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Profile Name PIK3CA K111N
Gene Variant Detail

PIK3CA K111N (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 Relevant Treatment Approaches Therapy Name Approval Status Evidence Type Efficacy Evidence References
PIK3CA K111N 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 K111N in culture and induced tumor regression in xenograft models (PMID: 26839307). 26839307
PIK3CA K111N breast cancer sensitive Akt1 Inhibitor Akt2 Inhibitor 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 breast cancer sensitive Akt Inhibitor (Pan) 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 Akt Inhibitor (Pan) 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 mTOR Inhibitor 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 Akt1 Inhibitor 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 Akt Inhibitor (Pan) 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 Akt Inhibitor (Pan) 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 Akt Inhibitor (Pan) 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 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 predicted - sensitive Akt Inhibitor (Pan) 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 Akt Inhibitor (Pan) 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 Akt Inhibitor (Pan) 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 Akt Inhibitor (Pan) 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 K111N breast cancer sensitive Akt Inhibitor (Pan) 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 Akt Inhibitor (Pan) 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 PI3K Inhibitor (Pan) 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