Preclinical comparison of regorafenib and sorafenib efficacy for hepatocellular carcinoma using multimodality molecular imaging.

Sorafenib has been used as a clinical targeted therapy for hepatocellular carcinoma (HCC) for more than a decade. In 2017, regorafenib was approved for HCC treatment and has since been reported to prolong the survival of advanced HCC patients after treatment failure with sorafenib. However, there has been no direct systematic comparison of the therapeutic effects of regorafenib and sorafenib against HCC. In this study, we comprehensively compared the therapeutic effects of sorafenib and regorafenib against HCC in vitro and in vivo using multimodality molecular imaging, which can show molecular and cellular differences at early stages. The side effects of sorafenib and regorafenib were also systematically evaluated. The data showed that compared with sorafenib treatment, regorafenib exerted stronger antitumor and antiangiogenic effects and significantly increased the survival rate of HCC mice. Sorafenib but not regorafenib treatment caused body weight loss and liver and kidney dysfunction, while regorafenib but not sorafenib treatment caused hypertension. Our study may provide an experimental basis for the guidance of clinical HCC targeted treatment with regorafenib and sorafenib.