Vivian Eva M
Eva M. Vivian, Pharm.D., M.S., BC-ADM, CDE, is Associate Professor, School of Pharmacy, University of Wisconsin, Madison (
Am J Health Syst Pharm. 2015 Mar 1;72(5):361-72. doi: 10.2146/ajhp140168.
The pharmacologic properties and clinical efficacy of dapagliflozin, a sodium-glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes, are reviewed.
Dapagliflozin (Farxiga, AstraZeneca) is a selective SGLT2 inhibitor approved as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes. Dapagliflozin lowers blood glucose independent of insulin secretion and action by inhibiting renal reabsorption of glucose, thus promoting increased urinary excretion of glucose. Dapagliflozin has been shown to improve glycemic parameters in patients with type 2 diabetes when used as monotherapy or in combination with metformin, glimepiride, pioglitazone, sitagliptin, or insulin. Dapagliflozin treatment is associated with weight reduction, it has a low intrinsic propensity to cause hypoglycemia, and it may offer the advantage of a complementary mechanism of action when added to other therapies. During Phase III clinical trials, dapagliflozin was generally well tolerated, with an overall frequency of adverse events similar to that reported with placebo use. However, increased rates of genital and, in some trials, urinary tract infections have been reported in dapagliflozin-treated groups relative to placebo groups. Pooled data from clinical trials indicated an imbalance in bladder cancer cases between dapagliflozin-treated and placebo groups; however, most cases were diagnosed within one year of exposure. Ongoing research is expected to further delineate the effects of dapagliflozin on bladder cancer risk and cardiovascular safety measures.
Dapagliflozin, an SGLT2 inhibitor, offers a novel treatment option for type 2 diabetes that is independent of insulin secretion or action.
综述达格列净（一种用于治疗2型糖尿病的钠-葡萄糖协同转运蛋白2[SGLT2]抑制剂）的药理特性和临床疗效。
达格列净（安达唐，阿斯利康公司）是一种选择性SGLT2抑制剂，被批准作为饮食和运动的辅助手段，用于改善2型糖尿病成人患者的血糖控制。达格列净通过抑制肾脏对葡萄糖的重吸收，从而促进葡萄糖尿排泄增加，降低血糖，其作用独立于胰岛素分泌和作用。已证明，达格列净作为单药治疗或与二甲双胍、格列美脲、吡格列酮、西格列汀或胰岛素联合使用时，可改善2型糖尿病患者的血糖参数。达格列净治疗与体重减轻相关联，其引起低血糖的内在倾向较低，并在添加到其他疗法时可能具有互补作用机制的优势。在III期临床试验期间，达格列净总体耐受性良好，不良事件总体发生率与使用安慰剂报告的相似。然而，与安慰剂组相比，达格列净治疗组报告的生殖器感染和在某些试验中的尿路感染发生率有所增加。临床试验的汇总数据表明，达格列净治疗组和安慰剂组之间膀胱癌病例存在失衡；然而，大多数病例是在暴露后一年内确诊的。正在进行的研究有望进一步阐明达格列净对膀胱癌风险和心血管安全措施的影响。
达格列净作为一种SGLT2抑制剂，为2型糖尿病提供了一种独立于胰岛素分泌或作用的新型治疗选择。
