BMS-908662

BMS-908662 (also known as XL281) is an orally active, small molecule inhibitor of RAF kinases, including wild-type and mutant forms of B-RAF and CRAF, within the RAS/RAF/MEK/ERK signaling pathway[1][9][8][3]. The drug was developed primarily as an antineoplastic agent, targeting cancers with aberrant RAF pathway activation, such as melanoma and colorectal cancer[1][7][8][6]. It showed selective potency for RAF kinases (IC50 for CRAF: 2.6 nM; B-RAF: 4.5 nM; B-RAFV600E: 6 nM)[9]. Development was led by Bristol Myers Squibb following in-licensing from Exelixis. Clinical trials included exploration as monotherapy and in combination with agents like cetuximab and ipilimumab for advanced melanoma and colorectal cancer. Although some clinical benefit and target inhibition were observed, development was discontinued[1][8].