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Therapy Name | GDC-0077 |
Synonyms | |
Therapy Description |
GDC-0077 inhibits PIK3CA, with selectivity for mutant PIK3CA over wild-type PIK3CA, potentially resulting in increased apoptosis and decreased growth of PIK3CA-mutant tumors (AACR; Cancer Res 2017;77(13 Suppl):Abstract nr 156). |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
GDC-0077 | RO7113755|RG6114|GDC0077|GDC 0077 | PIK3CA inhibitor 16 | GDC-0077 inhibits PIK3CA, with selectivity for mutant PIK3CA over wild-type PIK3CA, potentially resulting in increased apoptosis and decreased growth of PIK3CA-mutant tumors (AACR; Cancer Res 2017;77(13 Suppl):Abstract nr 156). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
PIK3CA E726K PIK3CA H1047R | breast cancer | sensitive | GDC-0077 | Preclinical - Cell culture | Actionable | In a preclinical study, breast epithelial cells expressing PIK3CA E726K and PIK3CA H1047R in cis demonstrated increased sensitivity to growth inhibition by GDC-0077 treatment compared to cells expressing individual PIK3CA mutations in culture (PMID: 31699932). | 31699932 |
PIK3CA E545K PIK3CA E726K | breast cancer | sensitive | GDC-0077 | Preclinical - Cell culture | Actionable | In a preclinical study, breast epithelial cells expressing PIK3CA E545K and PIK3CA E726K in cis demonstrated increased sensitivity to growth inhibition by GDC-0077 treatment compared to cells expressing individual PIK3CA mutations in culture (PMID: 31699932). | 31699932 |
PIK3CA mutant | breast cancer | predicted - sensitive | GDC-0077 | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, GDC-0077 inhibited proliferation and induced apoptosis in PIK3CA-mutant breast cancer cell lines in culture, and induced apoptosis and tumor regression in PIK3CA-mutant breast cancer cell line and patient-derived xenograft models (AACR; Cancer Res 2017;77(13 Suppl):Abstract nr 156). | detail... |
PIK3CA E545K PIK3CA M1043L | breast cancer | sensitive | GDC-0077 | Preclinical - Cell culture | Actionable | In a preclinical study, breast epithelial cells expressing PIK3CA E545K and PIK3CA M1043L in cis demonstrated increased sensitivity to growth inhibition by GDC-0077 treatment compared to cells expressing individual PIK3CA mutations in culture (PMID: 31699932). | 31699932 |
PIK3CA E453Q PIK3CA H1047R | breast cancer | sensitive | GDC-0077 | Preclinical - Cell culture | Actionable | In a preclinical study, breast epithelial cells expressing PIK3CA E453Q and PIK3CA H1047R in cis demonstrated increased sensitivity to growth inhibition by GDC-0077 treatment compared to cells expressing individual PIK3CA mutations in culture (PMID: 31699932). | 31699932 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
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NCT03006172 | Phase I | GDC-0077 + Letrozole + Palbociclib GDC-0077 Fulvestrant + GDC-0077 GDC-0077 + Letrozole | To Evaluate the Safety, Tolerability, and Pharmacokinetics of GDC-0077 Single Agent in Participants With Solid Tumors and in Combination With Endocrine and Targeted Therapies in Participants With Breast Cancer | Recruiting | USA | CAN | 3 |
NCT04632992 | Phase II | Ipatasertib Atezolizumab + Capecitabine Entrectinib Atezolizumab + Docetaxel Ado-trastuzumab emtansine + Atezolizumab Capecitabine + Pertuzumab/trastuzumab/hyaluronidase-zzxf Paclitaxel + Pertuzumab/trastuzumab/hyaluronidase-zzxf Alectinib GDC-0077 Pertuzumab/trastuzumab/hyaluronidase-zzxf Docetaxel + Pertuzumab/trastuzumab/hyaluronidase-zzxf Atezolizumab + Paclitaxel Ado-trastuzumab emtansine + Tucatinib | A Study Evaluating Targeted Therapies in Participants Who Have Advanced Solid Tumors With Genomic Alterations or Protein Expression Patterns Predictive of Response (MyTACTIC) | Recruiting | USA | 0 |