Glucagon-like peptide-1 (GLP-1) receptor agonists and their cardiovascular benefits-The role of the GLP-1 receptor

Br J Pharmacol. 2022 Feb;179(4):659-676. doi: 10.1111/bph.15462. Epub 2021 May 6.

Abstract

Cardiovascular outcome trials revealed cardiovascular benefits for type 2 diabetes mellitus patients when treated with long-acting glucagon-like peptide-1 (GLP-1) receptor agonists. In the last decade, major advances were made characterising the physiological effects of GLP-1 and its action on numerous targets including brain, liver, kidney, heart and blood vessels. However, the effects of GLP-1 and receptor agonists, and the GLP-1 receptor on the cardiovascular system have not been fully elucidated. We compare results from cardiovascular outcome trials of GLP-1 receptor agonists and review pleiotropic clinical and preclinical data concerning cardiovascular protection beyond glycaemic control. We address current knowledge on GLP-1 and receptor agonist actions on the heart, vasculature, inflammatory cells and platelets, and discuss evidence for GLP-1 receptor-dependent versus independent effects secondary of GLP-1 metabolites. We conclude that the favourable cardiovascular profile of GLP-1 receptor agonists might expand their therapeutic use for treating cardiovascular disease even in non-diabetic populations. 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 metabolites; cardiovascular outcome trial; cardiovascular protection; diabetes mellitus; glucagon-like peptide-1 receptor.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Cardiovascular Diseases* / prevention & control
  • Cardiovascular System*
  • Diabetes Mellitus, Type 2* / metabolism
  • Glucagon-Like Peptide 1 / metabolism
  • Glucagon-Like Peptide-1 Receptor / agonists
  • Humans
  • Hypoglycemic Agents / pharmacology
  • Hypoglycemic Agents / therapeutic use

Substances

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