Exenatide

also known as: Byetta, Bydureon, Bydureon BCise, Exendin-4

The first GLP-1 receptor agonist to reach market (2005), available in both twice-daily and weekly extended-release formulations.

A 39-amino-acid peptide with approximately 53% homology to native GLP-1 but resistant to DPP-4 degradation, giving a natural half-life of ~2.4 hours in the immediate-release form.

Mechanism of action

Agonist at the GLP-1 receptor with a natural structural modification (N-terminal histidine-glycine) that confers DPP-4 resistance. Effects mirror other GLP-1 agonists, though the shorter-acting BID formulation produces more pronounced effects on postprandial glucose and gastric emptying but less durable 24-hour glycemic control.

Primary uses

Type 2 diabetes mellitus

Typical dosing

5–10 mcg BID (Byetta) / 2 mg weekly (Bydureon) varies by formulation (subcutaneous)

Byetta injected within 60 min before morning and evening meals. Bydureon BCise is a weekly auto-injector.

Regulatory status

FDA-approved as Byetta (BID, 2005) and Bydureon / Bydureon BCise (weekly, 2012). Manufactured by AstraZeneca. First-in-class GLP-1 agonist.

References

[fda-pi] Byetta (exenatide) Prescribing Information. AstraZeneca.
[fda-pi] Bydureon BCise (exenatide extended-release) Prescribing Information. AstraZeneca.
[clinical-trial] Holman RR, et al. "Effects of Once-Weekly Exenatide on Cardiovascular Outcomes in Type 2 Diabetes (EXSCEL)." N Engl J Med, 2017;377:1228-1239.

Related peptides

Liraglutide

The first once-daily GLP-1 analog to be FDA-approved for both type 2 diabetes (Victoza) and chronic weight management (Saxenda).

Semaglutide

A once-weekly GLP-1 receptor agonist FDA-approved for type 2 diabetes and chronic weight management.

Lixisenatide

A short-acting, prandial GLP-1 agonist primarily used to target postprandial glucose excursions.

Disclaimer

This entry is for educational purposes only and does not constitute medical advice. Dosing information reflects published regulatory or research data and is not a recommendation. Many compounds described here are not approved for human use in the United States. Consult a licensed medical professional before considering any peptide therapy.