Dabrafenib is a kinase inhibitor used to treat patients with specific types of melanoma, non-small cell lung cancer, and thyroid cancer. Dabrafenib mesylate (Tafinlar) is a reversible ATP-competitive kinase inhibitor and targets the MAPK pathway.
- Mechanism
- Curator reviewed · 8 references
Dabrafenib is a competitive and selective BRAF inhibitor by binding to its ATP pocket. Although dabrafenib can inhibit wild-type BRAF, it has a higher affinity for mutant forms of BRAF, including BRAF V600E, BRAF V600K, and BRAF V600D. BRAF is a serine/threonine protein kinase and is involved in activating the RAS/RAF/MEK/ERK or MAPK pathway, a pathway that is implicated in cell cycle progression, cell proliferation, and arresting apoptosis. Therefore, constitutive active mutation of BRAF such as BRAF V600E is frequently observed in many types of cancer, including melanoma, lung cancer, and colon cancer.
- Primary indication
- As monotherapy, dabrafenib is indicated to treat unresectable or metastatic melanoma with BRAF V600E mutation as detected by an FDA-approved test.Curator reviewed · 14 structured indications
- Formula / weight
- C23H20F3N5O2S2 · 519.562 g/mol (avg)
- First approval
- Canada, 2015 · United States, 2013 · European Union, 2021
- Code names
- DRB436 · GSK-2118436 · GSK-2118436A
- Brand names
Resolves to
BFSMGDJOXZAERB-UHFFFAOYSA-NSMILESCC(C)(C)C1=NC(=C(S1)C1=NC(N)=NC=C1)C1=C(F)C(NS(=O)(=O)C2=C(F)C=CC=C2F)=CC=C1What you can answer from here — as of September 23, 2026
Which drugs share a target with Dabrafenib, and which of those have an active Phase 3 trial?
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