Therapy Detail

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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).

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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).

Filtering

  • Case insensitive filtering will display rows where any text in any cell matches the filter term
  • Simple literal full or partial string matches
  • Separate multiple filter terms with a spaces, order doesn't matter (a b c and c b a are equivalent )
  • Filtering will only apply to rows that are already loaded on the page, filtering has no impact on query parameters
  • Use quotes to match a longer phrase which contains spaces "mtor c1483f"

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
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 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 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 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 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 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 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 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 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 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 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
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 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

Filtering

  • Case insensitive filtering will display rows where any text in any cell matches the filter term
  • Simple literal full or partial string matches
  • Separate multiple filter terms with a spaces, order doesn't matter (a b c and c b a are equivalent )
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  • Use quotes to match a longer phrase which contains spaces "mtor c1483f"

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  • Generally, the default sort order for tables is set to be first column ascending, however, specific tables may set a different default sort order.
  • Click on any column header arrows to sort by that column
  • Hold down the Shift key and click multiple columns to sort by more than one column, be sure to set ascending or descending order for a given column, before moving on to the next column.

Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries


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