | oral squamous cell carcinoma | predicted - sensitive | PF-04691502 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, PF-04691502 treatment inhibited tumor growth in a cell line xenograft model of oral squamous cell carcinoma harboring PIK3CA H1047L (PMID: 31516747). | 31516747 |
PIK3CA H1047L | oral squamous cell carcinoma | sensitive | Palbociclib + PF-04691502 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, oral squamous cell carcinoma cells harboring PIK3CA H1047L demonstrated increased sensitivity to Ibrance (palbociclib) when combined with PF-04691502, and the combination treatment inhibited proliferation in cell culture, and reduced tumor growth in a cell line xenograft model (PMID: 31516747). | 31516747 |
PIK3CA H1047L | colon cancer | sensitive | STX-478 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, STX-478 inhibited viability in a colon cancer cell line harboring PIK3CA H1047L in culture, and inhibited tumor growth and induced tumor regression in a cell line xenograft model (PMID: 37623743). | 37623743 |
PIK3CA H1047L | Her2-receptor negative breast cancer | predicted - sensitive | HS-10352 | Case Reports/Case Series | Actionable | In a Phase I trial, HS-10352 treatment resulted in an objective response rate (ORR) of 27.8% (5/18, all partial responses), disease control rate (DCR) of 55.6%, and median progression-free survival (mPFS) of 3.9 mo in HR-positive, ERBB2 (HER2)-negative advanced breast cancer patients overall, and in the 6mg group led to an ORR of 66.7% and DCR of 83.3%, with an ORR of 75.0% (3/4) and DCR of 100% in patients with PIK3CA mutations (E542K, E545K, E545D, H1047L, H1047R) (PMID: 38037839; NCT04631835). | 38037839 |
PIK3CA H1047Y | endometrial cancer | sensitive | MEN1611 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, MEN1611 (CH5132799) inhibited cell growth in a human endometrial cancer cell line harboring a PIK3CA H1047Y mutation, and inhibited tumor growth in xenograft models (PMID: 21558396). | 21558396 |
PIK3CA H1047Y | glioblastoma | sensitive | YM-024 | Preclinical | Actionable | In a preclinical study, glioblastoma cell lines harboring PIK3CA H1047Y demonstrated increased sensitivity to YM-024 induced growth inhibition (PMID: 24718026). | 24718026 |
PIK3CA K111N | breast cancer | sensitive | Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, hormone receptor positive breast cancer cells harboring PIK3CA K111N were sensitive to Miransertib (ARQ092) in culture, demonstrating inhibition of cell growth (PMID: 26469692). | 26469692 |
PIK3CA K111N | breast cancer | sensitive | Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, Miransertib (ARQ092) treatment induced cell death and inhibited proliferation of a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 32439931). | 32439931 |
PIK3CA K111N | breast cancer | predicted - sensitive | Ipatasertib | Preclinical - Cell culture | Actionable | In a preclinical study, Ipatasertib (GDC-0068) treatment did not increase cell death but inhibited proliferation of a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 32439931). | 32439931 |
PIK3CA K111N | breast cancer | sensitive | MK2206 | Preclinical - Cell culture | Actionable | In a preclinical study, MK2206 treatment increased cell death and inhibited proliferation of a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 32439931). | 32439931 |
PIK3CA K111N | breast cancer | sensitive | BAY1125976 | Preclinical - Cell culture | Actionable | In a preclinical study, BAY1125976 inhibited proliferation of a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 27699769). | 27699769 |
PIK3CA K111N | estrogen-receptor positive breast cancer | sensitive | AZD8835 | Preclinical | Actionable | In a preclinical study, AZD8835 inhibited proliferation of estrogen receptor (ER)-positive breast cancer cells harboring PIK3CA K111N in culture and induced tumor regression in xenograft models (PMID: 26839307). | 26839307 |
PIK3CA K111N | breast cancer | sensitive | MEN1611 | Preclinical - Cell culture | Actionable | In a preclinical study, MEN1611 (CH5132799) inhibited viability in a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 36913051). | 36913051 |
PIK3CA K111N | breast cancer | predicted - sensitive | GSK690693 | Preclinical - Cell culture | Actionable | In a preclinical study, GSK690693 treatment did not increase cell death but inhibited proliferation of a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 32439931). | 32439931 |
