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Molecular Profile Indication/Tumor Type Response Type Relevant Treatment Approaches Therapy Name Approval Status Evidence Type Efficacy Evidence References
PIK3CA H1047R breast cancer sensitive mTOR Inhibitor PI3K Inhibitor (Pan) 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 Her2-receptor negative breast cancer no benefit mTORC1 Inhibitor 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 sensitive PIK3CA inhibitor 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 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 progesterone-receptor positive breast cancer predicted - sensitive mTORC1 Inhibitor 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 Advanced Solid Tumor predicted - sensitive PIK3CA inhibitor 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 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 PIK3CA inhibitor 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 lung cancer no benefit mTORC1 Inhibitor 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 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 Advanced Solid Tumor sensitive PIK3CA inhibitor 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 ovarian cancer sensitive mTOR Inhibitor PI3K Inhibitor (Pan) 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 breast cancer sensitive Akt Inhibitor (Pan) 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 lung cancer sensitive mTOR Inhibitor PI3K Inhibitor (Pan) 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 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 breast cancer sensitive PIK3CA inhibitor 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 thyroid gland cancer sensitive Akt Inhibitor (Pan) mTORC1 Inhibitor 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 breast metaplastic carcinoma predicted - sensitive PI3K Inhibitor (Pan) 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 breast cancer sensitive Akt1 Inhibitor Akt2 Inhibitor 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 thyroid gland cancer sensitive Akt Inhibitor (Pan) 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 PI3K Inhibitor (Pan) 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 Advanced Solid Tumor sensitive PI3K Inhibitor (Pan) 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 Advanced Solid Tumor sensitive mTORC1 Inhibitor 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 head and neck squamous cell carcinoma sensitive mTOR Inhibitor PI3K Inhibitor (Pan) 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 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 breast cancer sensitive PI3K Inhibitor (Pan) CH5132799 Preclinical Actionable In a preclinical study, CH5132799 inhibited proliferation of breast cancer cells harboring PIK3CA H1047R in culture (PMID: 21558396). 21558396
PIK3CA H1047R breast cancer sensitive PIK3CA inhibitor 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 malignant glioma sensitive PI3K Inhibitor (Pan) 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 lung squamous cell carcinoma no benefit PIK3CA inhibitor 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, none of the 4 patients harboring PIK3CA H1047R demonstrated response (PMID: 31158500; NCT02785913). 31158500
PIK3CA H1047R lung squamous cell carcinoma sensitive PI3K Inhibitor (Pan) 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 H1047R urinary bladder cancer sensitive mTOR Inhibitor PI3K Inhibitor (Pan) 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 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 lung adenocarcinoma sensitive mTOR Inhibitor PI3K Inhibitor (Pan) 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 lung squamous cell carcinoma sensitive PIK3CA inhibitor 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 sensitive mTOR Inhibitor 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 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 mTOR Inhibitor 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 breast cancer sensitive Akt1 Inhibitor 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 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 breast cancer sensitive Akt Inhibitor (Pan) 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 mTOR Inhibitor PI3K Inhibitor (Pan) 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 ovarian cancer sensitive PI3K Inhibitor (Pan) CH5132799 Phase I Actionable In a Phase I trial, 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 ovarian cancer sensitive PIK3CA inhibitor 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 sensitive mTORC1 Inhibitor 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 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 urinary bladder cancer sensitive PI3K Inhibitor (Pan) 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 urinary bladder cancer sensitive PI3K Inhibitor (Pan) 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 Akt Inhibitor (Pan) MK2206 Preclinical Actionable In a preclinical study, MK2206 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA H1047R in culture (PMID: 26627007). 26627007
PIK3CA H1047R lung adenocarcinoma no benefit mTORC1 Inhibitor 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 head and neck squamous cell carcinoma sensitive PIK3CA inhibitor 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 Akt Inhibitor (Pan) 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 mTOR Inhibitor 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 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 lung squamous cell carcinoma sensitive mTOR Inhibitor PI3K Inhibitor (Pan) 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 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 stomach cancer sensitive Akt Inhibitor (Pan) Capivasertib Preclinical - Pdx Actionable In a preclinical study, AZD5363 inhibited growth in a patient-derived xenograft model of gastric cancer harboring a PIK3CA H1047R mutation (PMID: 24088382). 24088382
PIK3CA H1047R estrogen-receptor positive breast cancer predicted - sensitive mTORC1 Inhibitor 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
Clinical Trial Phase Therapies Title Recruitment Status
NCT03941782 Phase 0 Alpelisib Compassionate Use of BYL 719 Alpelisib Available