mTOR抑制剂依维莫司在肿瘤治疗中的临床应用

摘要

Everolimus, a 40-O-[2-hydroxyethyl]derivative of rapamycin, is a mammalian target of rapamycin inhibitor. Excepting immunosuppression, everolimus exhibits an ability of continuously inhibiting mammalian target of rapamycin(mTOR), which may contribute to its triple activity of inhibiting development and proliferation, nutrition metabolism and angiogenesis of tumors. Everolimus has been approved overseas for the treatment of advanced metastatic renal cell carcinoma, breast cancer, ad-vanced pancreatic neuroendocrine tumor and subependymal giant-cell astrocytoma (SEGA) associated with tuberous sclerosis complex (TSC). In China, everolimus has just been approved for treating advanced metastatic renal cell carcinoma so far. The safety and efficacy of everolimus is still being studied on other tumors. In this review, it is focused to briefly introduce the mecha-nism and anti-cancer efficacy of everolimus.%依维莫司（everolimus）是雷帕霉素的40-O-2-(羟乙基)衍生物，为哺乳动物雷帕霉素靶蛋白（mTOR）抑制剂。除了免疫抑制作用外，它能持续抑制mTOR靶点，达到抑制肿瘤生长与增殖、抑制肿瘤营养代谢和抑制肿瘤新生血管形成等三重抗肿瘤作用。在国外已被批准用于治疗晚期肾癌、乳腺癌、不能外科切除的进展性或转移性胰腺神经内分泌瘤以及伴有结节性硬化症（TSC）的室管膜下巨细胞星形细胞瘤（SEGA）；在我国也已被批准用于晚期肾癌。依维莫司对其他的肿瘤的疗效及安全性也正在进行临床试验。本文简要介绍依维莫司的作用机制以及在肿瘤治疗中的临床应用。