Emerging GLP-1 receptor agonists

Expert Opin Emerg Drugs. 2011 Dec;16(4):607-18. doi: 10.1517/14728214.2011.616493. Epub 2011 Sep 9.

Abstract

Introduction: Recently, glucagon-like peptide-1 receptor (GLP-1R) agonists have become available for the treatment of type 2 diabetes. These agents exploit the physiological effects of GLP-1, which is able to address several of the pathophysiological features of type 2 diabetes. GLP-1R agonists presently available are administered once or twice daily, but several once-weekly GLP-1R agonists are in late clinical development.

Areas covered: The present review aims to give an overview of the clinical data on the currently available GLP-1R agonists used for treatment of type 2 diabetes, exenatide and liraglutide, as well as the emerging GLP-1R agonists including the long-acting compounds.

Expert opinion: An emerging therapeutic trend toward initial or early combination therapy with metformin- and incretin-based therapy is anticipated for patients with type 2 diabetes. GLP-1-based therapy has so far proven safe and tolerable. The determination of which incretin-based therapy to choose necessitates comparisons between the various GLP-1R agonists. The available GLP-1R agonists cause sustained weight loss and clinical relevant improvement of glycemic control. The long-acting GLP-1R agonists in late development may improve the effects of GLP-1 even further with optimized pharmacokinetic profiles resulting in fewer side effects. Meta-analyses have shown promising effects on cardiovascular disease and data from ongoing multicenter trials with cardiovascular endpoints are expected in 2015.

Publication types

  • Review

MeSH terms

  • Clinical Trials as Topic
  • Diabetes Mellitus, Type 2 / drug therapy*
  • Diabetes Mellitus, Type 2 / metabolism
  • Drug Design*
  • Drugs, Investigational / administration & dosage
  • Drugs, Investigational / adverse effects
  • Drugs, Investigational / pharmacology
  • Drugs, Investigational / therapeutic use*
  • Exenatide
  • Glucagon-Like Peptide 1 / administration & dosage
  • Glucagon-Like Peptide 1 / adverse effects
  • Glucagon-Like Peptide 1 / analogs & derivatives*
  • Glucagon-Like Peptide 1 / pharmacology
  • Glucagon-Like Peptide 1 / therapeutic use
  • Glucagon-Like Peptide-1 Receptor
  • Humans
  • Hypoglycemic Agents / administration & dosage
  • Hypoglycemic Agents / adverse effects
  • Hypoglycemic Agents / pharmacology
  • Hypoglycemic Agents / therapeutic use*
  • Liraglutide
  • Peptides / administration & dosage
  • Peptides / adverse effects
  • Peptides / pharmacology
  • Peptides / therapeutic use*
  • Receptors, Glucagon / agonists*
  • Treatment Outcome
  • Venoms / administration & dosage
  • Venoms / adverse effects
  • Venoms / pharmacology
  • Venoms / therapeutic use*

Substances

  • Drugs, Investigational
  • GLP1R protein, human
  • Glucagon-Like Peptide-1 Receptor
  • Hypoglycemic Agents
  • Peptides
  • Receptors, Glucagon
  • Venoms
  • Liraglutide
  • Glucagon-Like Peptide 1
  • Exenatide