GLP-1 Receptor Agonist
A class of therapeutic compounds that activate the glucagon-like peptide-1 receptor, mimicking the effects of the natural hormone GLP-1. These drugs stimulate insulin secretion, suppress appetite, and slow gastric emptying. Approved examples include semaglutide, liraglutide, dulaglutide, exenatide, lixisenatide, and tirzepatide (a dual GLP-1/GIP agonist).
Technical Context
GLP-1 receptor agonists bind to GLP-1 receptors on pancreatic beta cells (stimulating glucose-dependent insulin secretion), alpha cells (suppressing glucagon), brain regions (reducing appetite), and gastrointestinal smooth muscle (slowing gastric emptying). The approved agents differ in structure and dosing: exenatide (Byetta, twice-daily; Bydureon, weekly) is based on exendin-4 from Gila monster venom; liraglutide (Victoza/Saxenda, daily) and semaglutide (Ozempic/Wegovy, weekly; Rybelsus, daily oral) are human GLP-1 analogues with fatty acid modifications; dulaglutide (Trulicity, weekly) is fused to an Fc fragment; lixisenatide (Adlyxin, daily) is exendin-based; tirzepatide (Mounjaro/Zepbound, weekly) is a dual GLP-1/GIP agonist. The class has demonstrated cardiovascular benefits beyond glucose control.