Regorafenib is a novel oral multi-targeted small molecule tyrosine kinase inhibitor with a novel spectrum of action, inhibiting VEGF receptor 1~3, platelet-derived growth factor (PDGF) receptor, fibroblast growth factor (FGF) receptor, RET, KIT, TIE and other multi-targeted pathways, exerting anti-tumor effects through three pathways (angiogenesis, tumor growth and tumor microenvironment). It exerts anti-tumor effects through three pathways (angiogenesis, tumor growth and tumor microenvironment). Preclinical studies have shown that regorafenib can inhibit a variety of kinases involved in angiogenesis (including lymphatic vessel formation), cell proliferation and tumor growth, and tumor microenvironment, mainly including VEGFR1~3 (angiogenesis), KIT, RET (tumor formation), PDGFR-β, and FGFR (tumor microenvironment); moreover, compared with other kinase inhibitors, regorafenib has a unique Regorafenib has a unique mechanism of action and kinome target profile compared to other kinase inhibitors. The results of the phase I study of regorafenib indicated that regorafenib 160 mg/d with 3 weeks of dosing and 1 week of discontinuation showed good clinical efficacy and tolerability in patients with advanced refractory tumors. Subsequently, several phase II clinical studies of regorafenib were conducted, and preliminary results showed clinical benefit of regorafenib in patients with hepatocellular carcinoma, gastrointestinal mesenchymal tumor, and colorectal cancer. Subsequently, a phase III clinical study of regorafenib in gastrointestinal mesenchymal tumors (the GRID study) confirmed a significant benefit of regorafenib in patients with advanced GIST that had progressed after prior imatinib and sunitinib therapy. Significant Phase III therapeutic clinical studies of regorafenib for mCRC include primarily the Global CORRECT Study and the Asian CONCUR Study. The global CORRECT study showed that regorafenib significantly prolonged OS in mCRC patients who failed standard therapy compared to best supportive care. results from the CONCUR study in Asian mCRC patients also showed a significant survival benefit from regorafenib. A randomized, double-blind, placebo-controlled phase III study of regorafenib in patients with stage IV colorectal cancer who have received curative therapy and a phase III clinical study of regorafenib versus placebo-controlled treatment with sorafenib for post-progressive hepatocellular o are currently progressing, and it is expected that these results will provide evidence to support regorafenib in the treatment of additional tumors.