binimetinib + RAF265

Binimetinib (MEK162, ARRY-438162) is a potent and selective oral small molecule inhibitor of mitogen-activated protein kinase kinase 1 and 2 (MEK1/2), key kinases in the RAS/RAF/MEK/ERK signaling pathway that regulates cell proliferation, differentiation, survival, and angiogenesis. Binimetinib is approved as Mektovi for certain cancers. RAF265 is an orally available small molecule kinase inhibitor with activity against mutant and wild-type Serine/threonine-protein kinase B-Raf (BRAF), Serine/threonine-protein kinase C-Raf (CRAF), and vascular endothelial growth factor receptor 2 (VEGFR2), providing both anti-tumor and antiangiogenic effects. The combination of binimetinib plus RAF265 has been studied in early-phase clinical trials for advanced solid tumors harboring RAS or BRAFV600E mutations[3][4][5][2]. Both drugs are designed to target aberrant MAPK pathway signaling commonly found in various cancers such as melanoma.

Brand names

Mektovi

Other names

binimetinib