Exenatide
Research profile · How we handle evidence
Exenatide (brand names Byetta, Bydureon) is the synthetic form of exendin-4, a peptide originally isolated from Gila monster (Heloderma suspectum) saliva. It was the first FDA-approved GLP-1 receptor agonist, used as an adjunct to diet and exercise in type 2 diabetes.
Evidence Score
High confidence
Category
Therapeutic area
Standard Dose
Twice daily (Byetta) or weekly (Bydureon)
Half-life
Plasma elimination
Route
Subcutaneous
Safety Tier
Monitor closely
Overview
Exenatide is the original GLP-1 drug that came before liraglutide, semaglutide, and tirzepatide. It's naturally resistant to the enzyme that normally breaks down GLP-1 quickly, which is why a Gila-monster-derived peptide turned into a twice-daily (or once-weekly, extended-release) diabetes medication.
Mechanism of Action
Exenatide is the original GLP-1 drug that came before liraglutide, semaglutide, and tirzepatide. It's naturally resistant to the enzyme that normally breaks down GLP-1 quickly, which is why a Gila-monster-derived peptide turned into a twice-daily (or once-weekly, extended-release) diabetes medication.
Benefits
- Stimulates glucose-dependent insulin secretion
- Suppresses glucagon and slows gastric emptying
- Reduces appetite and supports modest weight loss
- Long clinical track record as the first-in-class GLP-1 agonist
Side Effects
- Nausea and vomiting, most common early in treatment
- Injection-site nodules with the extended-release formulation
- Rare pancreatitis reports
- Not recommended with severe renal impairment
Contraindications
- Personal or family history of medullary thyroid carcinoma (extended-release formulation)
- Severe renal impairment or end-stage renal disease
- History of pancreatitis
- Severe gastrointestinal disease
Structure & Sequence
Verified structure
Exenatide
Sequence illustration backed by PubChem match.
- Amino Acid Sequence
- HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2 (39aa, exendin-4)
- Molecular Weight
- 4,186.6 Da
- Chemical Formula
- C184H282N50O60S
- CAS Number
- 141758-74-9
- InChIKey
- HTQBXNHDCUEHJF-XWLPCZSASA-N
Stack & Route Context
Stacks with
No entries listed.
Administration
Subcutaneous
Research Status
FDA-approved since 2005 (Byetta) and 2012 (Bydureon extended-release), with nearly two decades of post-market human safety data as the first-in-class GLP-1 receptor agonist.
Approval Status
Approved
Sports Legal
Permitted
References
- 1View source
PDB-101: Exenatide (incretin drugs for diabetes mellitus)
2020
This profile summarizes research literature for education only. It is not medical advice, and it does not diagnose, treat, or recommend a dose. Consult a qualified professional before changing a protocol.