PIK3CA K111N | breast cancer | sensitive | ARQ 751 | Preclinical - Cell culture | Actionable | In a preclinical study, a breast cancer cell line harboring PIK3CA K111N was sensitive to ARQ 751 in culture, demonstrating inhibition of cell growth (PMID: 26469692). | 26469692 |
PIK3CA K111N | breast cancer | sensitive | ARQ 751 | Preclinical - Cell culture | Actionable | In a preclinical study, ARQ 751 treatment did not increase cell death but inhibited proliferation of a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 32439931). | 32439931 |
PIK3CA K111N | breast cancer | sensitive | DHM25 | Preclinical - Cell culture | Actionable | In a preclinical study, DHM25 increased cell death in a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 26237138). | 26237138 |
PIK3CA K111N | breast cancer | sensitive | Borussertib | Preclinical - Cell culture | Actionable | In a preclinical study, borussertib inhibited proliferation of a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 30858154). | 30858154 |
PIK3CA K111N | breast cancer | sensitive | AZD0156 + Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, AZD0156 and Miransertib (ARQ092) combination treatment increased cell death compared to Miransertib (ARQ092) alone in a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 32439931). | 32439931 |
PIK3CA K111N | breast cancer | sensitive | KU-57788 + Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, KU-57788 and Miransertib (ARQ092) combination treatment increased cell death compared to Miransertib (ARQ092) alone in a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 32439931). | 32439931 |
PIK3CA K111N | breast cancer | sensitive | Miransertib + OSU-T315 | Preclinical - Cell culture | Actionable | In a preclinical study, OSU-T315 and Miransertib (ARQ092) combination treatment increased cell death compared to Miransertib (ARQ092) alone in a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 32439931). | 32439931 |
PIK3CA K111N | breast cancer | sensitive | Ipatasertib + OSU-T315 | Preclinical - Cell culture | Actionable | In a preclinical study, OSU-T315 and Ipatasertib (GDC0068) combination treatment increased cell death compared to Ipatasertib (GDC0068) alone in a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 32439931). | 32439931 |
PIK3CA K111N | breast cancer | sensitive | GSK2334470 + Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, GSK2334470 and Miransertib (ARQ092) combination treatment increased cell death compared to Miransertib (ARQ092) alone in a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 32439931). | 32439931 |
PIK3CA M1043I | endometrial adenocarcinoma | no benefit | Copanlisib | Case Reports/Case Series | Actionable | In a Phase II (NRG-GY008) trial, Aliqopa (copanlisib) was well tolerated but demonstrated limited efficacy, resulted in stable disease in a patient with endometrioid adenocarcinoma harboring PIK3CA M1043I (PMID: 31934607). | 31934607 |
PIK3CA M1043I | lung squamous cell carcinoma | no benefit | Taselisib | Case Reports/Case Series | Actionable | In a Phase I (SWOG S1400B) trial, Taselisib (GDC-0032) treatment did not meet its primary endpoint for response rate in patients with lung squamous cell carcinoma harboring PIK3CA mutations, resulting in no response in a patient harboring PIK3CA M1043I (PMID: 31158500; NCT02785913). | 31158500 |
BRAF V600E PIK3CA M1043I | anaplastic thyroid carcinoma | sensitive | Dasatinib + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Sprycel (dasatinib) and Mekinist (trametinib) inhibited viability of an anaplastic thyroid cancer cell line harboring BRAF V600E and PIK3CA M1043I in culture (PMID: 37713162). | 37713162 |
PIK3CA M1043V | histiocytosis | predicted - sensitive | Alpelisib | Case Reports/Case Series | Actionable | In a clinical case study, Piqray (alpelisib) treatment resulted in symptom improvement and a complete metabolic response lasting at least 9 months in a patient with Langerhans cell histiocytosis harboring PIK3CA M1043V (PMID: 37874915). | 37874915 |
PIK3CA M1043V | head and neck squamous cell carcinoma | predicted - sensitive | Alpelisib | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, treatment with Piqray (alpelisib) resulted in inhibition of proliferation and increased apoptosis in a head and neck squamous cell carcinoma (HNSCC) cell line expressing PIK3CA M1043V in culture and led to inhibition of tumor growth and decreased phosphorylated Akt levels in a patient-derived xenograft (PDX) model of HNSCC with PIK3CA M1043V (PMID: 34779417). | 34779417 |
PIK3CA M1043V | Advanced Solid Tumor | sensitive | Sirolimus | Preclinical | Actionable | In a preclinical study, Rapamune (sirolimus) inhibited proliferation in cultured cells expressing PIK3CA M1043V (PMID: 17376864). | 17376864 |
