Therapy Detail

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Therapy Name ARQ 751
Synonyms
Therapy Description

ARQ 751 is an inhibitor of AKT1, AKT2, and AKT3, which may result in inhibition of the AKT/PI3K/MTOR pathway, thereby leading to tumor growth inhibition (PMID: 26469692).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
ARQ 751 ARQ-751|ARQ751 Akt Inhibitor (Pan) 21 ARQ 751 is an inhibitor of AKT1, AKT2, and AKT3, which may result in inhibition of the AKT/PI3K/MTOR pathway, thereby leading to tumor growth inhibition (PMID: 26469692).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
PIK3CA H1047R breast cancer sensitive ARQ 751 Preclinical - Cell culture Actionable In a preclinical study, ARQ 751 treatment did not increase cell death but inhibited proliferation of breast cancer cells harboring PIK3CA H1047R in culture (PMID: 32439931). 32439931
PIK3CA H1047R breast cancer sensitive 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 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 E545K breast cancer sensitive ARQ 751 Preclinical - Cell culture Actionable In a preclinical study, ARQ 751 treatment inhibited Akt signaling, induced cell death, and inhibited proliferation of breast cancer cell lines harboring PIK3CA E545K in culture (PMID: 32439931). 32439931
PIK3CA E545K breast cancer sensitive 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 P449T colorectal cancer sensitive ARQ 751 Preclinical - Cell culture Actionable In a preclinical study, ARQ 751 treatment induced cell death and inhibited proliferation of a colorectal cancer cell line harboring PIK3CA P449T in culture (PMID: 32439931). 32439931
PIK3CA K111N breast cancer sensitive 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 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 E542K stomach cancer sensitive ARQ 751 Preclinical - Cell culture Actionable In a preclinical study, ARQ 751 treatment induced cell death and inhibited proliferation of a gastric cancer cell line harboring PIK3CA E542K in culture (PMID: 32439931). 32439931
PTEN L108R breast cancer sensitive ARQ 751 Preclinical - Cell culture Actionable In a preclinical study, ARQ 751 treatment increased cell death and inhibited proliferation of a breast cancer cell line harboring PTEN L108R in culture (PMID: 32439931). 32439931
PIK3CA C420R breast cancer sensitive ARQ 751 Preclinical - Cell culture Actionable In a preclinical study, ARQ 751 treatment induced cell death and inhibited proliferation of a breast cancer cell line harboring PIK3CA C420R in culture (PMID: 32439931). 32439931

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries
NCT02761694 Phase I ARQ 751 + Paclitaxel ARQ 751 ARQ 751 + Fulvestrant ARQ 751 as a Single Agent or in Combination With Other Anti-Cancer Agents, in Solid Tumors With PIK3CA / AKT / PTEN Mutations Terminated USA 0


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