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Profile Name | PIK3CA H1047R |
Gene Variant Detail | |
Relevant Treatment Approaches | Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
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 |
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 | 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 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 | 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 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 |
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 | 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 | 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 |
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 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 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 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 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 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 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 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 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 |
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 | 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 | 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 |
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 |
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 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 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 |
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 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 | 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 | 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 | 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 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 | 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 | 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 | 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 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 | 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 | 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 | 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 | 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 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 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 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 |
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 |
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 |
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 |
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 |