Figure 1.

Regorafenib inhibits oncogenesis, angiogenesis, and the tumor microenvironment in metastatic colorectal cancer. Regorafenib is a multikinase inhibitor that targets several receptor tyrosine kinases (eg, fibroblast growth factor receptor [FGFR], platelet-derived growth factor receptor-β [PDGFR-β], vascular endothelial growth factor receptor [VEGFR], and tyrosine kinase with immunoglobulin and epidermal growth factor homology domain [TIE2]) that regulate angiogenesis and the tumor microenvironment in colorectal tumor cells. Regorafenib also inhibits oncogenesis, in part, by selectively targeting the intracellular kinases BRAF and RAF1, an activator of downstream mitogen-activated protein kinases (MEK and ERK) that promote cell proliferation.

Abbreviation: ANG-2, angiopoietin-2.