Faivre Sandrine, Kroemer Guido, Raymond Eric
Service Inter Hospitalier de Cancrologie, Beaujon University Hospital, 100 Boulevard du General Leclerc, 92118 Clichy Cedex, France.
Nat Rev Drug Discov. 2006 Aug;5(8):671-88. doi: 10.1038/nrd2062.
Mammalian target of rapamycin (mTOR) is a kinase that functions as a master switch between catabolic and anabolic metabolism and as such is a target for the design of anticancer agents. The most established mTOR inhibitors--rapamycin and its derivatives--showed long-lasting objective tumour responses in clinical trials, with CCI-779 being a first-in-class mTOR inhibitor that improved the survival of patients with advanced renal cell carcinoma. This heralded the beginning of extensive clinical programmes to further evaluate mTOR inhibitors in several tumour types. Here we review the clinical development of this drug class and look at future prospects for incorporating these agents into multitarget or multimodality strategies against cancer.
雷帕霉素哺乳动物靶点（mTOR）是一种激酶，在分解代谢和合成代谢之间起主开关的作用，因此是抗癌药物设计的靶点。最成熟的mTOR抑制剂——雷帕霉素及其衍生物——在临床试验中显示出持久的客观肿瘤反应，CCI-779是首个改善晚期肾细胞癌患者生存率的mTOR抑制剂。这预示着广泛的临床项目的开始，以进一步评估mTOR抑制剂在多种肿瘤类型中的作用。在此，我们回顾这类药物的临床进展，并探讨将这些药物纳入多靶点或多模式抗癌策略的未来前景。
