Phosphatidylinositol 3-kinase (PI3K)/Akt/mammalian target of rapamycin (mTOR) signaling pathway is one of the major cellular signaling pathways that plays an important role in basic intracellular functions. The PI3K/Akt/mTOR pathway regulates cell proliferation, growth, cell size, metabolism, and motility. Component genes of this pathway have been extensively studied and found to be commonly activated in human cancer. Inhibition of this pathway has been shown to lead to regression of human tumors and has been studied in preclinical setup and evaluated in many clinical trials at various levels. Some inhibitors of this pathway are approved by the Food and Drug Administration after their potency and safety have been shown in clinical trials. This review discusses the recent trends in exploiting the PI3K/Akt/mTOR pathway towards the molecular targeted therapy using small molecule inhibitors in human cancer.

磷脂酰肌醇3-激酶（PI3K）/ Akt /哺乳动物雷帕霉素靶标（mTOR）信号传导途径是主要的细胞信号传导途径之一，在基本的细胞内功能中起着重要的作用。PI3K / Akt / mTOR通路调节细胞增殖，生长，细胞大小，新陈代谢和运动性。已经对该途径的组成基因进行了广泛的研究，发现它们在人类癌症中通常被激活。已表明抑制该途径可导致人类肿瘤消退，并已在临床前研究中进行了研究，并在许多不同水平的临床试验中进行了评估。在临床试验中已证明其作用力和安全性后，该途径的某些抑制剂已获得美国食品药品监督管理局的批准。