PIK3CA M1043V | head and neck squamous cell carcinoma | sensitive | Celecoxib | Preclinical - Pdx | Actionable | In a preclinical study, Celebra (celecoxib) treatment reduced tumor growth rate in a patient-derived xenograft (PDX) model of head and neck squamous cell carcinoma harboring PIK3CA M1043V (PMID: 30683736). | 30683736 |
PIK3CA M1043V | head and neck squamous cell carcinoma | sensitive | Sulindac | Preclinical - Pdx | Actionable | In a preclinical study, Clinoril (sulindac) treatment reduced tumor growth rate in patient-derived xenograft (PDX) models of head and neck squamous cell carcinoma harboring PIK3CA mutations, including PIK3CA M1043V (PMID: 30683736). | 30683736 |
HRAS mut PIK3CA M1043V | high grade glioma | sensitive | Buparlisib + Selumetinib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination therapy of Buparlisib (BKM120) and Koselugo (selumetinib) led to a synergistic effect, resulting in growth inhibition of astrocytoma cells with an HRAS mutation and expressing PIK3CA M1043V in culture, but at a higher drug concentration compared to cells without mutant HRAS (PMID: 29975751). | 29975751 |
PIK3CA N1044K | colorectal cancer | predicted - sensitive | Alpelisib | Preclinical - Patient cell culture | Actionable | In a preclinical study, Piqray (alpelisib) inhibited cell proliferation in a patient-derived colorectal cancer organoid harboring PIK3CA N1044K, along with KRAS G12D, in culture (PMID: 32376656). | 32376656 |
PIK3CA N1044K | colorectal cancer | predicted - sensitive | MK2206 | Preclinical - Patient cell culture | Actionable | In a preclinical study, MK2206 inhibited cell proliferation in a patient-derived colorectal cancer organoid harboring PIK3CA N1044K, along with KRAS G12D, in culture (PMID: 32376656). | 32376656 |
PIK3CA N1044K | colorectal cancer | predicted - sensitive | Taselisib | Preclinical - Patient cell culture | Actionable | In a preclinical study, Taselisib (GDC-0032) inhibited cell proliferation in a patient-derived colorectal cancer organoid harboring PIK3CA N1044K, along with KRAS G12D, in culture (PMID: 32376656). | 32376656 |
PIK3CA N345K | breast cancer | sensitive | Trametinib | Preclinical | Actionable | In a preclinical study, Mekinist (trametinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA N345K in culture (PMID: 26627007). | 26627007 |
PIK3CA N345K | Advanced Solid Tumor | sensitive | Trametinib | Preclinical | Actionable | In a preclinical study, Mekinist (trametinib) inhibited survival of transformed cell lines overexpressing PIK3CA N345K in culture (PMID: 26627007). | 26627007 |
PIK3CA N345K | breast cancer | sensitive | Dactolisib | Preclinical | Actionable | In a preclinical study, BEZ235 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA N345K in culture (PMID: 26627007). | 26627007 |
PIK3CA N345K | breast cancer | sensitive | Alpelisib | Preclinical - Cell culture | Actionable | In a preclinical study, Alpelisib (BYL719) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA N345K in culture (PMID: 26627007). | 26627007 |
PIK3CA N345K | head and neck squamous cell carcinoma | predicted - sensitive | Alpelisib | Preclinical - Cell culture | Actionable | In a preclinical study, treatment with Piqray (alpelisib) resulted in inhibition of proliferation and increased apoptosis in a head and neck squamous cell carcinoma cell line expressing PIK3CA N345K in culture (PMID: 34779417). | 34779417 |
PIK3CA N345K | breast cancer | sensitive | Lapatinib | Preclinical | Actionable | In a preclinical study, Tykerb (lapatinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA N345K in culture (PMID: 26627007). | 26627007 |
PIK3CA N345K | breast cancer | sensitive | MK2206 | Preclinical | Actionable | In a preclinical study, MK2206 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA N345K in culture (PMID: 26627007). | 26627007 |
PIK3CA N345K | breast cancer | sensitive | Neratinib | Preclinical | Actionable | In a preclinical study, Nerlynx (neratinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA N345K in culture (PMID: 26627007). | 26627007 |
PIK3CA N345K | endometrial mixed adenocarcinoma | no benefit | Copanlisib | Case Reports/Case Series | Actionable | In a Phase II (NRG-GY008) trial, Aliqopa (copanlisib) was well tolerated but demonstrated limited efficacy, resulted in stable disease in a patient with endometrial mixed adenocarcinoma harboring PIK3CA N345K (PMID: 31934607). | 31934607 |
