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Therapy Name | CH5132799 |
Synonyms | |
Therapy Description |
CH5132799 inhibits class I PI3Ks, including the PIKC3A mutants E542K, E545K, and H1047R, resulting in decreased PI3K pathway signaling and decreased tumor growth (PMID: 21558396). |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
CH5132799 | MEN1611|CH 5132799|CH-5132799|PA 799|PA799 | PI3K Inhibitor (Pan) 38 | MEN1611 (CH5132799) inhibits class I PI3Ks, including the PIKC3A mutants E542K, E545K, and H1047R, resulting in decreased PI3K pathway signaling and decreased tumor growth (PMID: 21558396). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
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ERBB2 amp | breast cancer | sensitive | CH5132799 | Preclinical | Actionable | In a preclinical study, CH5132799 inhibited proliferation of breast cancer cells with ERBB2 (HER2) amplification in culture (PMID: 21558396). | 21558396 |
PIK3CA H1047Y | endometrial cancer | sensitive | CH5132799 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, CH5132799 inhibited cell growth in a human endometrial cancer cell line harboring a PIK3CA H1047Y mutation, and inhibited tumor growth in xenograft models (PMID: 21558396). | 21558396 |
PIK3CA mutant | breast cancer | sensitive | CH5132799 | Preclinical | Actionable | In a preclinical study, breast cancer cells with PIK3CA mutations, both with and without ERBB2 (HER2) amplification, demonstrated sensitivity to CH5132799 in culture (PMID: 21558396). | 21558396 |
PIK3CA Q546R | prostate cancer | sensitive | CH5132799 | Preclinical | Actionable | In a preclinical study, CH5132799 inhibited proliferation of prostate cancer cells harboring PIK3CA Q546R in culture (PMID: 21558396). | 21558396 |
PIK3CA E542K | breast cancer | sensitive | CH5132799 | Preclinical | Actionable | In a preclinical study, CH5132799 inhibited proliferation of a breast cancer cell line harboring PIK3CA E542K in culture (PMID: 21558396). | 21558396 |
PIK3CA mutant | endometrial cancer | sensitive | CH5132799 | Preclinical | Actionable | In a preclinical study, CH5132799 inhibited proliferation of endometrial cancer cells with PIK3CA mutations in culture (PMID: 21558396). | 21558396 |
Unknown unknown | Advanced Solid Tumor | not applicable | CH5132799 | Phase I | Actionable | In a Phase I trial, CH5132799 demonstrated safety and preliminary efficacy in patients with advanced solid tumors (PMID: 25231405). | 25231405 |
PIK3CA mutant | ovarian cancer | sensitive | CH5132799 | Preclinical | Actionable | In a preclinical study, CH5132799 inhibited proliferation of ovarian cancer cells with PIK3CA mutations in culture (PMID: 21558396). | 21558396 |
PIK3CA mutant | prostate cancer | sensitive | CH5132799 | Preclinical | Actionable | In a preclinical study, CH5132799 inhibited proliferation of prostate cancer cells with PIK3CA mutations in culture (PMID: 21558396). | 21558396 |
ERBB2 amp PIK3CA K111N | breast cancer | sensitive | CH5132799 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, CH5132799 inhibited cell growth and Akt phosphorylation, and promoted apoptosis in a human breast cancer cell line harboring PIK3CA K111N and ERBB2 (HER2) amplification, and inhibited tumor growth in xenograft models (PMID: 21558396). | 21558396 |
PIK3CA H1047R | ovarian cancer | sensitive | CH5132799 | Phase I | Actionable | In a Phase I trial, CH5132799 demonstrated safety and preliminary efficacy in patients with advanced solid tumors, including a partial response in a patient with ovarian cancer harboring PIK3CA H1047R (PMID: 25231405). | 25231405 |
PIK3CA H1047R | breast cancer | sensitive | CH5132799 | Preclinical | Actionable | In a preclinical study, CH5132799 inhibited proliferation of breast cancer cells harboring PIK3CA H1047R in culture (PMID: 21558396). | 21558396 |
ERBB2 amp PIK3CA C420R | breast cancer | sensitive | CH5132799 | Preclinical | Actionable | In a preclinical study, CH5132799 inhibited proliferation of a breast cancer cell line harboring PIK3CA C420R and ERBB2 (HER2) amplification (PMID: 21558396). | 21558396 |
PIK3CA E545K | breast cancer | sensitive | CH5132799 | Preclinical | Actionable | In a preclinical study, CH5132799 inhibited proliferation of breast cancer cells expressing PIK3CA E545K (PMID: 21558396). | 21558396 |
ERBB2 amp PIK3CA E545K | breast cancer | sensitive | CH5132799 | Preclinical | Actionable | In a preclinical study, CH5132799 inhibited proliferation of a breast cancer cell line harboring PIK3CA E545K and ERBB2 (HER2) amplification in culture (PMID: 21558396). | 21558396 |
ERBB2 amp PIK3CA N345K | breast cancer | sensitive | CH5132799 | Preclinical | Actionable | In a preclinical study, CH5132799 inhibited proliferation of a breast cancer cell line harboring PIK3CA N345K and ERBB2 (HER2) amplification in culture (PMID: 21558396). | 21558396 |
ERBB2 amp PIK3CA H1047R | ovarian cancer | sensitive | CH5132799 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, CH5132799 inhibited cell growth in a human ovarian cancer cell line harboring PIK3CA H1047R and ERBB2 (HER2) amplification, and inhibited tumor growth in xenograft models (PMID: 21558396). | 21558396 |
PIK3CA E545K | ovarian cancer | sensitive | CH5132799 | Preclinical | Actionable | In a preclinical study, CH5132799 inhibited proliferation of ovarian cancer cells harboring PIK3CA E545K in culture (PMID: 21558396). | 21558396 |
ERBB2 amp PIK3CA H1047R | breast cancer | sensitive | CH5132799 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, CH5132799 inhibited cell growth and Akt phosphorylation, and promoted apoptosis in a human breast cancer cell line harboring PIK3CA H1047R and ERBB2 (HER2) amplification, and inhibited tumor growth in xenograft models (PMID: 21558396). | 21558396 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
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