Metformin is the most commonly prescribed drug for type 2 diabetes mellitus as it is inexpensive, safe, and efficient in ameliorating hyperglycemia and hyperinsulinemia. Epidemiological and clinical observation studies have shown that metformin use reduces risk of cancer in patients with type 2 diabetes mellitus and improves prognosis and survival rate of the cancer patients. Furthermore, ongoing clinical trials of metformin in cancer therapy are extending to nondiabetic population. Thus, metformin is emerging as an attractive candidate for cancer prevention and treatment. This review summarizes recent progress in studies of metformin use in cancer and discusses the possibility to enhance its efficacy and to prevent cancer metastasis.