Metabolic responses and benefits of glucagon-like peptide-1 (GLP-1) receptor ligands

Br J Pharmacol. 2022 Feb;179(4):526-541. doi: 10.1111/bph.15485. Epub 2021 May 10.

Abstract

Glucagon-like peptide-1 (GLP-1) is an incretin hormone that has undergone a revolutionary turnaround from discovery to clinically approved therapeutic. Rapid progress in drug design and formulation has led from initial development of short- and long-acting drugs suitable for daily or weekly parenteral administration, respectively, through to the most recent approval of an orally active GLP-1 agent. The current review outlines the biological action profile of GLP-1 including the various beneficial metabolic responses in pancreatic and extra-pancreatic tissues, including the gastrointestinal tract, liver, bone and kidney as well as the reproductive cardiovascular and CNS. We then briefly consider clinically approved GLP-1 receptor ligands and recent advances in this field. Given the sustained evolution in the area of GLP-1 drug development and excellent safety profile, as well as the plethora of metabolic benefits, clinical approval for use in diseases beyond diabetes and obesity is very much conceivable. LINKED ARTICLES: This article is part of a themed issue on GLP1 receptor ligands (BJP 75th Anniversary). To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v179.4/issuetoc.

Keywords: GLP-1; diabetes; incretin; obesity.

Publication types

  • Review

MeSH terms

  • Diabetes Mellitus, Type 2* / drug therapy
  • Glucagon-Like Peptide 1 / metabolism
  • Glucagon-Like Peptide-1 Receptor* / metabolism
  • Heart
  • Humans
  • Hypoglycemic Agents / pharmacology
  • Hypoglycemic Agents / therapeutic use
  • Ligands
  • Obesity / drug therapy

Substances

  • Glucagon-Like Peptide-1 Receptor
  • Hypoglycemic Agents
  • Ligands
  • Glucagon-Like Peptide 1