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Drugs. 2015 Apr;75(5):553-60. doi: 10.1007/s40265-015-0383-0.
Lenvatinib (Lenvima™) is a multitargeted receptor kinase inhibitor that inhibits the kinase activities of vascular endothelial-derived growth factor receptors 1, 2 and 3, fibroblast growth factor receptors 1, 2, 3 and 4, platelet-derived growth factor receptor α, RET and KIT. In addition to their role in normal cellular function, these kinases have been implicated in pathogenic angiogenesis, tumour growth and cancer progression. Lenvatinib is being developed by Eisai Co. Ltd for the treatment of solid tumours, primarily for differentiated thyroid cancer, and other malignancies. A capsule formulation of the drug has received approval in the USA for use in locally recurrent or metastatic, progressive, radioactive iodine-refractory differentiated thyroid cancer. Lenvatinib is in pre-registration for this indication in the EU, Australia, Brazil, Canada, Japan, South Korea, Russia, Singapore and Switzerland, and is in phase 3 development in Argentina, Chile and Thailand. Lenvatinib has orphan designation in the EU and Japan for use in differentiated thyroid cancer. In addition, an ongoing global, phase 3 trial is evaluating the use of lenvatinib as first-line treatment in unresectable hepatocellular carcinoma. This article summarizes the milestones in the development of lenvatinib leading to this first approval in locally recurrent or metastatic, progressive, radioactive iodine-refractory differentiated thyroid cancer.
乐伐替尼（Lenvima™）是一种多靶点受体激酶抑制剂，可抑制血管内皮衍生的生长因子受体 1、2 和 3、成纤维细胞生长因子受体 1、2、3 和 4、血小板衍生生长因子受体 α、RET 和 KIT 的激酶活性。除了在正常细胞功能中的作用外，这些激酶还与病理性血管生成、肿瘤生长和癌症进展有关。乐伐替尼由卫材株式会社开发用于治疗实体瘤，主要用于分化型甲状腺癌和其他恶性肿瘤。该药的胶囊制剂已获得美国批准用于局部复发性或转移性、进行性、放射性碘难治性分化型甲状腺癌。该药在欧盟、澳大利亚、巴西、加拿大、日本、韩国、俄罗斯、新加坡和瑞士的注册前阶段用于该适应症，在阿根廷、智利和泰国也处于 3 期开发阶段。乐伐替尼在欧盟和日本被指定用于治疗分化型甲状腺癌的孤儿药。此外，一项正在进行的全球 3 期试验正在评估乐伐替尼作为不可切除肝细胞癌一线治疗的用途。本文总结了乐伐替尼开发过程中的重要里程碑，最终使其在局部复发性或转移性、进行性、放射性碘难治性分化型甲状腺癌中获得首次批准。
