Saisho Yoshifumi
Department of Internal Medicine, Keio University School of Medicine, Tokyo, Japan.
Vasc Health Risk Manag. 2015 Apr 10;11:229-43. doi: 10.2147/VHRM.S68564. eCollection 2015.
Dipeptidyl peptidase-4 (DPP-4) inhibitors, a new class of oral hypoglycemic agents, augment glucose-dependent insulin secretion and suppress glucagon levels through enhancement of the action of endogenous incretin by inhibiting DPP-4, an incretin-degrading enzyme. DPP-4 inhibitors are generally well tolerated because of their low risk of hypoglycemia and other adverse events. Moreover, with their potential to improve beta cell function, a core defect of type 2 diabetes, DPP-4 inhibitors are becoming a major component of treatment of type 2 diabetes. Alogliptin benzoate is a newly developed, highly selective DPP-4 inhibitor which has been approved in many countries throughout the world. Once-daily administration of alogliptin as either monotherapy or combination therapy with other oral antidiabetic drugs or insulin has a potent glucose-lowering effect which is similar to that of other DPP-4 inhibitors, with a low risk of hypoglycemia and weight gain. The cardiovascular safety of this drug has been confirmed in a recent randomized controlled trial. This review summarizes the efficacy and safety of alogliptin, and discusses the role of DPP-4 inhibitors in the treatment of type 2 diabetes.
二肽基肽酶-4（DPP-4）抑制剂是一类新型口服降糖药，通过抑制二肽基肽酶-4（一种肠促胰岛素降解酶）增强内源性肠促胰岛素的作用，从而增加葡萄糖依赖性胰岛素分泌并抑制胰高血糖素水平。DPP-4抑制剂通常耐受性良好，因为其低血糖和其他不良事件风险较低。此外，由于DPP-4抑制剂具有改善2型糖尿病核心缺陷——β细胞功能的潜力，它们正成为2型糖尿病治疗的主要组成部分。苯甲酸阿格列汀是一种新开发的、高选择性的DPP-4抑制剂，已在世界许多国家获得批准。阿格列汀每日一次单药治疗或与其他口服抗糖尿病药物或胰岛素联合治疗，均具有强效降糖作用，与其他DPP-4抑制剂相似，低血糖和体重增加风险较低。该药物的心血管安全性已在最近一项随机对照试验中得到证实。本综述总结了阿格列汀的疗效和安全性，并讨论了DPP-4抑制剂在2型糖尿病治疗中的作用。
