Demaris K M, White J R
Washington State University, Spokane, WA, USA.
Drugs Today (Barc). 2013 May;49(5):289-301. doi: 10.1358/dot.2013.49.5.1964714.
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.
达格列净是一种选择性、竞争性钠-葡萄糖协同转运蛋白2（SGLT2）抑制剂，作用是阻断肾脏中滤过葡萄糖的重吸收。这种新型治疗策略不依赖于胰腺β细胞功能或胰岛素敏感性的调节，可促进糖尿并直接降低血浆葡萄糖浓度。达格列净已在欧盟获批用于治疗2型糖尿病；然而，美国食品药品监督管理局基于缺乏有效评估获益-风险状况的临床数据而拒绝批准达格列净。本文将重点介绍肾脏葡萄糖调节和重吸收的生理学，简要概述达格列净的药理学，并讨论已完成的临床试验结果以及该药物的当前状况。
