Novel GLP-1 receptor agonists for diabetes

Expert Opin Investig Drugs. 2012 Jan;21(1):45-57. doi: 10.1517/13543784.2012.638282. Epub 2011 Nov 24.


Introduction: GLP-1 receptor agonists have been shown to be effective in the treatment of type 2 diabetes mellitus (T2DM). Although the first GLP-1 receptor agonist, exenatide, was approved in the mid-2000s, other agents with longer durations of action (that do not require twice-daily dosing) are now being developed. Indeed, liraglutide, a once-daily GLP-1 receptor agonist, was approved in 2010, and more recently, a once-weekly formulation of exenatide was approved in 2011. This review considers the mechanism of action of GLP-1 receptor agonists and considers the various agents in this class.

Areas covered: The importance of GLP-1 itself in glycemic control and the use of GLP-1 receptor agonists in T2DM are discussed. An overview of the clinical development of the five GLP-1 receptor agonists (exenatide, liraglutide, lixisenatide, albiglutide and taspoglutide) since 2005 is provided and their mechanisms of action, efficacy in terms of glycemic control and weight loss, and tolerability are reviewed.

Expert opinion: GLP-1 receptor agonists result in clinically meaningful weight loss in addition to their beneficial effects on glucose homeostasis. These agents provide substantial clinical benefits for patients compared with sulfonylureas or DPP-4 inhibitors and will, therefore, become one of the major therapeutic choices for patients with T2DM.

Publication types

  • Review

MeSH terms

  • Animals
  • Blood Glucose / drug effects
  • Diabetes Mellitus, Type 2 / drug therapy*
  • Diabetes Mellitus, Type 2 / physiopathology
  • Drug Approval
  • Glucagon-Like Peptide-1 Receptor
  • Homeostasis / drug effects
  • Humans
  • Hypoglycemic Agents / adverse effects
  • Hypoglycemic Agents / pharmacology
  • Hypoglycemic Agents / therapeutic use*
  • Receptors, Glucagon / antagonists & inhibitors*


  • Blood Glucose
  • GLP1R protein, human
  • Glucagon-Like Peptide-1 Receptor
  • Hypoglycemic Agents
  • Receptors, Glucagon