GLP-1 receptor agonists

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GLP-1 receptor agonists are a class of medications approved for the treatment of diabetes mellitus type 2 and obesity. They mimic the action of glucagon-like peptide-1 (GLP-1), a hormone that stimulates insulin secretion, inhibits glucagon release, and promotes satiety. GLP-1 receptor agonists exert their effects by activating GLP-1 receptors on pancreatic beta cells, leading to enhanced insulin secretion and improved blood glucose control. In addition to their glucose-lowering effects, GLP-1 receptor agonists have been shown to promote weight loss and may have cardiovascular benefits.

Approved Medications

• Semaglutide (Trade names: Ozempic for diabetes, Rybelsus for diabetes, Wegovy for obesity) - Manufactured by Novo Nordisk. Approved in 2017 for diabetes and 2021 for obesity.
• Tirzepatide (Dual GLP-1 and GIP agonist; Trade names: Mounjaro for diabetes, Zepbound for obesity) - Manufactured by Eli Lilly. Approved in 2022.
• Liraglutide (Trade names: Victoza for diabetes, Saxenda for obesity) - Manufactured by Novo Nordisk. Approved in 2010 for diabetes and 2014 for obesity.
• Exenatide (Brand names: Byetta, Bydureon) - Manufactured by AstraZeneca. Approved in 2005/2012.
• Albiglutide (Trade name: Tanzeum) - Manufactured by GSK. Approved in 2014.
• Dulaglutide (Trade name: Trulicity) - Manufactured by Eli Lilly. Approved in 2014.
• Lixisenatide (Brand names: Lyxumia in Europe, Adlyxin in the United States) - Manufactured by Sanofi. Approved in 2016.

Mechanism of Action

GLP-1 receptor agonists bind to and activate GLP-1 receptors on pancreatic beta cells, leading to increased insulin secretion in response to elevated blood glucose levels. They also suppress glucagon secretion, which helps reduce hepatic glucose production. Additionally, GLP-1 receptor agonists slow gastric emptying, leading to increased satiety and reduced food intake. These actions result in improved glycemic control and may contribute to weight loss in patients with diabetes and obesity.

Indications

GLP-1 receptor agonists are indicated for the management of diabetes mellitus type 2 in adults who have not achieved adequate glycemic control with diet and exercise alone. They are also approved for the treatment of obesity in conjunction with lifestyle modifications, such as diet and exercise. Some GLP-1 receptor agonists may have additional cardiovascular benefits and are recommended for patients with established cardiovascular disease or those at high risk of cardiovascular events.

Side Effects

Common side effects of GLP-1 receptor agonists include nausea, vomiting, diarrhea, and abdominal discomfort, especially when initiating treatment or titrating the dose. These gastrointestinal symptoms usually improve over time. Other potential side effects include hypoglycemia (especially when used in combination with insulin or sulfonylureas), pancreatitis, and allergic reactions.

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