PIK3CA N345K | lung squamous cell carcinoma | no benefit | Taselisib | Case Reports/Case Series | Actionable | In a Phase I (SWOG S1400B) trial, Taselisib (GDC-0032) treatment did not meet its primary endpoint for response rate in patients with lung squamous cell carcinoma harboring PIK3CA mutations, resulting in no response in two patients harboring PIK3CA N345K (PMID: 31158500; NCT02785913). | 31158500 |
PIK3CA V344G | glioblastoma | no benefit | YM-024 | Preclinical | Actionable | In a preclinical study, YM-024 did not inhibit proliferation of glioblastoma cell lines harboring PIK3CA V344G in culture (PMID: 24718026). | 24718026 |
PIK3CA Q75E | head and neck squamous cell carcinoma | predicted - sensitive | Alpelisib | Case Reports/Case Series | Actionable | In clinical case study, treatment with Piqray (alpelisib) resulted in a partial response with 73% tumor shrinkage in a patient with head and neck squamous cell carcinoma (HNSCC) harboring PIK3CA Q75E, and in a preclinical analysis, resulted in inhibition of proliferation and increased apoptosis in a HNSCC cell line expressing PIK3CA Q75E in culture (PMID: 34779417). | 34779417 |
PIK3CA R108H PTEN mut | endometrial cancer | sensitive | Dactolisib | Preclinical | Actionable | In a preclinical study, BEZ235 inhibited proliferation of endometrial cancer cells harboring PIK3CA R108H and PTEN mutations in culture (PMID: 22662154). | 22662154 |
PIK3CA R38C | head and neck squamous cell carcinoma | sensitive | Sulindac | Preclinical - Pdx | Actionable | In a preclinical study, Clinoril (sulindac) treatment reduced tumor growth rate in patient-derived xenograft (PDX) models of head and neck squamous cell carcinoma harboring PIK3CA mutations, including PIK3CA R38C (PMID: 30683736). | 30683736 |
PIK3CA R38C PTEN mut | endometrial cancer | sensitive | Dactolisib | Preclinical | Actionable | In a preclinical study, BEZ235 decreased growth of endometrial cancer cells harboring PIK3CA R38C and PTEN mutations in culture and in xenograft models (PMID: 22662154). | 22662154 |
PIK3CA R38C PTEN loss | endometrial cancer | sensitive | MEN1611 | Preclinical | Actionable | In a preclinical study, MEN1611 (CH5132799) inhibited proliferation of an endometrial cancer cell line harboring PIK3CA R38C and PTEN loss in culture (PMID: 21558396). | 21558396 |
PIK3CA E365K PTEN mut | endometrial cancer | sensitive | Dactolisib | Preclinical | Actionable | In a preclinical study, BEZ235 inhibited proliferation of endometrial cancer cells harboring PIK3CA E365K and PTEN mutations in culture (PMID: 22662154). | 22662154 |
PIK3CA E365K PTEN mut | endocervical carcinoma | sensitive | Dactolisib | Preclinical | Actionable | In a preclinical study, BEZ235 inhibited proliferation of endometrial cancer cells harboring PIK3CA E365K and PTEN mutations in culture (PMID: 22662154). | 22662154 |
PIK3CA E545X | endometrial adenocarcinoma | no benefit | Copanlisib | Case Reports/Case Series | Actionable | In a Phase II (NRG-GY008) trial, Aliqopa (copanlisib) was well tolerated but demonstrated limited efficacy, resulted in progressive disease in a patient with endometrioid adenocarcinoma harboring a PIK3CA E545 mutation, and progressive disease in a patient with serous endometrial adenocarcinoma harboring a PIK3CA E545 mutation (PMID: 31934607). | 31934607 |
PIK3CA H1047X | endometrial adenocarcinoma | predicted - sensitive | Temsirolimus | Case Reports/Case Series | Actionable | In a clinical study, a patient with endometrial adenocarcinoma harboring a PIK3CA H1047 mutation demonstrated a partial response when treated with Torisel (temsirolimus) (PMID: 21216929). | 21216929 |
PIK3CA H1047X | endometrial adenocarcinoma | no benefit | Copanlisib | Case Reports/Case Series | Actionable | In a Phase II (NRG-GY008) trial, Aliqopa (copanlisib) was well tolerated but demonstrated limited efficacy, resulted in progressive disease in a patient with endometrioid adenocarcinoma harboring a PIK3CA H1047 mutation (PMID: 31934607). | 31934607 |
PIK3CA H1047X | endometrial mixed adenocarcinoma | no benefit | Copanlisib | Case Reports/Case Series | Actionable | In a Phase II (NRG-GY008) trial, Aliqopa (copanlisib) was well tolerated but demonstrated limited efficacy, resulted in progressive disease in a patient with endometrial mixed adenocarcinoma harboring a PIK3CA H1047 mutation (PMID: 31934607). | 31934607 |
PIK3CA H1047X | lung non-small cell carcinoma | sensitive | Taselisib | Phase I | Actionable | In a Phase I trial, a non-small cell lung carcinoma patient harboring a mutation at PIK3CA H1047 demonstrated a confirmed partial response when treated with Taselisib (GDC-0032) (PMID: 28331003). | 28331003 |
