Neuwelt A J, Mathur S, Johnson A T, Kessler E R, Bowles D W
University of Colorado School of Medicine, Division of Medical Oncology, Aurora, Colorado, USA.
University of Colorado School of Medicine, Division of General Internal Medicine, Aurora, Colorado, USA.
Drugs Today (Barc). 2017 May;53(5):299-307. doi: 10.1358/dot.2017.53.5.2623107.
In the last several years, many new drugs have been approved to treat metastatic renal cell carcinoma (RCC). Cabozantinib is a novel multikinase inhibitor with activity against vascular endothelial growth factor receptor (VEGFR), proto-oncogene tyrosine-protein kinase receptor Ret and other kinases that recently joined this impressive list of approved agents. Cabozantinib is an active agent in the preclinical and clinical setting, having recently demonstrated superiority over everolimus in a blinded, randomized phase III study of patients with progressive RCC after at least one prior line of antiangiogenic therapy. This agent's toxicity profile is similar to those of other multikinase inhibitors approved to treat RCC. This review will explore cabozantinib's pharmacologic and safety profile and its preclinical and clinical activity in RCC.
在过去几年中，许多新药已被批准用于治疗转移性肾细胞癌（RCC）。卡博替尼是一种新型多激酶抑制剂，对血管内皮生长因子受体（VEGFR）、原癌基因酪氨酸蛋白激酶受体Ret及其他激酶具有活性，它最近加入了这一令人瞩目的已获批药物名单。卡博替尼在临床前和临床环境中均为活性药物，最近在一项针对至少接受过一线抗血管生成治疗后病情进展的RCC患者的双盲、随机III期研究中显示出优于依维莫司的疗效。该药物的毒性特征与其他获批用于治疗RCC的多激酶抑制剂相似。本综述将探讨卡博替尼的药理和安全性概况及其在RCC中的临床前和临床活性。
