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, advanced pancreatic neuroendocrine tumor and subependymal giant-cell astrocytoma (SEGA) associated with tuberous sclerosis complex (TSC). In China, everolimus has just been approved to treating advanced metastatic renal cell carcinoma so far. The safety and efficacy of everolimus has still been studied on other tumors. In this review, it is focused to briefly introduce the mechanism and anti-cancer efficacy of everolimus.