Emerging gliptins for type 2 diabetes

作者：Cahn Avivit; Raz Itamar^*

来源：Expert Opinion on Emerging Drugs, 2013, 18(2): 245-258.

DOI：10.1517/14728214.2013.807796

• aloglitpin
• anagliptin
• DPP-4 inhibitor
• evogliptin
• gemigliptin
• gosogliptin
• linagliptin
• melogliptin
• omarigliptin
• saxagliptin
• sitagliptin
• teneligliptin
• trelagliptin
• vildagliptin

Introduction: The dipeptidyl peptidase-4 (DPP-4) inhibitors (gliptins) are novel oral hypoglycemic drugs which have been in clinical use for the past 7 years. The drugs are safe, weight neutral and widely prescribed. There are currently eight gliptins registered worldwide with several more in advanced stages of development.
Areas covered: The place of the gliptins in the treatment algorithm of type 2 diabetes is discussed as well as unique features of the individual drugs. The gliptins may possess cardiovascular protective effects and their administration may promote beta-cell survival; claims currently being evaluated in clinical and preclinical studies. The global market revenues and future prospects of the gliptins are discussed and the gliptins in Phases II and III of development are reviewed.
Expert opinion: The gliptins are an optional second-line therapy after metformin; they are generally well tolerated with low risk of hypoglycemia. The various compounds differ with respect to their pharmacokinetic and pharmacodynamic properties; however, their clinical efficacy appears to be similar. The clinical differences between the various compounds stem from effects other than hypoglycemic effects, their safety and side effects profile. The currently registered compounds appear to have maximized the clinical potential of DPP-4 inhibition, and the new compounds in the companies' pipelines seem to be as effective as the ones presently in use. There are two gliptins in advanced stages of development which will be registered for once-weekly dosing, possibly increasing patient adherence to therapy. Several individual gliptins are being evaluated for treatment in diabetes subpopulations such as type 1 patients or adolescents.

• 出版日期2013-6