Clinical utility of dipeptidyl peptidase-4 inhibitors: a descriptive summary of current efficacy trials

To review efficacy and safety data of dipeptidyl peptidase-4 inhibitors used in treatment of patients with type 2 diabetes mellitus.

A search of MEDLINE®/PubMed®, a service of the National Library of Medicine of the National Institutes of Health as well as of the original publications of individual trials with dipeptidyl peptidase-4 inhibitors was carried out.

Dipeptidyl peptidase-4 inhibitors are orally administered medications indicated for improved glycemic control in patients with type 2 diabetes. They inhibit activity of the enzyme dipeptidyl peptidase-4 responsible for inactivating nutrient-released incretin hormones (mainly glucagon-like peptide-1 and glucose-dependent insulinotropic peptide). As a result, the effect of the incretin hormones is enhanced, leading to improved β-cell function and inhibition of the glucagon secretion from the pancreatic islets. Patients can expect to see lowering of fasting and postprandial glucose levels (by 0.5-1 mmol/l and 2-3 mmol/l, respectively), leading to reduction of hemoglobin A1c by 0.5-0.9% (depending on the baseline hemoglobin A1c).

Dipeptidyl peptidase-4 inhibitors are generally well tolerated, with minimal risks of hypoglycemia or weight gain. Many postmarketing and surveillance studies are now conducted which focus on long-term safety and cardiovascular outcomes.