Inhibitors of sodium-dependent glucose co-transporter 2 (SGLT2) with a novel insulin-independent action are a promising new therapeutic option for the treatment of type 2 diabetes by suppressing the reabsorption of filtered glucose in the kidney, which leads to urinary glucose excretion and hence reduces the plasma glucose concentration. In addition to the therapeutic benefit in attaining glycemic control, low risk of hypoglycemia and reduction in weight and blood pressure make SGLT2 inhibitors more unique; however, long-term follow-up of patients was recommended due to the unexpected side-effects. Herein, the development of SGLT2 inhibitors is briefly summarized in this article.