GLP-1 agonists and dipeptidyl-peptidase IV inhibitors

Handb Exp Pharmacol. 2011:(203):53-74. doi: 10.1007/978-3-642-17214-4_3.

Abstract

Novel therapeutic options for type 2 diabetes based on the action of the incretin hormone glucagon-like peptide-1 (GLP-1) were introduced in 2005. Incretin-based therapies consist of two classes: (1) the injectable GLP-1 receptor agonists solely acting on the GLP-1 receptor and (2) dipeptidyl-peptidase inhibitors (DPP-4 inhibitors) as oral medications raising endogenous GLP-1 and other hormone levels by inhibiting the degrading enzyme DPP-4. In type 2 diabetes therapy, incretin-based therapies are attractive and more commonly used due to their action and safety profile. Stimulation of insulin secretion and inhibition of glucagon secretion by the above-mentioned agents occur in a glucose-dependent manner. Therefore, incretin-based therapies have no intrinsic risk for hypoglycemias. GLP-1 receptor agonists allow weight loss; DPP-4 inhibitors are weight neutral. This review gives an overview on the mechanism of action and the substances and clinical data available.

Publication types

  • Review

MeSH terms

  • Diabetes Mellitus, Type 1 / drug therapy
  • Diabetes Mellitus, Type 2 / drug therapy*
  • Dipeptidyl Peptidase 4 / physiology
  • Dipeptidyl-Peptidase IV Inhibitors / therapeutic use*
  • Glucagon-Like Peptide 1 / agonists*
  • Guidelines as Topic
  • Humans
  • Hypoglycemic Agents / therapeutic use*
  • Incretins / antagonists & inhibitors
  • Incretins / physiology

Substances

  • Dipeptidyl-Peptidase IV Inhibitors
  • Hypoglycemic Agents
  • Incretins
  • Glucagon-Like Peptide 1
  • Dipeptidyl Peptidase 4