Adis, Auckland, New Zealand.
Drugs. 2009 Oct 22;69(15):2115-24. doi: 10.2165/11203770-000000000-00000.
Everolimus is an orally administered, targeted therapy indicated for the treatment of advanced renal cell carcinoma. It inhibits the mammalian target of rapamycin, an integral component of multiple pathways involved in cell growth and proliferation. Median progression-free survival was significantly longer with everolimus 10 mg once daily than with placebo in both second interim (4.0 vs 1.9 months) and updated (4.9 vs 1.9 months) analyses of a randomized, double-blind, placebo-controlled, multicentre, phase III trial in patients with metastatic renal cell carcinoma that had progressed while receiving sunitinib and/or sorafenib treatment. At the second interim analysis, median overall survival was 8.8 months for placebo recipients; at this analysis, overall survival had not yet been reached for everolimus recipients. With regard to objective response at the second interim analysis, 64% of everolimus and 32% of placebo recipients had either a partial response (1% and 0%) or stable disease (63% and 32%). The tolerability profile of everolimus was largely manageable in the phase III trial, with most treatment-related adverse events being of grade 1 or 2 severity.
依维莫司是一种口服靶向治疗药物，适用于治疗晚期肾细胞癌。它抑制哺乳动物雷帕霉素靶蛋白，这是参与细胞生长和增殖的多个途径的重要组成部分。在接受舒尼替尼和/或索拉非尼治疗后进展的转移性肾细胞癌患者的一项随机、双盲、安慰剂对照、多中心、III 期试验的第二次中期分析（4.0 与 1.9 个月）和更新分析（4.9 与 1.9 个月）中，依维莫司 10mg 每日一次的无进展生存期显著长于安慰剂。在第二次中期分析中，安慰剂组的中位总生存期为 8.8 个月；在此次分析中，依维莫司组的总生存期尚未达到。在第二次中期分析时，依维莫司组的客观缓解率为 64%，安慰剂组为 32%，分别为部分缓解（1%和 0%）或疾病稳定（63%和 32%）。在 III 期试验中，依维莫司的耐受性特征在很大程度上是可控的，大多数与治疗相关的不良事件为 1 级或 2 级严重程度。
