口服多靶点酪氨酸激酶抑制剂——乐伐替尼  

An oral multiple receptor tyrosine kinase inhibitor——Lenvatinib

作　　者：王凌霄[1] 肖典[1] 周辛波[1] 

机构地区：[1]国家应急防控药物工程技术研究中心军事医学科学院毒物药物研究所,北京100850

出　　处：《临床药物治疗杂志》2015年第5期11-14,共4页Clinical Medication Journal

基　　金：国家应急防控药物工程技术研究中心学术支持

摘　　要：乐伐替尼(Lenvatinib)是由日本卫材公司研制的口服多靶点酪氨酸激酶抑制剂(TKI)。2015年2月,美国FDA批准其用于晚期放射性-碘难治性分化型甲状腺癌的治疗,或将成为不可切除性甲状腺癌临床治疗的新标准。业界对乐伐替尼非常看好,其在肾细胞癌等其他适应证方面的研究也值得期待。笔者就乐伐替尼的基本性质、作用机制、药动学、药效学、临床试验及应用等研发动态作一概述,以期能为医院临床用药起到指导作用。Lenvatinib is an oral multiple receptor tyrosine kinase inhibitor （TKI） developed by Eisai. In February 2005, Lenvatinib has been approved for the treatment of patients with locally recurrent or metastatic, progressive, radioactive iodine-refractory differentiated thyroid cancer （DTC）, which provides an option to alleviate the seriously unmet medical needs for thyroid cancer. People generally believe that the future of lenvatinib is promising, and the studies of lenvatinib in renal cell carcinoma and other indications are also really to be expected. In this paper, the development process, properties, mechanism, pharmacokinetics, pharmacodynamics, clinical trials and applications of lenvatinib are summarized, in order to provide reference for clinical treatment.

关 键 词：乐伐替尼 多靶点酪氨酸激酶抑制剂 分化型甲状腺癌 

分 类 号：R979.1[医药卫生—药品]