Regorafenib, a novel multi- kinase inhibitor, has been approved for the treatment of metastatic colorectal cancer and gastrointestinal stromal tumors. The clinical trials of Regorafenib for the treatment of hepatocellular carcinoma ( HCC) are summarized. Phase Ⅰ and Ⅱ clinical trials have demonstrated the safety of Regorafenib in patients with HCC. A phase Ⅱ clinical trial has shown that as a second-line therapy for HCC, Regorafenib can achieve a relatively high disease control rate. In addition, an ongoing phase Ⅲ randomized, controlled trial will compare the safety and efficacy between Regorafenib and placebo as second- line therapies for advanced HCC. These results indicate that Regorafenib can effectively control the progression of HCC and may be used as a second- line therapy for advanced HCC.
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