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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- Use quotes to match on a longer phrase with spaces (i.e. "mtor c1483f")
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| 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 |
| 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 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 |
| 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 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 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 |
| 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 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 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 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 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 |
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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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