Glucagon-like Peptide-1 Receptor Agonists

Abstract

Glucagon-like peptide-1 (GLP-1) receptor agonists (GLP-1RAs) have been used to treat patients with type 2 diabetes mellitus (T2DM) since exenatide, the first GLP-1RA, was approved in 2005. GLP-1 is a peptide hormone secreted by L cells of the small intestine in response to nutrients. GLP-1 presents a glucose-lowering effect via their insulinotropic action on pancreatic β-cells. In addition to their insulinotropic effect, GLP-1 also has pleiotropic actions associated with clinical benefits. GLP-1RAs are a well-established effective treatment for patients with T2DM. GLP-1RAs have antihyperglycemic effects with a low risk of hypoglycemia and reduce body weight. Additionally, GLP-1RAs have beneficial effects on cardiovascular risk factors, such as blood pressure and lipid levels. Large randomized cardiovascular outcome trials and meta-analyses demonstrated that GLP-1RAs reduce cardiovascular disease in T2DM patients. GLP-1RAs are recommended as part of glucose-lowering regimens in patients with T2DM and established cardiovascular disease, or those at high risk. Renal protective and beneficial effects of GLP-1RAs on nonalcoholic fatty liver disease have also been suggested.