Therapy Detail

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Therapy Name Dabrafenib + Regorafenib + Trametinib
Synonyms
Therapy Description

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Dabrafenib Tafinlar GSK2118436 BRAF Inhibitor 25 Tafinlar (dabrafenib) inhibits the activity of BRAF, including V600E, which results in the inhibition of tumor cell proliferation (PMID: 22735384). Tafinlar (dabrafenib) is FDA approved for BRAF V600E/K- 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, BRAF V600E-mutant anaplastic thyroid cancer, for adult and pediatric patients of 6 years or older with unresectable or metastatic solid tumors harboring BRAF V600E, and for pediatric patients of 1 year or older with low-grade glioma harboring BRAF V600E (FDA.gov).
Regorafenib Stivarga BAY 73-4506 BRAF Inhibitor 25 CRAF Inhibitor 12 KIT Inhibitor 57 PDGFR Inhibitor (Pan) 30 RET Inhibitor 52 VEGFR Inhibitor (Pan) 36 VEGFR2 Inhibitor 37 Stivarga (regorafenib) is an inhibitor of several kinases including VEGFR, RET, KIT, PDGFR and RAF, thereby inhibiting tumor angiogenesis and tumor cell proliferation (PMID: 24756792). Stivarga (regorafenib) is FDA approved for colorectal cancer, hepatocellular carcinoma, and GIST (FDA.gov).
Trametinib Mekinist GSK1120212 MEK inhibitor (Pan) 24 MEK1 Inhibitor 26 MEK2 Inhibitor 24 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 (dabrafenib) for BRAF V600E/K-mutant melanoma, BRAF V600E- mutant non-small cell lung cancer, BRAF V600E-mutant anaplastic thyroid cancer, for adult and pediatric patients of 6 years or older with unresectable or metastatic solid tumors harboring BRAF V600E, and for pediatric patients of 1 year or older with low-grade glioma harboring BRAF V600E (FDA.gov).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
BRAF V600E colorectal cancer sensitive Dabrafenib + Regorafenib + Trametinib Preclinical - Cell line xenograft Actionable In a preclinical study, combination treatment with Stivarga (regorafenib), Tafinlar (dabrafenib), and Mekinist (trametinib) in colorectal cancer cell lines harboring BRAF V600E resulted in suppression of colony formation in culture, and inhibition of tumor growth in a cell line xenograft model (PMID: 33568355). 33568355
BRAF V600E melanoma sensitive Dabrafenib + Regorafenib + Trametinib Preclinical - Pdx & cell culture Actionable In a preclinical study, combination treatment with Stivarga (regorafenib), Tafinlar (dabrafenib), and Mekinist (trametinib) in a melanoma cell line harboring BRAF V600E resulted in suppression of colony formation in culture, and suppressed tumor growth in patient-derived xenograft (PDX) models (PMID: 33568355). 33568355
BRAF V600E colon adenocarcinoma predicted - sensitive Dabrafenib + Regorafenib + Trametinib Case Reports/Case Series Actionable In a clinical case study, combination treatment with Stivarga (regorafenib), Tafinlar (dabrafenib), and Mekinist (trametinib) in a patient with colon adenocarcinoma harboring BRAF V600E led to stable disease, and treatment continued for eight months, at which time some disease progression was observed (PMID: 33568355). 33568355

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries


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