Small-Molecule Oral Versus Injectable Glucagon-Like Peptide-1 (GLP-1) Receptor Agonists: Comparative Efficacy, Safety, and Future Clinical Perspectives - PubMed
6 hours ago
- #oral incretin therapy
- #GLP-1 receptor agonists
- #type 2 diabetes
- GLP-1 receptor agonists (GLP-1RAs) have transformed the management of type 2 diabetes, obesity, and cardiometabolic disease.
- Historically, GLP-1RA therapy relied on injectable peptide agonists, which require parenteral administration.
- Oral GLP-1RAs have emerged via two strategies: oral peptide agonists with absorption enhancers (e.g., oral semaglutide) and small-molecule non-peptide agonists (e.g., orforglipron).
- Recent phase 3 evidence suggests oral small-molecule GLP-1RAs can deliver glycemic and weight benefits approaching injectable standards.
- Challenges include long-term outcome data, optimizing titration for tolerability, and equitable access amid rapid market expansion.