Stock Christian, Zaccagnini Massimo, Schulze Michael, Teber Dogu, Rassweiler Jens J
Department of Urology, SLK-Kliniken Heilbronn GmbH, Medizinsche Klinik III, Germany.
Recent Results Cancer Res. 2010;184:189-97. doi: 10.1007/978-3-642-01222-8_13.
Temsirolimus, an ester of sirolimus (rapamycin), selectively inhibits the kinase mammalian target of rapamycin and consequently blocks the translation of cell cycle regulatory proteins and prevents overexpression of angiogenic growth factors. Patients with advanced renal cell carcinoma (RCC) and a poor prognosis who received a once-weekly intravenous (IV) infusion of temsirolimus 25 mg, experienced significant survival benefits when compared with patients receiving standard interferon-alpha (IFNalpha) therapy in a large phase III clinical study. In this study, median overall survival was 10.9 vs. 7.3 months and objective response rates were 8.6% in temsirolimus recipients vs. 4.8% IFNalpha recipient group.Temsirolimus monotherapy recipients experienced significantly fewer grade 3 or 4 adverse events and had fewer withdrawals for adverse events than patients receiving IFNalpha.
替西罗莫司是西罗莫司（雷帕霉素）的酯化物，它选择性抑制雷帕霉素的哺乳动物靶点激酶，从而阻断细胞周期调节蛋白的翻译，并防止血管生成生长因子的过度表达。在一项大型III期临床研究中，与接受标准α干扰素（IFNα）治疗的患者相比，接受每周一次静脉输注25mg替西罗莫司的晚期肾细胞癌（RCC）且预后较差的患者有显著的生存获益。在该研究中，替西罗莫司组的中位总生存期为10.9个月，而IFNα组为7.3个月；替西罗莫司组的客观缓解率为8.6%，IFNα组为4.8%。与接受IFNα的患者相比，接受替西罗莫司单药治疗的患者发生3级或4级不良事件的情况明显更少，因不良事件而停药的情况也更少。
