Everolimus.
Everolimus.
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DOI：
10.1158/1078-0432.ccr-09-1314
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发表时间：
2010-03-01
期刊：
影响因子：
--
通讯作者：
Houghton PJ
中科院分区：
文献类型：
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作者：
Houghton PJ
依维莫司是一种口服雷帕霉素类似物，最近已被FDA批准用于治疗血管内皮生长因子（VEGF）受体信号传导抑制剂难治性肾细胞癌（RCC）。依维莫司显著增加了无进展生存期（依维莫司治疗组的中位PFS为4.0个月，而安慰剂组为1.9个月），尽管肿瘤消退仅偶尔观察到。虽然依维莫司的靶点（丝氨酸/苏氨酸激酶mTOR）已经很好地建立，但这种药物延缓肿瘤生长的机制还没有很好地确定。此外，预测肿瘤敏感性的生物标志物仍然难以捉摸。本文综述了依维莫司抗肾细胞癌的作用机制、临床前抗肿瘤活性和临床活性。
Everolimus, an orally adminstered rapamycin analog, has recently been approved by the FDA for treatment of renal cell carcinoma (RCC) refractory to inhibitors of vascular endothelial growth factor (VEGF) receptor signaling. Everolimus significantly increased progression-free survival (median PFS for the everolimus treated group was 4.0 months versus 1.9 months for the placebo group), although tumor regressions were observed only infrequently. While the target for everolimus, (the serine/threonine kinase mTOR) is well established, the mechanism by which this agent retards tumor growth is not well defined. Further, biomarkers that predict tumor sensitivity are still elusive. The mechanism of action, preclinical antitumor activity, and clinical activity of everolimus against RCC are reviewed.