Exenatide and liraglutide: different approaches to develop GLP-1 receptor agonists (incretin mimetics)--preclinical and clinical results

Best Pract Res Clin Endocrinol Metab. 2009 Aug;23(4):463-77. doi: 10.1016/j.beem.2009.03.008.

Abstract

The GLP-1 analogues exenatide and liraglutide stimulate insulin secretion and inhibit glucagon output in a glucose-dependent manner, slow gastric emptying and decrease appetite. The injectable glucagon-like peptide-1 (GLP-1) receptor agonist exenatide significantly improves glycaemic control, with average reductions in HbA1c of about 1.0% point, fasting plasma glucose of about 1.4 mmol l(-1), and causes a weight loss of approximately 2-3 kg after 30 weeks of treatment. The adverse effects are transient nausea and vomiting. The long-acting once-daily human GLP-1 receptor agonist liraglutide reduces HbA1c by about 1.0-2.0% point, weight by 1-3 kg and seems to have fewer gastrointestinal side effects than exenatide. The final place of the GLP-1 receptor agonists in the diabetes treatment algorithm will be clarified when we have long-term trials with cardiovascular end-points and data illustrating the effects on the progression of type 2 diabetes.

Publication types

  • Review

MeSH terms

  • Anti-Obesity Agents / therapeutic use
  • Clinical Trials as Topic
  • Clinical Trials, Phase II as Topic
  • Delayed-Action Preparations / therapeutic use
  • Diabetes Mellitus, Type 2 / drug therapy*
  • Exenatide
  • Glucagon-Like Peptide 1 / analogs & derivatives*
  • Glucagon-Like Peptide 1 / therapeutic use
  • Glucagon-Like Peptide-1 Receptor
  • Glycated Hemoglobin A / metabolism
  • Humans
  • Liraglutide
  • Peptides / adverse effects
  • Peptides / therapeutic use*
  • Receptors, Glucagon / agonists*
  • Venoms / adverse effects
  • Venoms / therapeutic use*

Substances

  • Anti-Obesity Agents
  • Delayed-Action Preparations
  • GLP1R protein, human
  • Glucagon-Like Peptide-1 Receptor
  • Glycated Hemoglobin A
  • Peptides
  • Receptors, Glucagon
  • Venoms
  • hemoglobin A1c protein, human
  • Liraglutide
  • Glucagon-Like Peptide 1
  • Exenatide