Therapy Detail

Therapy Name Dabrafenib + SCH772984 + Trametinib
Synonym
Therapy Description

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Dabrafenib Tafinlar GSK2118436 BRAF Inhibitor 18 Tafinlar (dabrafenib) inhibits the activity of BRAF, including V600E, which results in inhibition of tumor cell proliferation (PMID: 22735384). Tafinlar (dabrafenib) is FDA approved for BRAF V600E positive unresectable or metastatic melanoma, and in combination with Mekinist (trametinib) for BRAF V600E/K-mutant melanoma, BRAF V600E-mutant non-small cell lung cancer, and BRAF V600E-mutant anaplastic thyroid cancer (FDA.gov).
SCH772984 SCH984 ERK Inhibitor (pan) 14 SCH772984 is an ATP-competitive inhibitor of both ERK1 and ERK2, which may result in growth inhibition and tumor regression (PMID: 23614898).
Trametinib Mekinist GSK1120212 MEK inhibitor (Pan) 20 MEK1 Inhibitor 20 MEK2 Inhibitor 18 Mekinist (trametinib) inhibits MEK 1 and 2, which potentially leads to reduced tumor cell proliferation (PMID: 27956260). Mekinist (trametinib) is FDA approved for melanoma patients harboring BRAF V600E or BRAF V600K mutations, and in combination with Tafinlar (dabrafinib) for BRAF V600E/K-mutant melanoma, BRAF V600E- mutant non-small cell lung cancer, and BRAF V600E-mutant anaplastic thyroid cancer (FDA.gov).
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
BRAF V600E melanoma decreased response Dabrafenib + SCH772984 + Trametinib Preclinical - Cell culture Actionable In a preclinical study, combination of Tafinlar (dabrafenib), SCH772984, and Mekinist (trametinib) resulted in durable inhibition of Erk signaling and proliferation of melanoma cells overexpressing BRAF V600E in culture (PMID: 28714990). 28714990
BRAF amp BRAF V600E lung adenocarcinoma sensitive Dabrafenib + SCH772984 + Trametinib Preclinical - Pdx Actionable In a preclinical study, combination of Tafinlar (dabrafenib), SCH772984, and Mekinist (trametinib) resulted in durable tumor inhibition in cell line xenograft models of BRAF V600E mutated lung adenocarcinoma cells that acquired resistance to Erk inhibitors through BRAF amplification (PMID: 28714990). 28714990
Clinical Trial Phase Therapies Title Recruitment Status