PIK3CA H1047X | colorectal cancer | predicted - resistant | Bevacizumab + Temsirolimus | Case Reports/Case Series | Actionable | In a clinical study, a colorectal cancer patient harboring a mutation at PIK3CA H1047 demonstrated progressive disease when treated with Torisel (temsirolimus) and Avastin (bevacizumab) (PMID: 21216929). | 21216929 |
PIK3CA H1047X | small intestine adenocarcinoma | predicted - resistant | Bortezomib + Temsirolimus + Topotecan | Case Reports/Case Series | Actionable | In a clinical study, the combination of Torisel (temsirolimus) plus Velcade (bortezomib) and Hycamtin (topotecan) resulted in progressive disease in a patient with small intestine adenocarcinoma harboring a PIK3CA H1047 mutation (PMID: 21216929). | 21216929 |
BRAF V600X PIK3CA H1047X | ovarian carcinoma | predicted - sensitive | Bevacizumab + Pegylated liposomal doxorubicin + Temsirolimus | Case Reports/Case Series | Actionable | In a clinical study, the combination of Torisel (temsirolimus) plus Avastin (bevacizumab) and Doxil (pegylated liposomal-doxorubicin) resulted in a partial response in a patient with ovarian clear cell carcinoma harboring PIK3CA H1047 and BRAF V600 mutations (PMID: 21216929). | 21216929 |
PIK3CA R93W PIK3CA D350G PTEN R130G | endometrial cancer | sensitive | Miransertib | Preclinical - Pdx | Actionable | In a preclinical study, a patient-derived xenograft (PDX) model of endometrial cancer harboring PIK3CA D350G, PIK3CA R93W, and PTEN R130G was sensitive to Miransertib (ARQ092), demonstrating greater than 90% inhibition of tumor growth (PMID: 26469692). | 26469692 |
PIK3CA E39K | breast cancer | resistant | Buparlisib | Preclinical - Cell culture | Actionable | In a preclinical study, breast cancer cells expressing PIK3CA E39K demonstrated resistance to treatment with Buparlisib (BKM120) in culture (PMID: 29636477). | 29636477 |
PIK3CA R88L PIK3CA E453del PIK3CA T1052K PTEN loss PTEN mut | endometrial carcinoma | sensitive | Copanlisib | Phase I | Actionable | In a Phase I clinical trial, an endometrial carcinoma patient harboring PIK3CA T1052K, R88L, and E453del, as well as a PTEN mutation and loss of PTEN protein expression demonstrated a complete response to treatment with Aliqopa (copanlisib) (PMID: 27672108). | 27672108 |
PIK3CA N345I | breast cancer | resistant | Buparlisib | Preclinical - Cell culture | Actionable | In a preclinical study, breast cancer cells expressing PIK3CA N345I demonstrated resistance to treatment with Buparlisib (BKM120) in culture (PMID: 29636477). | 29636477 |
PIK3CA P449T | colorectal cancer | sensitive | Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, Miransertib (ARQ092) treatment induced cell death and inhibited proliferation of a colorectal cancer cell line harboring PIK3CA P449T in culture (PMID: 32439931). | 32439931 |
PIK3CA P449T | colorectal cancer | predicted - sensitive | Ipatasertib | Preclinical - Cell culture | Actionable | In a preclinical study, Ipatasertib (GDC-0068) treatment did not increase cell death but inhibited proliferation of a breast cancer cell line harboring PIK3CA P449T in culture (PMID: 32439931). | 32439931 |
PIK3CA P449T | colorectal cancer | sensitive | MK2206 | Preclinical - Cell culture | Actionable | In a preclinical study, MK2206 treatment induced cell death and inhibited proliferation of a colorectal cancer cell line harboring PIK3CA P449T in culture (PMID: 32439931). | 32439931 |
PIK3CA P449T | colorectal cancer | sensitive | GSK690693 | Preclinical - Cell culture | Actionable | In a preclinical study, GSK690693 treatment induced cell death and inhibited proliferation of a colorectal cancer cell line harboring PIK3CA P449T in culture (PMID: 32439931). | 32439931 |
PIK3CA P449T | colorectal cancer | sensitive | ARQ 751 | Preclinical - Cell culture | Actionable | In a preclinical study, ARQ 751 treatment induced cell death and inhibited proliferation of a colorectal cancer cell line harboring PIK3CA P449T in culture (PMID: 32439931). | 32439931 |
BRAF V600E PIK3CA P449T | colorectal cancer | resistant | Cetuximab | Preclinical | Actionable | In a preclinical study, human colorectal cancer cells harboring BRAF V600E and PIK3CA P449T were resistant to Erbitux (cetuximab) in culture (PMID: 25838391). | 25838391 |
BRAF V600E PIK3CA P449T | colorectal cancer | sensitive | Pimasertib | Preclinical - Cell culture | Actionable | In a preclinical study, Pimasertib (MSC1936369B) inhibited proliferation of colorectal cancer cells harboring BRAF V600E and PIK3CA P449T in culture (PMID: 23629727). | 23629727 |
