title: Dapagliflozin, an SGLT2 inhibitor for the treatment of type 2 diabetes.
abstract: 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.
authors.affiliation: Washington State University, Spokane, WA, USA. kdemaris@wsu.edu
authors.forename: K M
authors.initials: KM
authors.lastname: Demaris
authors.forename: J R
authors.initials: JR
authors.lastname: White
mesh_terms: D001559:Benzhydryl Compounds; D001786:Blood Glucose / Q000187:drug effects; D002986:Clinical Trials as Topic; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy* / Q000503:physiopathology; D017277:Drug Approval; D005960:Glucosides / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D006801:Humans; D007004:Hypoglycemic Agents / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D007328:Insulin / Q000378:metabolism; D051297:Sodium-Glucose Transporter 2; D000077203:Sodium-Glucose Transporter 2 Inhibitors
chemical_list: D001559:Benzhydryl Compounds; D001786:Blood Glucose; D005960:Glucosides; D007004:Hypoglycemic Agents; D007328:Insulin; C089180:SLC5A2 protein, human; D051297:Sodium-Glucose Transporter 2; D000077203:Sodium-Glucose Transporter 2 Inhibitors; C529054:dapagliflozin
keywords: BMS-512148; Dapagliflozin; SGLT2 inhibitor; Sodium/glucose cotransporter; Type 2 diabetes