The sodium glucose cotransporter 2 (SGLT2) is expressed primarily in the kidneys and is involved in the reabsorption of filtered glucose in the renal tubule. Clinical trials of SGLT2 inhibitors in patients with type 2 diabetes mellitus demonstrate a significant clinical effect in decreasing serum glucose, hemoglobin A1C, body weight, systolic blood pressure, improving β-cell function, and minimizing the risk of hypoglycemia. This report reviews the potentially beneficial effects of SGLT2 inhibitors in type 2 diabetes mellitus, specifically focusing on canagliflozin, the only SGLT2 inhibitor approved for use in the United States.