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Profile Name PIK3CA E545K
Gene Variant Detail

PIK3CA E545K (gain of function)

Relevant Treatment Approaches Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
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
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
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
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
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
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 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 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 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
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 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
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 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 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 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 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 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 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
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 - 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 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
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
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
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
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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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