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依维莫司(everolimus)是具有口服活性的雷帕霉素靶蛋白(mTOR)抑制剂,2009年2月获FDA批准用于治疗晚期肾细胞癌(商品名:Afinitor)。2010年4月,FDA批准其用于预防成人肾脏移植器官排斥(商品名:Zortress),同年10月,又批准其用于室管膜下巨细胞星形细胞瘤(SEGA)的治疗(商品名:Afinitor)。文中对依维莫司在治疗SEGA中的药理作用、药代动力学、临床研究及安全性等做一综述,并对其在其他适应症上的应用做一简单介绍。
Everolimus, an orally active rapamycin target protein (mTOR) inhibitor, was approved by the FDA in February 2009 for the treatment of advanced renal cell carcinoma (product name: Afinitor). In April 2010, the FDA approved its use for the prevention of organ transplant rejection in adults (Zortress), and in October of the same year, approved its use for subependymal giant cell astrocytoma (SEGA) Name: Afinitor). This article reviews the pharmacological effects, pharmacokinetics, clinical studies and safety of everolimus in the treatment of SEGA, and gives a brief introduction of its application in other indications.