Rapamycin 和它的类似物(rapalogs ) 是 mTOR 禁止者的第一代,它有一样的分子的支架,而是不同 physiochemical 性质。Rapalogs 作为 monotherapy 和联合治疗的一个部件在大量人的肿瘤正在被测试。在他们之中, temsirolimus 和 everolimus 为胸和肾的癌症的治疗被同意了。然而,有在临床的试用的 rapalogs 的客观反应率谦虚、可变。预言反应到 rapalogs 的 biomarkers 的鉴定,和有改进功效和容忍的毒性的药联合的发现对向前移动指向的治疗学的这个班批评。这评论为 rapalog 功效作为预兆的 biomarkers 在人的肿瘤房间或纸巾在 PI3K/mTOR 小径集中于错误。用 rapalogs 和另外的 anticancer 药的 combinational 治疗的最近的结果被记录。与下一代的 genomic 定序和精确药的快速的发展, rapalogs 将提供更大的好处给癌症病人。
Rapamycin and its analogs (rapalogs) are the first generation of mTOR inhibitors, which have the same molecular scaffold, but different physiochemical properties. Rapalogs are being tested in a wide spectrum of human tumors as both monotherapy and a component of combination therapy. Among them, temsirolimus and everolimus have been approved for the treatment of breast and renal cancer. However, objective response rates with rapalogs in clinical trials are modest and variable. Identification of biomarkers predicting response to rapalogs, and discovery of drug combinations with improved efficacy and tolerated toxicity are critical to moving this class of targeted therapeutics forward. This review focuses on the aberrations in the PI3K/mTOR pathway in human tumor cells or tissues as predictive biomarkers for rapalog efficacy. Recent results of combinational therapy using rapalogs and other anticancer drugs are documented. With the rapid development of next-generation genomic sequencing and precision medicine, rapalogs will provide greater benefits to cancer patients.