BRAF V600E PIK3CA P449T | colorectal cancer | resistant | Regorafenib | Preclinical | Actionable | In a preclinical study, human colorectal cancer cells harboring BRAF V600E and PIK3CA P449T were resistant to Stivarga (regorafenib) in culture (PMID: 25838391). | 25838391 |
BRAF V600E PIK3CA P449T | colorectal cancer | sensitive | Cetuximab + Regorafenib | Preclinical | Actionable | In a preclinical study, the combination of Erbitux (cetuximab) and Stivarga (regorafenib) inhibited growth, reduced Akt and Mapk phosphorylation, and induced apoptosis of human colorectal cancer cell lines harboring BRAF V600E and PIK3CA P449T in culture (PMID: 25838391). | 25838391 |
BRAF V600E PIK3CA P449T | colorectal cancer | sensitive | Pimasertib + Sorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Pimasertib (MSC1936369B) and Nexavar (sorafenib) synergistically inhibited proliferation of colorectal cancer cells harboring BRAF V600E and PIK3CA P449T in culture (PMID: 23629727). | 23629727 |
BRAF V600E PIK3CA P449T | colorectal cancer | sensitive | Everolimus + Pimasertib | Preclinical - Cell culture | Actionable | In a preclinical study, Pimasertib (MSC1936369B) and Afinitor (everolimus) synergistically inhibited proliferation of colorectal cancer cells harboring BRAF V600E and PIK3CA P449T in culture (PMID: 23629727). | 23629727 |
BRAF V600E PIK3CA P449T | colorectal cancer | sensitive | Pimasertib + Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Pimasertib (MSC1936369B) and Stivarga (regorafenib) synergistically inhibited proliferation of colorectal cancer cells harboring BRAF V600E and PIK3CA P449T in culture (PMID: 23629727). | 23629727 |
BRAF V600E PIK3CA P449T TP53 R273H | colorectal cancer | sensitive | PD-0325901 + Sapanisertib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Sapanisertib (MLN0128) and PD-0325901 synergistically inhibited Erk and PI3K signaling and growth of colorectal cancer cells harboring BRAF V600E, PIK3CA P449T, and TP53 R273H in culture and in cell line xenograft models, but did not have synergistic effect on apoptosis (PMID: 26272063). | 26272063 |
PIK3CA over exp | lung squamous cell carcinoma | sensitive | Dactolisib | Preclinical - Cell culture | Actionable | In a preclinical study, BEZ235 induced apoptosis, inhibited cell proliferation, migration, and invasion of lung squamous cell carcinoma cells over expressing wild-type Pik3ca in culture (PMID: 26013318). | 26013318 |
PIK3CA over exp | lung squamous cell carcinoma | sensitive | Buparlisib | Preclinical - Cell culture | Actionable | In a preclinical study, Buparlisib (BKM120) induced apoptosis, inhibited cell proliferation, migration, and invasion of lung squamous cell carcinoma cells over expressing wild-type Pik3ca in culture (PMID: 26013318). | 26013318 |
PIK3CA over exp | lung squamous cell carcinoma | sensitive | Alpelisib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Alpelisib (BYL719) induced apoptosis, inhibited cell proliferation, migration, and invasion of lung squamous cell carcinoma cells over expressing wild-type PIK3CA in culture, and inhibited tumor growth in cell line xenograft models (PMID: 26013318). | 26013318 |
PIK3CA over exp | head and neck squamous cell carcinoma | sensitive | Gedatolisib | Preclinical - Cell culture | Actionable | In a preclinical study, some head and neck squamous cell carcinoma cell lines over expressing PIK3CA demonstrated sensitivity to treatment with Gedatolisib (PF-05212384) (PMID: 25977343). | 25977343 |
PIK3CA over exp | glioblastoma | sensitive | YM-024 | Preclinical | Actionable | In a preclinical study, YM-024 inhibited proliferation and anchorage-independent growth of glioblastoma cell lines with elevated Pik3ca protein level in culture (PMID: 24718026). | 24718026 |
PIK3CA E78K PIK3CA E726K PIK3CA D939G | estrogen-receptor positive breast cancer | no benefit | Alpelisib + Letrozole | Phase Ib/II | Actionable | In a Phase Ib trial, an estrogen-receptor positive breast cancer patient harboring PIK3CA mutations, E78K, D939G, and E726K, demonstrated progressive disease when treated with a combination of Femara (letrozole) and Alpelisib (BYL719) (PMID: 27126994). | 27126994 |
FGFR3 S249C FGFR3 E587Q FGFR3 amp PIK3CA E726K TSC1 S561fs | bladder urothelial carcinoma | predicted - resistant | Erdafitinib | Case Reports/Case Series | Actionable | In a clinical case study, FGFR3 E587Q was identified in the post-progression circulating tumor DNA and FGFR3 amplification (>10 copies) and PIK3CA E726K were identified in the post-progression tissue biopsy of a patient with bladder urothelial cancer harboring FGFR3 S249C and TSC1 S561fs who previously responded to Balversa (erdafitinib) treatment (PMID: 37377403). | 37377403 |
