肿瘤药学
腫瘤藥學
종류약학
ANTI-TUMOR PHARMACY
2013年
6期
422-425
,共4页
依维莫司%mTOR抑制剂%肿瘤%临床应用
依維莫司%mTOR抑製劑%腫瘤%臨床應用
의유막사%mTOR억제제%종류%림상응용
Everolimus%mTOR inhibitor%Tumor%Clinical application
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。
依維莫司(everolimus)是雷帕黴素的40-O-2-(羥乙基)衍生物,為哺乳動物雷帕黴素靶蛋白(mTOR)抑製劑。除瞭免疫抑製作用外,它能持續抑製mTOR靶點,達到抑製腫瘤生長與增殖、抑製腫瘤營養代謝和抑製腫瘤新生血管形成等三重抗腫瘤作用。在國外已被批準用于治療晚期腎癌、乳腺癌、不能外科切除的進展性或轉移性胰腺神經內分泌瘤以及伴有結節性硬化癥(TSC)的室管膜下巨細胞星形細胞瘤(SEGA);在我國也已被批準用于晚期腎癌。依維莫司對其他的腫瘤的療效及安全性也正在進行臨床試驗。本文簡要介紹依維莫司的作用機製以及在腫瘤治療中的臨床應用。
의유막사(everolimus)시뢰파매소적40-O-2-(간을기)연생물,위포유동물뢰파매소파단백(mTOR)억제제。제료면역억제작용외,타능지속억제mTOR파점,체도억제종류생장여증식、억제종류영양대사화억제종류신생혈관형성등삼중항종류작용。재국외이피비준용우치료만기신암、유선암、불능외과절제적진전성혹전이성이선신경내분비류이급반유결절성경화증(TSC)적실관막하거세포성형세포류(SEGA);재아국야이피비준용우만기신암。의유막사대기타적종류적료효급안전성야정재진행림상시험。본문간요개소의유막사적작용궤제이급재종류치료중적림상응용。
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.