Exenatide
Byetta / Bydureon / Exendin-4 / AC2993
The first GLP-1 receptor agonist approved by the FDA (2005), originally derived from exendin-4 found in Gila monster (Heloderma suspectum) saliva. Available as twice-daily Byetta or once-weekly extended-release Bydureon. A pioneer in the GLP-1 class that paved the way for semaglutide, tirzepatide, and retatrutide. Produces moderate weight loss and HbA1c reduction.
Half-life
2.4 hours (Byetta); ~2 weeks (Bydureon extended-release)
Typical Dose
5–10 mcg BID (Byetta) or 2 mg weekly (Bydureon)
6/10Route
subcutaneous
Category
metabolic
Evidence Overview
Strength of evidence across clinical, expert, and experimental lanes.
How Exenatide is dosed in practice
Usually taken by subcutaneous (SubQ) injection. Typical range: 5–10 mcg BID (Byetta) or 2 mg weekly (Bydureon). Half-life: 2.4 hours (Byetta); ~2 weeks (Bydureon extended-release). Each card gives the dose, frequency and duration from one evidence lane: Clinical (human trials), Expert (practitioner protocols) or Experimental (early or animal data). These ranges describe what has been studied or used; they are not a prescription.
Work out the units to draw with the reconstitution calculator, how long a vial lasts with the vial duration calculator, and how levels fall between doses with the half-life calculator.
First-in-class GLP-1 agonist FDA-approved in 2005. Clinical trials showed HbA1c reduction of 0.8–1.1% and weight loss of 2–4 kg. Bydureon (extended-release microspheres) approved 2012 for once-weekly dosing. EXSCEL cardiovascular outcomes trial showed non-inferiority but not superiority. Largely superseded by semaglutide for new prescriptions.
- FDA prescribing information for Byetta and Bydureon
- EXSCEL cardiovascular outcomes trial
- DeFronzo et al., 2005 — Diabetes Care
Historical significance as the first GLP-1 RA. Still prescribed when newer agents are unavailable or cost-prohibitive. Twice-daily Byetta is inconvenient but some patients prefer the shorter-acting formulation for postprandial glucose control. Bydureon weekly is better tolerated. Less weight loss than semaglutide.
- Diabetes treatment algorithm guidelines
- GLP-1 agonist prescribing experience
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Upgrade to ProSafety & Contraindications
- Personal or family history of medullary thyroid carcinoma
- Severe renal impairment (CrCl < 30 mL/min)
- History of pancreatitis
- Severe GI disease
Exenatide: common questions
What is Exenatide?
The first GLP-1 receptor agonist approved by the FDA (2005), originally derived from exendin-4 found in Gila monster (Heloderma suspectum) saliva. Available as twice-daily Byetta or once-weekly extended-release Bydureon. A pioneer in the GLP-1 class that paved the way for semaglutide, tirzepatide, and retatrutide. Produces moderate weight loss and HbA1c reduction.
How is Exenatide dosed?
Exenatide is usually taken by subcutaneous (SubQ) injection. Typical range in DoseCraft's library: 5–10 mcg BID (Byetta) or 2 mg weekly (Bydureon). Clinical (human trials): 5 mcg BID for 1 month, then 10 mcg BID (Byetta); 2 mg weekly (Bydureon); Twice daily (Byetta) or once weekly (Bydureon); Chronic therapy. Expert (practitioner protocols): 5–10 mcg BID or 2 mg weekly; Twice daily or once weekly; Long-term. These ranges describe what has been studied or used; they are not a prescription.
Is Exenatide FDA-approved?
Yes. Exenatide is an FDA-approved prescription medicine; uses outside its approved indication are off-label.
What is the half-life of Exenatide?
DoseCraft's library lists a half-life of 2.4 hours (Byetta); ~2 weeks (Bydureon extended-release). Half-life sets how often a compound is dosed and how long it takes to clear: about five half-lives.
Who should not use Exenatide?
Listed contraindications: Personal or family history of medullary thyroid carcinoma; Severe renal impairment (CrCl < 30 mL/min); History of pancreatitis; Severe GI disease.
Information is for educational purposes only. Always consult a licensed healthcare provider before starting any peptide regimen.
Page updated . How we grade evidence: methodology.