School of Life Sciences, Fudan University, Shanghai 200438, China.
International Cooperation Laboratory of Signal Transduction, Eastern Hepatobiliary Surgery Institute, China.
Biochim Biophys Acta Rev Cancer. 2020 Aug;1874(1):188391. doi: 10.1016/j.bbcan.2020.188391. Epub 2020 Jul 10.
Lenvatinib, a multi-target tyrosine kinase inhibitor (TKI), is an emerging first-line therapy for hepatocellular carcinoma (HCC). Its application has changed the status of sorafenib as the only first-line TKI treatment for HCC for more than a decade. Evidence has shown that lenvatinib possesses antitumor proliferation and immunomodulatory activity in preclinical studies. In comparison, lenvatinib was non-inferior to sorafenib in overall survival (OS), and even shows superiority with regard to all the secondary efficacy endpoints. Immune-checkpoint inhibitors(ICIs)are now being incorporated into HCC treatment. Positive outcomes have been achieved in the combination of lenvatinib plus ICIs, bringing broader prospects for HCC. This review presents an overview on the therapeutic mechanisms and clinical efficacy of lenvatinib in HCC, and we discuss the future perspectives of lenvatinib in HCC management with focus on biomarker-guided precision medicine.
仑伐替尼是一种多靶点酪氨酸激酶抑制剂（TKI），是新兴的肝细胞癌（HCC）一线治疗药物。其应用改变了索拉非尼作为 HCC 唯一一线 TKI 治疗药物十余年的局面。临床前研究表明仑伐替尼具有抗肿瘤增殖和免疫调节活性。与索拉非尼相比，仑伐替尼在总生存期（OS）方面非劣效，甚至在所有次要疗效终点方面都显示出优势。免疫检查点抑制剂（ICIs）现在已被纳入 HCC 的治疗。仑伐替尼联合 ICIs 取得了积极的结果，为 HCC 带来了更广阔的前景。本文综述了仑伐替尼治疗 HCC 的治疗机制和临床疗效，并讨论了基于生物标志物的精准医学指导下仑伐替尼在 HCC 管理中的未来前景。
