Department of Medical Oncology, Beatson West of Scotland Cancer Centre, 1053 Great Western Road, Glasgow, G12 OYN, UK.
Future Oncol. 2016 Oct;12(19):2195-204. doi: 10.2217/fon-2016-0215. Epub 2016 Jun 24.
Despite advances in metastatic renal cell carcinoma (mRCC) treatments, patients eventually progress and develop resistance to therapies targeting a single pathway. Lenvatinib inhibits VEGFR1-3, FGFR1-4, PDGFRβ, RET and KIT proto-oncogenes. In a randomized, Phase II trial evaluating patients with mRCC who had progressed after one prior VEGF-targeted therapy, progression-free survival was significantly improved with lenvatinib alone or in combination with everolimus versus everolimus alone. This review summarizes the clinical development of lenvatinib in mRCC, and how simultaneous targeting of multiple pathways involved in carcinogenesis and/or therapeutic resistance may improve patient outcomes. Lenvatinib plus everolimus may be a promising second-line treatment in patients with mRCC.
尽管转移性肾细胞癌（mRCC）的治疗取得了进展，但患者最终仍会进展并对靶向单一途径的治疗产生耐药性。仑伐替尼抑制 VEGFR1-3、FGFR1-4、PDGFRβ、RET 和 KIT 原癌基因。在一项评估先前接受过一种 VEGF 靶向治疗后进展的 mRCC 患者的随机、二期试验中，仑伐替尼单药或联合依维莫司治疗与依维莫司单药治疗相比，无进展生存期显著改善。本综述总结了仑伐替尼在 mRCC 中的临床开发情况，以及同时靶向参与肿瘤发生和/或治疗耐药性的多个途径如何改善患者的预后。仑伐替尼联合依维莫司可能是 mRCC 患者有前途的二线治疗药物。
