Autophagy is an important basic metabolic mechanism by engulfing and degrading the unnecessary or dysfunctional cellular components within double-membered autolysosomes to maintain cellular homeostasis. Autophagy has sparkled great interest for its complicated functions in different stages of cancer, and is regarded as a potential target for anticancer therapy. As a suppressor pathway, autophagy prevents tumor initiation and as a survival pathway, autophagy contributes to tumor growth and progression by attenuating cellular metabolic stress and resisting therapeutic agents-induced cell death. Many autophagy regulators have been identified as potential cancer therapeutic agents and some cytotoxic anticancer drugs also induce autophagy. Combination regimen of autophagy regulators with other anticancer agent exhibits desirable efficacy and several protocols are underway in clinical trials. This review delineates the possible role of autophagy in anticancer therapy, and discusses reported potent autophagy regulators in cancer treatment.