Abstract: Hepatocellular carcinoma (HCC) is one of the most common malignant neoplasms worldwide, and remains a formidable challenge for clinical therapy. The skin of Bufo bufo gargarizans Cantor has been reported to have antipyretic, detoxicant, diuresis, stasis-eliminative, and pus-discharging properties. Cinobufacini (Huachansu), an aqueous extract of dried skin of B. bufo gargarizans Cantor, is a traditional Chinese medicinal preparation widely used in clinical cancer therapy in China. In recent years, attentions have been paid to cinobufacini for the treatment of HCC. These clinical data have demonstrated that cinobufacini is effective against HCC through intravenous drip, drug combination, or other methods. Moreover, cinobufacini is a promising candidate for the treatment of hepatitis B or hepatic fibrosis to prevent the development of HCC. The present review focuses on clinical researches about cinobufacini for prevention and treatment of HCC in recent years.