Advances in Therapy

, 25:627

First online:

DPP4 Inhibitors: a new approach in diabetes treatment

  • John DoupisAffiliated withHarvard Medical School, Joslin Diabetes Center
  • , Aristidis VevesAffiliated withHarvard Medical School, Research Director, Microcirculation Lab, and Joslin-Beth Israel Deaconess Foot CenterMicrocirculation Lab, Palmer 317, Beth Israel Deaconess Medical Center Email author 

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The role of dipeptidyl peptidase-IV (DPP4) as both a regulatory enzyme and a signalling factor has been evaluated and described in many studies. DPP4 inhibition results in increased blood concentration of the incretin hormones glucagon-like peptide-1 (GLP-1) and gastric inhibitory polypeptide (GIP). This causes an increase in glucose-dependent stimulation of insulin secretion, resulting in a lowering of blood glucose levels. Recent studies have shown that DPP4 inhibitors can induce a significant reduction in glycosylated haemoglobin (HbA1c) levels, either as monotherapy or as a combination with other antidiabetic agents. Research has also demonstrated that DPP4 inhibitors portray a very low risk of hypoglycaemia development. This review article focuses on the two leading agents of this category (sitagliptin and vildagliptin), providing an overview of their function along with the latest data regarding their clinical efficacy as antidiabetic agents.


diabetes dipeptidyl peptidase-IV DPP4 sitagliptin vildagliptin