University of Liège, Division of Diabetes, Nutrition and Metabolic Disorders, and Division of Clinical Pharmacology, Department of Medicine, CHU Sart Tilman (B35), B-4000 LIEGE 1, Belgium.
Expert Opin Pharmacother. 2012 Jan;13(1):81-99. doi: 10.1517/14656566.2012.642866.
Dipeptidylpeptidase-4 (DPP-4) inhibitors offer new options for the management of type 2 diabetes (T2DM).
This paper is an updated review, providing an analysis of both the similarities and the differences between the various compounds known as gliptins, currently used in the clinic (sitagliptin, vildagliptin, saxagliptin, alogliptin and linagliptin). This paper discusses the pharmacokinetic and pharmacodynamic characteristics of gliptins; both the efficacy and safety profiles of gliptins in clinical trials (compared with classical glucose-lowering agents), given as monotherapy or in combination, including in special populations; the positioning of DPP-4 inhibitors in the management of T2DM in recent guidelines; and various unanswered questions and perspectives.
The role of DPP-4 inhibitors in the therapeutic armamentarium of T2DM is evolving, as their potential strengths and weaknesses become better defined. Future critical issues may include the durability of glucose control, resulting from better β-cell protection, positive effects on cardiovascular outcomes and long-term safety issues.
二肽基肽酶-4(DPP-4)抑制剂为 2 型糖尿病(T2DM)的治疗提供了新的选择。
本文是一篇更新的综述,对目前临床应用的各种称为gliptins 的化合物(西他列汀、维格列汀、沙格列汀、阿格列汀和利格列汀)进行了分析,比较了它们之间的异同。本文讨论了 gliptins 的药代动力学和药效学特征;gliptins 在临床试验中的疗效和安全性概况(与传统降糖药物相比),包括单药治疗和联合治疗,包括特殊人群;在最近的指南中,DPP-4 抑制剂在 T2DM 治疗中的定位;以及各种未解决的问题和前景。
DPP-4 抑制剂在 T2DM 治疗武器库中的作用正在发展,因为其潜在的优势和劣势变得更加明确。未来的关键问题可能包括更好的β细胞保护带来的血糖控制的持久性、对心血管结局的积极影响以及长期安全性问题。