Therapy Detail

Therapy Name GDC0879
Synonym
Therapy Description

GDC0879 is a selective small molecular inhibitor of BRAF and CRAF (RAF1), which inhibits survival of tumor cells (PMID: 19276360).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
GDC0879 GDC-0879 BRAF Inhibitor 18 CRAF Inhibitor 10 GDC0879 is a selective small molecular inhibitor of BRAF and CRAF (RAF1), which inhibits survival of tumor cells (PMID: 19276360).
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
BRAF wild-type KRAS G12D pancreatic cancer resistant GDC0879 Preclinical - Cell line xenograft Actionable In a preclinical study, GDC0879 failed to inhibit growth of BRAF wild-type pancreatic cancer cells harboring KRAS G12D in cell line xenograft models (PMID: 19276360). 19276360
MAP2K1 F53L Advanced Solid Tumor resistant GDC0879 Preclinical - Cell culture Actionable In a preclinical study, Map2k1 F53L displayed resistance to the Braf inhibitor, GDC-0879, as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). 29753091
NRAS mutant colon cancer resistant GDC0879 Preclinical - Cell culture Actionable In a preclinical study, colon cancer cells harboring NRAS mutations were resistant to GDC0879 induced growth inhibition in culture (PMID: 19276360). 19276360
BRAF N581Y colon cancer resistant GDC0879 Preclinical - Cell culture Actionable In a preclinical study, colon cancer cells harboring BRAF N581Y were resistant to GDC0879 induced growth inhibition in culture (PMID: 19276360). 19276360
BRAF wild-type KRAS Q61K non-small cell lung carcinoma resistant GDC0879 Preclinical - Cell line xenograft Actionable In a preclinical study, GDC0879 failed to inhibit growth of BRAF wild-type non-small cell lung cancer cells harboring KRAS Q61K in culture and in cell line xenograft models (PMID: 19276360). 19276360
MAP2K1 Q56P Advanced Solid Tumor resistant GDC0879 Preclinical - Cell culture Actionable In a preclinical study, Map2k1 Q56P displayed resistance to the Braf inhibitor, GDC-0879, as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). 29753091
MAP2K1 K57N Advanced Solid Tumor resistant GDC0879 Preclinical - Cell culture Actionable In a preclinical study, Map2k1 K57N displayed resistance to the Braf inhibitor, GDC-0879, as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). 29753091
BRAF wild-type KRAS G12C non-small cell lung carcinoma resistant GDC0879 Preclinical - Pdx Actionable In a preclinical study, GDC0879 failed to inhibit growth of BRAF wild-type non-small cell lung cancer cells harboring KRAS G12C in patient-derived xenograft models (PMID: 19276360). 19276360
MAP2K1 C121S Advanced Solid Tumor resistant GDC0879 Preclinical - Cell culture Actionable In a preclinical study, Map2k1 C121S displayed resistance to the Braf inhibitor, GDC-0879, as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). 29753091
KRAS mutant non-small cell lung carcinoma resistant GDC0879 Preclinical - Cell culture Actionable In a preclinical study, non-small cell lung cancer cells harboring KRAS mutations were resistant to GDC0879 induced growth inhibition in culture (PMID: 19276360). 19276360
BRAF wild-type melanoma resistant GDC0879 Preclinical - Pdx & cell culture Actionable In a preclinical study, GDC0879 failed to inhibit growth of BRAF wild-type melanoma cells in cell culture, cell line xenograft models, and patient-derived xenograft models (PMID: 19276360). 19276360
BRAF wild-type KRAS G13D colon cancer resistant GDC0879 Preclinical - Cell line xenograft Actionable In a preclinical study, GDC0879 failed to inhibit growth of BRAF wild-type colon cancer cells harboring KRAS G13D in culture ann in cell line xenograft models (PMID: 19276360). 19276360
BRAF wild-type NRAS Q61K melanoma resistant GDC0879 Preclinical - Pdx Actionable In a preclinical study, GDC0879 failed to inhibit growth of BRAF wild-type melanoma cells harboring NRAS Q61K in patient-derived xenograft models (PMID: 19276360). 19276360
BRAF wild-type KRAS G12V non-small cell lung carcinoma resistant GDC0879 Preclinical - Pdx Actionable In a preclinical study, GDC0879 failed to inhibit growth of BRAF wild-type non-small cell lung cancer cells harboring KRAS G12V in patient-derived xenograft models (PMID: 19276360). 19276360
BRAF V600E melanoma sensitive GDC0879 Preclinical - Pdx & cell culture Actionable In a preclinical study, GDC0879 inhibited survival of melanoma cell lines harboring BRAF V600E in cell culture, cell line xenograft and patient-derived xenograft (PDX) models (PMID: 19276360). 19276360
MAP2K1 I111S Advanced Solid Tumor resistant GDC0879 Preclinical - Cell culture Actionable In a preclinical study, Map2k1 I111S displayed resistance to the Braf inhibitor, GDC-0879, as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). 29753091
MAP2K1 V211D Advanced Solid Tumor resistant GDC0879 Preclinical - Cell culture Actionable In a preclinical study, Map2k1 V211D displayed resistance to the Braf inhibitor, GDC-0879, as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). 29753091
BRAF V600E colon cancer sensitive GDC0879 Preclinical - Cell line xenograft Actionable In a preclinical study, GDC0879 inhibited survival of colon cancer cell lines harboring BRAF V600E in cell culture and cell line xenograft models (PMID: 19276360). 19276360
KRAS mutant colon cancer resistant GDC0879 Preclinical - Cell culture Actionable In a preclinical study, colon cancer cells harboring KRAS mutations were resistant to GDC0879 induced growth inhibition in culture (PMID: 19276360). 19276360
BRAF wild-type non-small cell lung carcinoma resistant GDC0879 Preclinical - Pdx & cell culture Actionable In a preclinical study, GDC0879 failed to inhibit growth of BRAF wild-type non-small cell lung cancer cells in culture and in patient-derived xenograft models (PMID: 19276360). 19276360
MAP2K1 F129L Advanced Solid Tumor resistant GDC0879 Preclinical - Cell culture Actionable In a preclinical study, Map2k1 F129L displayed resistance to the Braf inhibitor, GDC-0879, as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). 29753091
BRAF L485Y non-small cell lung carcinoma resistant GDC0879 Preclinical - Cell culture Actionable In a preclinical study, non-small cell lung cancer cells harboring BRAF L485Y were resistant to GDC0879 induced growth inhibition in culture (PMID: 19276360). 19276360
Clinical Trial Phase Therapies Title Recruitment Status