ABSTRACT
As the first-line drug for the treatment of primary liver cancer, sorafenib has been widely used in clinical practice, but its drug resistance and toxic and side effects have become increasingly apparent, along with limited efficacy. In recent years, the research on regorafenib for the treatment of hepatocellular carcinoma (HCC) has gradually become a hotspot. The RESORCE trial has shown that regorafenib can significantly extend the overall survival time of patients with failed sorafenib treatment to 10.6 months, and regorafenib was approved as a second-line drug for advanced HCC by Food and Drug Administration in 2017. This article reviews the molecular mechanism, efficacy evaluation, combination therapy, and criteria for patient selection in the treatment of HCC with regorafenib, so as to provide a direction for further research in the future.