Missing content? – Request curation!
Request curation for specific Genes, variants, or PubMed publications.
Have questions, comments or suggestions? - Let us know!
Email us at : ckbsupport@jax.org
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) 39 | 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 |
---|---|---|---|---|---|---|---|
PIK3CA R38C PTEN loss | endometrial cancer | sensitive | CH5132799 | Preclinical | Actionable | In a preclinical study, CH5132799 inhibited proliferation of an endometrial cancer cell line harboring PIK3CA R38C and PTEN loss in culture (PMID: 21558396). | 21558396 |
PTEN del | stomach cancer | sensitive | CH5132799 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, CH5132799 induced tumor regression in xenograft models of a human stomach cancer cell line with deletion of PTEN (PMID: 21558396). | 21558396 |
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 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 |
PTEN del | prostate cancer | sensitive | CH5132799 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, CH5132799 inhibited tumor growth in xenograft models of a human prostate cancer cell line with deletion of PTEN (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 |
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 |
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 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 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 |
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 |
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 |
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 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
---|