Dabrafenib

Dabrafenib is a selective inhibitor of mutant B-RafV600E (IC50 = 0.8 nM), with 4- and 6-fold reduced potency against wild type B-Raf and c-Raf (IC50s = 3.2 and 5 nM, respectively). It has been investigated in clinical trials in patients with B-RafV600E metastatic melanoma and other solid tumors and is often combined with the MEK inhibitor trametinib (Cay-16292) to circumvent the development of B-Raf inhibitor resistance.