Clinical pharmacology of glucagon-like peptide-1 receptor agonists

Jun 28, 2018Hormones (Athens, Greece)

How drugs that activate the glucagon-like peptide-1 receptor work in the body

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Abstract

Glucagon-like peptide-1 receptor agonists (GLP-1 RAs) significantly reduce haemoglobin A1C (HbA1c) levels in patients with type 2 diabetes mellitus.

GLP-1 RAs mimic the action of natural incretin GLP-1 and have a longer half-life due to resistance to degradation by DPP-4.
They are categorized into short-acting and long-acting formulations based on their duration of action.
Unique characteristics exist among GLP-1 RAs regarding their effectiveness in managing fasting and postprandial blood sugar levels.
Differences among these agents also extend to weight loss effects, cardiovascular protection, and the profile of adverse events.
An individualized, patient-centered approach is essential for effective management of type 2 diabetes, addressing multiple underlying mechanisms.

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Glucagon-like peptide-1 receptor agonists (GLP-1 RAs) are an important asset in the armamentarium for the treatment of type 2 diabetes mellitus (type 2 DM). Incretin failure is a critical etiopathogenetic feature of type 2 DM, which, if reversed, results in improved glycaemic control. GLP-1 RAs are injectable peptides that resemble the structure and function of endogenous incretin GLP-1, but as they are not deactivated by the dipeptidyl peptidase-4 (DPP-4), their half-life is prolonged compared with native GLP-1. Based on their ability to activate GLP-1 receptor, GLP-1 RAs are classified as short-acting (exenatide twice-daily and lixisenatide once-daily), and long-acting (liraglutide once-daily and the once-weekly formulations of exenatide extended-release, dulaglutide, and albiglutide). Semaglutide, another long-acting, once-weekly GLP-1 RA, was recently approved by the FDA and EMA. Although all of these agents potently reduce haemoglobin A1C (HbA1c), there are unique features and fundamental differences among them related to fasting and postprandial hyperglycaemia reduction, weight loss potency, cardiovascular protection efficacy, and adverse events profile. It is imperative that current evidence be integrated and applied in the context of an individualised patient-centred approach. This should include not only glucose management but also targeting as many as possible of the pathophysiologic mechanisms responsible for type 2 DM development and progression.

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Clinical pharmacology of glucagon-like peptide-1 receptor agonists

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