From Venom‐to‐Vial‐to‐Pill: The Translational Journey of GLP‐1 Peptides and the Evolving Landscape of Biopharmaceutics Modeling
Abstract
Glucagon-like peptide-1 receptor agonists (GLP-1RAs) have become an important therapeutic option for metabolic disorders. Their development, from the early identification of exendin-4 in Gila-monster venom to the creation of long-acting analogues and the first oral peptide, marks a significant step in translational drug design. Each generation resolved issues of enzymatic instability, rapid clearance, and low permeability. These gains stemmed from improvements in acylation, fusion-protein engineering, and sodium N-(8-[2-hydroxybenzoyl]amino)caprylate (SNAC)-enabled absorption. This review integrates molecular evolution, formulation advances, and biopharmaceutics modeling, including physiologically based biopharmaceutics modeling (PBBM), to illustrate emerging strategies shaping next-generation oral peptide therapeutics.
Fields of Study & Subjects
Biochemical and Structural Characterization
Advanced Drug Delivery Systems
Monoclonal and Polyclonal Antibodies Research
Publication details
- Journal / source
- Journal of Peptide Science
- Publisher
- Wiley
- Volume
- 32
- Issue
- 4
- Pages
- e70092–e70092
- Publication date
- 1 January 2026
- Language
- EN