Exenatide
A GLP-1 receptor agonist derived from Gila monster venom (exendin-4).
Identity
- Class
- GLP-1 receptor agonist (exendin-4, 39 aa)
- Source
- Synthetic exendin-4; originally from Gila monster venom
- Receptor
- GLP-1 receptor (GLP-1R)
Key properties
Molecular weight
~4,186.6 Da
Approximate values for the native hormone. Engineered analogs are often deliberately larger and far longer-acting.
Mechanism
Exenatide is the synthetic form of exendin-4, a peptide from Gila monster venom that fully activates GLP-1R but — unlike human GLP-1 — is naturally resistant to DPP-4. That built-in resistance gives a far longer half-life than native GLP-1 without any acylation.
Reference notes
- Exendin-4's natural DPP-4 resistance is the discovery that made long-acting GLP-1 therapy feasible.
- Shares only ~53% identity with human GLP-1 yet fully activates the receptor.
- Available in immediate-release and extended-release (microsphere) formulations.
Selected literature
Curated peer-reviewed reviews, sourced from PubMed. Selected for relevance, not exhaustive — open any entry on PubMed for the full record and its primary citations.
- 1.GLP-1 receptor agonists in the treatment of type 2 diabetes - state-of-the-art · Molecular metabolism, 2021 · PMID 33068776
- 2.Emerging Role of GLP-1 Agonists in Obesity: A Comprehensive Review of Randomised Controlled Trials · International journal of molecular sciences, 2023 · PMID 37445623