Regorafenib is an orally-bioavailable multi-kinase inhibitor that is structurally related to sorafenib (BAY 43-9006; ), another multi-kinase inhibitor with applications in cancer. Regorafenib inhibits c-Raf, B-Raf, VEGFR1, VEGFR2, VEGFR3, Tie2, PDGFRβ, FGFR1, c-Kit, and RET with IC50 values of 2.5, 28, 13, 4.2, 46, 311, 22, 202, 7, and 1.5 nM, respectively, as well as other kinases. It also inhibits soluble epoxide hydrolase (IC50 = 0.5 nM). Regorafenib has value against a range of cancers, including advanced colorectal cancer.
