Abstract: Lacking of available treatments for metastatic colorectal cancer（mCRC） patients progressed with standard prior therapies， it has lead to the research into new active molecules. Regorafenib is an oral smallmolecule multi kinase inhibitor， targeting both tumor cell proliferation and vasculature， with potent inhibitory activity against vascular endothelial growth factor receptors， plateletderived growth factor receptor， fibroblast growth factor receptor 1， Raf， TIE-2， and the kinases KIT，RET， and BRAF. The antitumor activity of regorafenib has been confirmed in vitro and in vivo study. The results of several clinical trials reveal that the benefit of regorafenib on the overall survival of mCRC patients. In this paper， the progression of regorafenib on mCRC are summarized.