Springer, Private Bag 65901, Mairangi Bay, 0754, Auckland, New Zealand.
Drugs. 2015 Nov;75(16):1903-13. doi: 10.1007/s40265-015-0483-x.
Axitinib (Inlyta(®)) is a potent, selective inhibitor of vascular endothelial growth factor receptor-1, -2 and -3. This article reviews the clinical efficacy and tolerability of axitinib in patients with previously-treated advanced renal cell carcinoma (RCC), as well as summarizing its pharmacological properties. Axitinib was effective in the second-line treatment of advanced RCC, according to the results of the pivotal, phase III AXIS trial. Median progression-free survival (PFS) was significantly prolonged with axitinib versus sorafenib (primary endpoint; independent review committee assessment); this PFS benefit was seen in patients who had received prior treatment with cytokines or sunitinib. The objective response rate was also significantly higher with axitinib than with sorafenib, with no significant between-group difference in median overall survival. Axitinib had a manageable tolerability profile in the AXIS trial, with the most commonly reported treatment-related adverse events including diarrhoea, hypertension, fatigue, decreased appetite, nausea, dysphonia, hand-foot syndrome and hypothyroidism. In conclusion, axitinib is an important option in previously-treated patients with advanced RCC.
阿昔替尼（英立达）是一种强效、选择性的血管内皮生长因子受体-1、-2 和 -3 抑制剂。本文回顾了阿昔替尼在先前治疗的晚期肾细胞癌（RCC）患者中的临床疗效和耐受性，并总结了其药理学特性。AXIS 关键性 III 期试验的结果表明，阿昔替尼在晚期 RCC 的二线治疗中是有效的。与索拉非尼相比，阿昔替尼显著延长了中位无进展生存期（PFS）（主要终点；独立审查委员会评估）；这一 PFS 获益见于接受过细胞因子或舒尼替尼治疗的患者中。阿昔替尼的客观缓解率也显著高于索拉非尼，两组之间的中位总生存期无显著差异。阿昔替尼在 AXIS 试验中的耐受性特征是可控的，最常见的报告治疗相关不良事件包括腹泻、高血压、疲劳、食欲下降、恶心、发音困难、手足综合征和甲状腺功能减退。总之，阿昔替尼是先前治疗的晚期 RCC 患者的一个重要选择。
