A review of gliptins in 2011

• Published in: Expert opinion on pharmacotherapy Vol. 13; no. 1; p. 81
• Main Author: Scheen, André J
• Format: Journal Article
• Language: English
• Published: England 01.01.2012
• Subjects: Blood Glucose - drug effects; Diabetes Mellitus, Type 2 - blood; Diabetes Mellitus, Type 2 - drug therapy; Dipeptidyl-Peptidase IV Inhibitors - pharmacokinetics; Dipeptidyl-Peptidase IV Inhibitors - pharmacology; Dipeptidyl-Peptidase IV Inhibitors - therapeutic use; Humans; Hypoglycemic Agents - pharmacokinetics; Hypoglycemic Agents - pharmacology; Hypoglycemic Agents - therapeutic use
• ISSN: 1744-7666
• 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.