Description
Dabrafenib is a reversible kinase inhibitor with anticancer chemotherapeutic activity. This compound is selective primarily for mutant (V600E) B-Raf, but has also inhibited tumor growth in cells expressing other B-Raf mutants (V600K, V600D) and WT B-Raf. Dabrafenib is partially active against c-Raf as well. Dabrafenib is an ATP-competitive inhibitor that has been approved for clinical use in the treatment of unresectable or metastatic melanomas; it is also being examined for treatment of brain metastases and other cancers. This compound has a very high oral bioavailability.
References
Ballantyne AD, Garnock-Jones KP. Dabrafenib: First Global Approval. Drugs. 2013 Jul 24. [Epub ahead of print] PMID: 23881668.
Huang T, Karsy M, Zhuge J, et al. B-Raf and the inhibitors: from bench to bedside. J Hematol Oncol. 2013 Apr 25;6:30. PMID: 23617957.
Klinac D, Gray ES, Millward M, et al. Advances in personalized targeted treatment of metastatic melanoma and non-invasive tumor monitoring. Front Oncol. 2013;3:54. PMID: 23515890.
Hauschild A, Grob JJ, Demidov LV, et al. Dabrafenib in BRAF-mutated metastatic melanoma: a multicentre, open-label, phase 3 randomised controlled trial. Lancet. 2012 Jul 28;380(9839):358-65. PMID: 22735384.
