DPP4 inhibitors: a new approach in diabetes treatment

Adv Ther. 2008 Jul;25(7):627-43. doi: 10.1007/s12325-008-0076-1.

Abstract

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 (HbA(1c)) 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.

Publication types

  • Review

MeSH terms

  • Adamantane / analogs & derivatives
  • Adamantane / pharmacology
  • Adamantane / therapeutic use
  • Animals
  • Blood Glucose / analysis
  • Diabetes Mellitus, Type 2 / drug therapy*
  • Diabetes Mellitus, Type 2 / physiopathology
  • Dipeptidyl-Peptidase IV Inhibitors / pharmacology
  • Dipeptidyl-Peptidase IV Inhibitors / therapeutic use*
  • Drug Therapy, Combination
  • Gastric Inhibitory Polypeptide / blood
  • Glucagon-Like Peptide 1 / blood
  • Glycated Hemoglobin A / analysis
  • Humans
  • Hypoglycemic Agents / pharmacology
  • Hypoglycemic Agents / therapeutic use*
  • Incretins / metabolism
  • Insulin / metabolism
  • Insulin Secretion
  • Nitriles / pharmacology
  • Nitriles / therapeutic use
  • Pyrazines / pharmacology
  • Pyrazines / therapeutic use
  • Pyrrolidines / pharmacology
  • Pyrrolidines / therapeutic use
  • Sitagliptin Phosphate
  • Triazoles / pharmacology
  • Triazoles / therapeutic use
  • Vildagliptin

Substances

  • Blood Glucose
  • Dipeptidyl-Peptidase IV Inhibitors
  • Glycated Hemoglobin A
  • Hypoglycemic Agents
  • Incretins
  • Insulin
  • Nitriles
  • Pyrazines
  • Pyrrolidines
  • Triazoles
  • Gastric Inhibitory Polypeptide
  • Glucagon-Like Peptide 1
  • Vildagliptin
  • Adamantane
  • Sitagliptin Phosphate