PIK3CA P447_L455del | estrogen-receptor positive breast cancer | predicted - sensitive | Alpelisib + Letrozole | Case Reports/Case Series | Actionable | In a clinical case study, a patient with estrogen-receptor positive breast cancer harboring PIK3CA P447_L455del demonstrated an 11 month sustained response to the combination therapy of Femara (letrozole) and Alpelisib (BYL719) (PMID: 29284706). | 29284706 |
BRAF V600E PIK3CA H1047K | melanoma | sensitive | Miransertib + Trametinib | Preclinical - Pdx | Actionable | In a preclinical study, a melanoma patient-derived xenograft (PDX) model harboring BRAF V600E and PIK3CA H1047K was sensitive to the combination treatment of Miransertib (ARQ092) and Mekinist (trametinib), demonstrating a greater inhibition of tumor growth when compared to either agent alone (PMID: 26469692). | 26469692 |
PIK3CA K944N | colorectal cancer | resistant | Cetuximab + Fluorouracil | Case Reports/Case Series | Actionable | In a clinical study, PIK3CA K944N was identified as a potential mechanism for acquired Erbitux (cetuximab) resistance in two colorectal cancer patients, which is supported by cell culture studies demonstrating resistance to Erbitux (cetuximab) and Fluorouracil combination treatment in colorectal cancer cells over expressing PIK3CA K944N (PMID: 28424201). | 28424201 |
PIK3CA V955G | colorectal cancer | resistant | Cetuximab + Fluorouracil | Case Reports/Case Series | Actionable | In a clinical study, PIK3CA V955G was identified as a potential mechanism for acquired Erbitux (cetuximab) resistance in a colorectal cancer patient, which is supported by cell culture studies demonstrating resistance to Erbitux (cetuximab) and Fluorouracil combination treatment in colorectal cancer cells over expressing PIK3CA V955G (PMID: 28424201). | 28424201 |
PIK3CA V955I | colorectal cancer | resistant | Cetuximab + Fluorouracil | Case Reports/Case Series | Actionable | In a clinical study, PIK3CA V955I was identified as a potential mechanism for acquired Erbitux (cetuximab) resistance in a colorectal cancer patient, which is supported by cell culture studies demonstrating resistance to Erbitux (cetuximab) and Fluorouracil combination treatment in colorectal cancer cells over expressing PIK3CA V955I (PMID: 28424201). | 28424201 |
PIK3CA K966E | colorectal cancer | resistant | Cetuximab + Fluorouracil | Clinical Study - Cohort | Actionable | In a clinical study, PIK3CA K966E was identified as a potential mechanism for acquired Erbitux (cetuximab) resistance in a colorectal cancer patient, which is supported by cell culture studies demonstrating resistance to Erbitux (cetuximab) and Fluorouracil combination treatment in colorectal cancer cells overexpressing PIK3CA K966E (PMID: 28424201). | 28424201 |
PIK3CA F930S | colorectal cancer | resistant | Cetuximab + Fluorouracil | Case Reports/Case Series | Actionable | In a clinical study, PIK3CA F930S was identified as a potential mechanism for acquired Erbitux (cetuximab) resistance in a colorectal cancer patient, which is consistent with cell culture studies demonstrating moderate resistance to Erbitux (cetuximab) and Fluorouracil combination treatment in colorectal cancer cells over expressing PIK3CA F930S (PMID: 28424201). | 28424201 |
PIK3CA V952A | colorectal cancer | resistant | Cetuximab + Fluorouracil | Case Reports/Case Series | Actionable | In a clinical study, PIK3CA V952A was identified as a potential mechanism for acquired Erbitux (cetuximab) resistance in a colorectal cancer patient, which is consistent with cell culture studies demonstrating moderate resistance to Erbitux (cetuximab) and Fluorouracil combination treatment in colorectal cancer cells over expressing PIK3CA V952A (PMID: 28424201). | 28424201 |
PIK3CA P124L | urinary bladder cancer | resistant | MK2206 | Preclinical - Cell culture | Actionable | In a preclinical study, a bladder cancer cell line harboring PIK3CA P124L was resistant to MK2206 in culture (PMID: 25349966). | 25349966 |
PIK3CA P124L PTEN del | urinary bladder cancer | decreased response | Pictilisib | Preclinical - Cell culture | Actionable | In a preclinical study, Pictilisib (GDC-0941) demonstrated limited inhibition of Akt phosphorylation and growth in bladder cancer cells harboring PIK3CA P124L and PTEN deletion in culture (PMID: 28808038). | 28808038 |
