Sodium-glucose cotransporter 2 (SGLT2), located in the renal proximal convoluted tubule, is responsible for the glucose reabsorption by the kidney, and SGLT2 inhibitors are new class of glucose-lowering drugs that reduce renal glucose reabsorption and lead to increased urinary glucose excretion. SGLT2 is a low-affinity, high-capacity transporter and is overexpressed in patients with type 2 diabetes mellitus and is responsible for over 80% of renal glucose reabsorption. The mechanism of action is independent of insulin secretion or action. Several SGLT2 inhibitors had been developed and some of them are recently approved for the treatment of type 2 diabetes by US FDA and EMA. They effectively improve glycemic control in patients with type 2 diabetes when used as monotherapy, or added to other oral hypoglycemic agents and/or insulin. They are well tolerated and showed a low risk of hypoglycaemia. Other favorable effects associated with SGLT2 inhibitors include decreased body weight and reductions in systolic blood pressure. Adverse effects associated with SGLT2 inhibitors included genital and urinary tract infections. As SGLT2 inhibitors directly target the kidney, and is expected to be effective regardless of the degree of beta-cell dysfunction, they might be a promising antidiabetic drug both as monotherapy or in combination with any other diabetic medications.