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Molecular Profile Indication/Tumor Type Response Type Relevant Treatment Approaches Therapy Name Approval Status Evidence Type Efficacy Evidence References
PIK3CA E545K Advanced Solid Tumor resistant PIK3CA inhibitor 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 colorectal cancer sensitive mTOR Inhibitor PI3K Inhibitor (Pan) 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 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 E545K in culture (PMID: 26013318). 26013318
PIK3CA E545K breast cancer sensitive mTORC1 Inhibitor 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 urinary bladder cancer sensitive PI3K Inhibitor (Pan) 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 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 PIK3CA E545K in culture (PMID: 26013318). 26013318
PIK3CA E545K head and neck squamous cell carcinoma predicted - sensitive mTORC1 Inhibitor 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 gastrointestinal system cancer sensitive Akt Inhibitor (Pan) Capivasertib Preclinical Actionable In a preclinical study, gastric cancer cells harboring PI3KCA E545K mutations were sensitive to the AKT inhibitor AZD5363 (PMID: 24088382). 24088382
PIK3CA E545K stomach cancer sensitive Akt Inhibitor (Pan) Capivasertib Preclinical - Cell culture Actionable In a preclinical study, a gastric cancer cell line harboring PIK3CA E545K was sensitive to treatment with Capivasertib (AZD5363), demonstrating decreased cell proliferation in culture (PMID: 32070411). 32070411
PIK3CA E545K thyroid gland cancer sensitive Akt Inhibitor (Pan) 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 breast cancer no benefit mTOR Inhibitor PI3K Inhibitor (Pan) 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 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 Akt Inhibitor (Pan) 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 mTOR Inhibitor PI3K Inhibitor (Pan) 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 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 E545K in culture (PMID: 27104980). 27104980
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 breast cancer sensitive Akt1 Inhibitor 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 urinary bladder cancer sensitive PI3K Inhibitor (Pan) 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 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, only 1 of the 11 patients harboring PIK3CA E545K demonstrated response (PMID: 31158500; NCT02785913). 31158500
PIK3CA E545K Advanced Solid Tumor sensitive mTOR Inhibitor PI3K Inhibitor (Pan) GDC-0980 Phase I Actionable In a Phase I trial, Apitolisib (GDC-0980) resulted in a partial response in two patients, one with head and neck squamous cell carcinoma and another with ovarian cancer, both harboring PIK3CA E545K (PMID: 26787751). 26787751
PIK3CA E545K breast cancer sensitive PI3K Inhibitor (Pan) CH5132799 Preclinical Actionable In a preclinical study, CH5132799 inhibited proliferation of breast cancer cells expressing PIK3CA E545K (PMID: 21558396). 21558396
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 breast cancer sensitive mTOR Inhibitor 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 breast cancer predicted - sensitive mTOR Inhibitor PI3K Inhibitor (Pan) 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 mTOR Inhibitor PI3K Inhibitor (Pan) 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 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 E545K in culture (PMID: 26627007). 26627007
PIK3CA E545K estrogen-receptor positive breast cancer sensitive PIK3CA inhibitor 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 ovarian cancer sensitive PI3K Inhibitor (Pan) CH5132799 Preclinical Actionable In a preclinical study, CH5132799 inhibited proliferation of ovarian cancer cells harboring PIK3CA E545K in culture (PMID: 21558396). 21558396
PIK3CA E545K breast cancer sensitive Akt1 Inhibitor Akt2 Inhibitor 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 breast cancer sensitive Akt Inhibitor (Pan) 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 Akt Inhibitor (Pan) Ipatasertib + Paclitaxel Preclinical - Cell line xenograft Actionable In a preclinical study, the combination of Ipatasertib (GDC-0068) and Taxol (paclitaxel) synergistically inhibited tumor growth in cell line xenograft models of breast cancer cells harboring PIK3CA E545K (PMID: 32205017). 32205017
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 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 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 breast cancer sensitive mTOR Inhibitor 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 breast cancer sensitive mTOR Inhibitor PI3K Inhibitor (Pan) 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 breast cancer sensitive Akt Inhibitor (Pan) 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 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 E545K in culture (PMID: 26013318). 26013318
PIK3CA E545K cervical cancer sensitive PIK3CA inhibitor PW12 Preclinical Actionable In a preclinical study, PW12 inhibited proliferation of cervical cancer cells with a PIK3CA E545K mutation (PMID: 22391131). 22391131
PIK3CA E545K 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 E545K Advanced Solid Tumor sensitive mTORC1 Inhibitor 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 Klatskin's tumor unknown mTORC1 Inhibitor 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 PIK3CA inhibitor 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 esophagus squamous cell carcinoma sensitive PI3K Inhibitor (Pan) 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 lung non-small cell carcinoma sensitive PIK3CA inhibitor 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 colon cancer sensitive Akt Inhibitor (Pan) LY2780301 Phase I 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 leukemia sensitive mTOR Inhibitor PI3K Inhibitor (Pan) 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 head and neck squamous cell carcinoma sensitive PI3K Inhibitor (Pan) 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 breast cancer resistant PI3K Inhibitor (Pan) 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 breast cancer sensitive PIK3CA inhibitor 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 breast carcinoma sensitive PI3K Inhibitor (Pan) 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 Akt Inhibitor (Pan) Ipatasertib Preclinical - Cell line xenograft Actionable In a preclinical study, Ipatasertib (GDC-0068) demonstrated activity against tumor growth in cell line xenograft models of breast cancer cells harboring PIK3CA E545K (PMID: 32205017). 32205017
PIK3CA E545K urinary bladder cancer sensitive PI3K Inhibitor (Pan) 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 PI3K Inhibitor (Pan) 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 predicted - sensitive PIK3CA inhibitor 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
Clinical Trial Phase Therapies Title Recruitment Status