Exenatide
Also known as: Byetta, Bydureon, Bydureon BCise, Exendin-4
The first GLP-1 receptor agonist, a synthetic exendin-4, FDA-approved in 2005 as Byetta for type 2 diabetes. Prescription medication.
Last updated
Mechanism of Action
Exenatide is a synthetic version of exendin-4, a 39-amino-acid peptide first found in Gila monster venom that shares about 53% sequence identity with human GLP-1. It activates the GLP-1 receptor, increasing glucose-dependent insulin secretion, suppressing glucagon, slowing gastric emptying and reducing food intake. Unlike native GLP-1 it resists DPP-4 breakdown; the extended-release form encapsulates it in biodegradable microspheres for weekly dosing.
- Half-life
- ~2.4 hours (immediate-release)
- Administration Routes
- Subcutaneous
- Research Status
- Clinical
Reported Benefits
- Improves glycemic control in type 2 diabetes
- Modest weight reduction
- Cardiovascular safety shown in the EXSCEL trial (once-weekly form)
Potential Side Effects
- Nausea, vomiting and diarrhea
- Injection-site nodules (extended-release)
- Boxed warning (extended-release): thyroid C-cell tumors in rodents
- Pancreatitis and acute kidney injury (warnings)
- Hypoglycemia with sulfonylureas or insulin
Common Dosing
The twice-daily form was labeled at 5 mcg subcutaneously within an hour before morning and evening meals, increasing to 10 mcg after a month; the extended-release form was 2 mg once weekly. Dosing is set and supervised by the prescribing clinician.
The dosing information above is aggregated from research literature and anecdotal community reports for educational purposes only. It is not a recommendation, prescription, or medical advice. Peptides are sold as research chemicals only and are not intended for human use.
Contraindications
- Not recommended in severe kidney impairment or end-stage kidney disease
- History of drug-induced immune thrombocytopenia from exenatide
- Extended-release: personal or family history of medullary thyroid carcinoma or MEN 2
- Serious hypersensitivity
No documented stacking partners for Exenatide yet.
- View
Effects of exenatide (exendin-4) on glycemic control and weight over 30 weeks in metformin-treated patients with type 2 diabetes
2005
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Exenatide once weekly versus twice daily for the treatment of type 2 diabetes: a randomised, open-label, non-inferiority study
2008
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Effects of Once-Weekly Exenatide on Cardiovascular Outcomes in Type 2 Diabetes
2017