Therapy Detail

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Therapy Name Miransertib
Synonyms
Therapy Description

Miransertib (ARQ092) is a pan-AKT inhibitor, resulting in inhibition of the PI3K/AKT signaling pathway and cell proliferation (PMID: 26469692, PMID: 31058421).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Miransertib ARQ-092|ARQ092|ARQ 092 Akt Inhibitor (Pan) 21 Miransertib (ARQ092) is a pan-AKT inhibitor, resulting in inhibition of the PI3K/AKT signaling pathway and cell proliferation (PMID: 26469692, PMID: 31058421).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
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 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 R93W PIK3CA D350G PTEN R130G endometrial cancer sensitive Miransertib Preclinical - Pdx Actionable In a preclinical study, a patient-derived xenograft (PDX) model of endometrial cancer harboring PIK3CA D350G, PIK3CA R93W, and PTEN R130G was sensitive to Miransertib (ARQ092), demonstrating greater than 90% inhibition of tumor growth (PMID: 26469692). 26469692
PIK3CA E542K breast cancer sensitive Miransertib Preclinical - Cell culture Actionable In a preclinical study, a hormone breast cancer cell line harboring PIK3CA E542K was sensitive to Miransertib (ARQ092) in culture, demonstrating inhibition of cell growth (PMID: 26469692). 26469692
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 E545K PIK3CA Q859H breast cancer sensitive Miransertib Preclinical - Cell culture Actionable In a preclinical study, Miransertib (ARQ092) decreased viability of a breast cancer cell line harboring PIK3CA E545K and expressing PIK3CA Q859H in culture (PMID: 37916958). 37916958
TSC1 M271T TSC2 L604P endometrial cancer sensitive Miransertib Preclinical - Pdx Actionable In a preclinical study, a patient-derived xenograft (PDX) model of endometrial cancer harboring TSC1 M271T and TSC2 L604P was sensitive to Miransertib (ARQ092), demonstrating greater than 90% inhibition of tumor growth (PMID: 26469692). 26469692
PIK3CA E545K PIK3CA I817F breast cancer sensitive Miransertib Preclinical - Cell culture Actionable In a preclinical study, Miransertib (ARQ092) decreased viability of a breast cancer cell line harboring PIK3CA E545K and expressing PIK3CA I817F 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 H1047R breast cancer sensitive Miransertib Preclinical - Cell culture Actionable In a preclinical study, Miransertib (ARQ092) 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 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 E545K breast cancer sensitive 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 breast cancer sensitive Miransertib Preclinical - Cell culture Actionable In a preclinical study, Miransertib (ARQ092) treatment inhibited Akt signaling, induced cell death, and inhibited proliferation of breast cancer cell lines harboring PIK3CA E545K in culture (PMID: 32439931). 32439931
PIK3CA P449T colorectal cancer sensitive Miransertib Preclinical - Cell culture Actionable In a preclinical study, Miransertib (ARQ092) treatment induced cell death and inhibited proliferation of a colorectal cancer cell line harboring PIK3CA P449T in culture (PMID: 32439931). 32439931
PIK3CA C420R breast cancer sensitive 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 C420R in culture (PMID: 32439931). 32439931
PIK3CA K111N breast cancer sensitive 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 sensitive 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 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
PTEN E235* TSC2 G440S endometrial cancer sensitive Miransertib Preclinical - Pdx Actionable In a preclinical study, a patient-derived xenograft (PDX) model of endometrial cancer harboring PTEN E235* and TSC2 G440S was sensitive to Miransertib (ARQ092), demonstrating greater than 90% inhibition of tumor growth (PMID: 26469692). 26469692
PIK3CA E542K stomach cancer sensitive Miransertib Preclinical - Cell culture Actionable In a preclinical study, Miransertib (ARQ092) treatment induced cell death and inhibited proliferation of a gastric cancer cell line harboring PIK3CA E542K in culture (PMID: 32439931). 32439931
PIK3CA E545K PIK3CA W780R breast cancer sensitive Miransertib Preclinical - Cell culture Actionable In a preclinical study, Miransertib (ARQ092) decreased viability of a breast cancer cell line harboring PIK3CA E545K and expressing PIK3CA W780R in culture (PMID: 37916958). 37916958
PTEN L108R breast cancer sensitive Miransertib Preclinical - Cell culture Actionable In a preclinical study, Miransertib (ARQ092) inhibited proliferation of a breast cancer cell line harboring PTEN L108R in culture (PMID: 30858154). 30858154
PTEN L108R breast cancer sensitive Miransertib Preclinical - Cell culture Actionable In a preclinical study, Miransertib (ARQ092) treatment increased cell death and inhibited proliferation of a breast cancer cell line harboring PTEN L108R in culture (PMID: 32439931). 32439931

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries
NCT01473095 Phase I Miransertib Phase 1 Dose Escalation Study of ARQ 092 in Adult Subjects With Advanced Solid Tumors and Recurrent Malignant Lymphoma Completed USA 0
NCT02476955 Phase I Miransertib Carboplatin + Paclitaxel Open-label Phase 1b Study of ARQ 092 in Combination With Carboplatin Plus Paclitaxel Terminated USA 0


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