Dapagliflozin, an SGLT2 inhibitor for the treatment of type 2 diabetes.

摘要

Dapagliflozin is a selective, competitive inhibitor of sodium/glucose cotransporter 2 (SGLT2) acting to block reabsorption of filtered glucose in the kidney. Independent of pancreatic β cell function or the modulation of insulin sensitivity, this novel treatment strategy promotes glucosuria and direct lowering of plasma glucose concentrations. Dapagliflozin has been approved for the treatment of type 2 diabetes in the European Union; however, the United States Food and Drug Administration rejected the approval of dapagliflozin based on lack of clinical data to effectively assess the benefit-to-risk profile. This manuscript will highlight the physiology of renal glucose regulation and reabsorption, briefly outline the pharmacology of dapagliflozin and discuss the results of completed clinical trials as well as the current status of the drug.