Dapagliflozin: A new sodium-glucose cotransporter 2 inhibitor for treatment of type 2 diabetes
Dapagliflozin: A new sodium-glucose cotransporter 2 inhibitor for treatment of type 2 diabetes
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DOI：
10.2146/ajhp140168
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发表时间：
2015-03-01
影响因子：
2.7
通讯作者：
Vivian, Eva M.
中科院分区：
文献类型：
--
作者：
Vivian, Eva M.
目的。本文综述了治疗2型糖尿病的糖钠共转运体2(SGLT2)抑制剂达帕格列酮的药理性质和临床疗效。达帕利夫津(Farxiga，AstraZeneca)是一种选择性SGLT2抑制剂，被批准作为饮食和运动的补充，以改善成年2型糖尿病患者的血糖控制。达帕格列酮通过抑制肾脏对葡萄糖的重吸收来降低血糖，不依赖于胰岛素的分泌和作用，从而促进尿糖排泄增加。达格列酮已被证明可以改善2型糖尿病患者的血糖参数，当作为单一治疗或与二甲双胍、格列美脲、吡格列酮、西格列汀或胰岛素联合使用时。达帕利嗪治疗与减轻体重有关，它引起低血糖的内在倾向很低，当与其他治疗方法一起使用时，它可能提供补充作用机制的优势。在I期临床试验期间，达帕利嗪总体耐受性良好，不良事件的总体频率与使用安慰剂报告的相似。然而，与安慰剂组相比，达帕利嗪治疗组的生殖器感染率和一些试验中的尿路感染发生率都有所增加。来自临床试验的汇集数据表明，达格列酮治疗组和安慰剂组之间的膀胱癌病例比例不平衡；然而，大多数病例是在暴露后一年内被诊断出来的。正在进行的研究有望进一步阐明达格列酮对膀胱癌风险和心血管安全措施的影响。达帕利福秦是一种SGLT2抑制剂，它为2型糖尿病提供了一种不依赖于胰岛素分泌或作用的新治疗选择。
Purpose. The pharmacologic properties and clinical efficacy of dapagliflozin, a sodium glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes, are reviewed.Summary. 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 Ill 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.Conclusion. Dapagliflozin, an SGLT2 inhibitor, offers a novel treatment option for type 2 diabetes that is independent of insulin secretion or action.