Apatinib is effective for treatment of advanced hepatocellular carcinoma

Abstract

As treatment options for hepatocellular carcinoma (HCC) are currently limited, we evaluated the efficacy and safety of oral apatinib, a VEGFR-2 inhibitor, on patients with advanced HCC. Twenty-two patients from Tianjin Medical University Cancer Institute and Hospital were enrolled for evaluation. Apatinib was administered at 500 mg/day or 250 mg/day continuously. Clinical endpoints were time to disease progression (TTP), overall survival (OS), and safety. The median TTP of treated patients was 10.4 months (95% CI 3.4 -17.5). At the last follow-up, 50% patients had survived longer than 11.4 months from the first dose. Complete response (CR), partial response (PR), stable disease (SD), and progressive disease (PD) rates were 0%, 40.9%, 40.9%, and 18.2%, respectively. The most common apatinib-related adverse events were hand-foot skin reaction (HFSR) (81.8%) and diarrhea (77.3%). Hypertension (27.3%) and HFSR (13.6%) were the most frequent grade 3/4 adverse events. In summary, results of this small study indicate that apatinib is well tolerated and extremely effective for the treatment of advanced HCC. It is therefore imperative to design and carry out well-controlled clinical trials to confirm its efficacy.

Efficacy and safety of sorafenib versus apatinib in the treatment of intermediate and advanced hepatocellular carcinoma: a comparative retrospective study

“…Though the tested and recommended dose of apatinib is 750–850 mg/day, there are retrospective studies and case reports that have demonstrated significant efficacy and safety at a lower dose of 250–500 mg/day. 29 , 36 However, further well-controlled studies are required to validate the benefit of altered dosing in HCC patients. Our study strengths included 1) no loss of patients at follow-up, and 2) being the first reported study from China comparing the effectiveness of these two antiangiogenic drugs in patients with intermediate or advanced HCC.…”

Novel ADAM-17 inhibitor ZLDI-8 enhances the in vitro and in vivo chemotherapeutic effects of Sorafenib on hepatocellular carcinoma cells

“…Sorafenib is the first approved front-line anti-tumor agents for advanced HCC 11 , 12 , 52 . Recently, some other molecular target agents, e.g., Regorafenib or apatinib, were also approved for advanced HCC treatment 53 , 54 . Although these molecular targeted agents bring new hope for patients with advanced HCC, the efficacy of these agents is still far from satisfying.…”

Autophagy: A Potential Therapeutic Target of Polyphenols in Hepatocellular Carcinoma

“…Apatinib, a small molecule kinase inhibitor, is considered as a better alternative for patients who were resistant to sorafenib treatment. A study conducted with a limited number of subjects (22 patients with HCC) showed that apatinib decreased the levels of the HCC biomarker α-fetoprotein, proving its effectiveness in the treatment of advanced HCC [208] However, the later phase III clinical trial, EVOLVE-1, conducted in patients with advanced HCC after sorafenib treatment or in patients with sorafenib intolerance, did not reveal a substantial difference in the overall survival rate when everolimus was given alone [209]. So far, as per the ClinicalTrials.gov website maintained by the National Library of Medicine at the National Institutes of Health, 334 findings have been identified on sorafenib and its use to treat early and advanced stages of HCC.…”