FGFR3 K652E PIK3CA P124L | urinary bladder cancer | sensitive | Alpelisib + Nintedanib | Preclinical - Cell culture | Actionable | In a preclinical study, combination treatment with Ofev (nintedanib) and Piqray (alpelisib) led to synergistic inhibition of growth in a bladder cancer cell line harboring FGFR3 K652E and PIK3CA P124L in culture (PMID: 36805958). | 36805958 |
FGFR3 K652E PIK3CA P124L | urinary bladder cancer | sensitive | Nintedanib + Pictilisib | Preclinical - Cell culture | Actionable | In a preclinical study, combination treatment with Ofev (nintedanib) and Pictilisib (GDC-0941) inhibited cell proliferation in a bladder cancer cell line harboring FGFR3 K652E PIK3CA P124L in culture (PMID: 36805958). | 36805958 |
PIK3CA D549Y | urinary bladder cancer | decreased response | Pictilisib | Preclinical - Pdx | Actionable | In a preclinical study, Pictilisib (GDC-0941) demonstrated limited tumor growth inhibition and survival benefit in patient-derived xenograft (PDX) models of bladder cancer harboring PIK3CA D549Y (PMID: 28808038). | 28808038 |
PIK3CA H450_P458del | breast cancer | sensitive | Alpelisib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed breast epithelial cells expressing PIK3CA H450_P458del were sensitive to treatment with Alpelisib (BYL719) in culture, demonstrating growth inhibition and decreased invasiveness of acini (PMID: 29284706). | 29284706 |
PIK3CA N1068Kfs*5 PTEN Y174H PTEN K263* | colorectal cancer | predicted - sensitive | Alpelisib | Preclinical - Patient cell culture | Actionable | In a preclinical study, Piqray (alpelisib) inhibited cell proliferation in a patient-derived colorectal cancer organoid harboring PIK3CA N1068Kfs*5, PTEN Y174H, and PTEN K263* in culture (PMID: 32376656). | 32376656 |
PIK3CA N1068Kfs*5 PTEN Y174H PTEN K263* | colorectal cancer | predicted - sensitive | Taselisib | Preclinical - Patient cell culture | Actionable | In a preclinical study, Taselisib (GDC-0032) inhibited cell proliferation in a patient-derived colorectal cancer organoid harboring PIK3CA N1068Kfs*5, PTEN Y174H, and PTEN K263* in culture (PMID: 32376656). | 32376656 |
PIK3CA F977Y | head and neck squamous cell carcinoma | resistant | Pictilisib | Preclinical - Cell culture | Actionable | In a preclinical study, a head and neck squamous cell carcinoma cell line harboring PIK3CA F977Y demonstrated resistance to growth inhibition by Pictilisib (GDC-0941) in culture (PMID: 30108165). | 30108165 |
PIK3CA Q546X | endometrial adenocarcinoma | no benefit | Copanlisib | Case Reports/Case Series | Actionable | In a Phase II (NRG-GY008) trial, Aliqopa (copanlisib) was well tolerated but demonstrated limited efficacy, resulted in 1 stable disease and 1 progressive disease in 2 patients with endometrioid adenocarcinoma harboring PIK3CA Q546 mutations, and stable disease in a patient with serous endometrial adenocarcinoma harboring a PIK3CA Q546 mutation (PMID: 31934607). | 31934607 |
PIK3CA exon10 | Her2-receptor negative breast cancer | predicted - sensitive | Everolimus | Phase III | Actionable | In a retrospective analysis of a Phase III trial (BOLERO-2), Afinitor (everolimus) demonstrated greater benefit on progression-free survival in patients with hormone receptor-positive, Erbb2 (Her2)-negative breast cancer harboring PIK3CA exon 10 (reported as exon 9) mutations (HR=0.26) compared to patients harboring PIK3CA exon 21 (reported as exon 20) mutations (HR=0.56) (PMID: 26503204; NCT00863655). | 26503204 |
PIK3CA exon21 | Her2-receptor negative breast cancer | no benefit | Everolimus | Phase III | Actionable | In a retrospective analysis of a Phase III trial (BOLERO-2), Afinitor (everolimus) demonstrated greater benefit on progression-free survival in patients with hormone receptor-positive, Erbb2 (Her2)-negative breast cancer harboring PIK3CA exon 10 (reported as exon 9) mutations (HR=0.26) compared to patients harboring PIK3CA exon 21 (reported as exon 20) mutations (HR=0.56) (PMID: 26503204; NCT00863655). | 26503204 |
PIK3CA A1066V | urinary bladder cancer | resistant | MK2206 | Preclinical - Cell culture | Actionable | In a preclinical study, a bladder cancer cell line harboring PIK3CA A1066V, along with KRAS and NRAS mutations, was resistant to MK2206 in culture (PMID: 25349966). | 25349966 |
FGFR3 R248C PIK3CA A1066V | urinary bladder cancer | sensitive | Nintedanib + Pictilisib | Preclinical - Cell culture | Actionable | In a preclinical study, combination treatment with Ofev (nintedanib) and Pictilisib (GDC-0941) inhibited cell proliferation in a bladder cancer cell line harboring FGFR3 R248C and PIK3CA A1066V in culture (PMID: 36805958). | 36805958 |