BAY-73-4506 (Regorafenib) is an orally active and highly potent inhibitor against multiple tyrosine kinases, including VEGFR1/2/3, PDGFR?, Kit, RET and Raf-1. Regorafenib inhibits the proliferation of HUVEC cells stimulated with VEGF, and inhibits FGFR signaling in breast cancer MCF-7 cells stimulated with FGF. Regorafenib is anti-angiogenic due to its inhibitions against VEGFR2-TIE2 tyrosine kinase. [1]
Co-administration of Regorafenib and a PI3K/Akt inhibitor (MK-2206) clearly demonstrated synergistic effect in a HCT116 xenocraft mouse model [2]. Regorafenib is currently being studied as a potential treatment option in multiple tumor types, and has recently be approved in treating patients with Metastatic Colorectal cancer. [3]