GLP's ⏱ Half-life: ~2.4 hours (Byetta); ~2 weeks effective (Bydureon)

Exenatide

Exenatide (Byetta / Bydureon)

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Half-Life
~2.4 hours (Byetta); ~2 weeks effective (Bydureon)
Purity
Pharmaceutical grade
Mol. Weight
4,186.6 Da
Form
Solution (Byetta) or extended-release suspension (Bydureon)

What is Exenatide?

Exenatide was the first GLP-1 receptor agonist approved for clinical use (2005), marking a landmark in incretin-based diabetes therapy. Derived from a compound in Gila monster saliva, it demonstrated that peptides from venomous animals could be adapted into effective medications. Available as Byetta (twice-daily injection) and Bydureon (once-weekly extended-release microsphere injection).

Dosage Information (Research Use)

Byetta: 5mcg SC twice daily for 1 month, then 10mcg twice daily. Bydureon: 2mg SC once weekly. Prescription medication.

Reconstitution & Handling

Byetta: pre-filled pen. Bydureon: requires reconstitution of microsphere suspension before injection.

Half-Life & Pharmacokinetics

~2.4 hours (Byetta); ~2 weeks effective (Bydureon)

Reported Observations in Literature

Nausea (44% — most common, usually subsides within weeks), vomiting (13%), diarrhea (13%), injection site reactions (Bydureon — subcutaneous nodules). Risk of pancreatitis and thyroid C-cell tumors (rodent data). Anti-exenatide antibodies develop in some patients.

Key Research References

  • Eng J. “Exendin peptides.” Mt Sinai J Med. 1992;59:147-9
  • Holman RR et al. “Effects of once-weekly exenatide on cardiovascular outcomes (EXSCEL).” N Engl J Med. 2017;377:1228-1239

How Exenatide Works

Exendin-4 Analog

Exenatide is a synthetic version of exendin-4, a 39-amino acid peptide originally isolated from the saliva of the Gila monster (Heloderma suspectum). It shares 53% sequence homology with human GLP-1 but is resistant to DPP-4 degradation, providing a much longer duration of action than native GLP-1.

Glucose-Dependent Action

Like native GLP-1, exenatide enhances insulin secretion only when blood glucose is elevated, minimizing hypoglycemia risk. It also suppresses inappropriately elevated glucagon secretion, slows gastric emptying, and reduces food intake through central appetite regulation.

Research Applications

🔬 Type 2 diabetes management
🔬 GLP-1 receptor pharmacology
🔬 Incretin-based therapy research

Research Findings

The AC2993 clinical trial program demonstrated HbA1c reductions of 0.8-1.0% with twice-daily exenatide. The extended-release formulation (Bydureon) showed superior HbA1c reduction in the DURATION trial series. The EXSCEL cardiovascular outcomes trial showed non-inferiority but did not achieve superiority for MACE reduction.

Dosage & Administration

Byetta: 5mcg SC twice daily for 1 month, then 10mcg twice daily. Bydureon: 2mg SC once weekly. Prescription medication.

Safety & Side Effects

Nausea (44% — most common, usually subsides within weeks), vomiting (13%), diarrhea (13%), injection site reactions (Bydureon — subcutaneous nodules). Risk of pancreatitis and thyroid C-cell tumors (rodent data). Anti-exenatide antibodies develop in some patients.

Important: All safety information is derived from published research, primarily animal studies. No controlled human clinical trial data exists unless explicitly noted. This compound is sold for research purposes only.

Quick Facts

Sequence HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS
Molecular Weight 4,186.6 Da
Half-Life ~2.4 hours (Byetta); ~2 weeks effective (Bydureon)
Purity Pharmaceutical grade
Form Solution (Byetta) or extended-release suspension (Bydureon)
Storage Refrigerate. Bydureon may be stored at room temperature up to 4 weeks.

Key Research References

  • Eng J. "Exendin peptides." Mt Sinai J Med. 1992;59:147-9
  • Holman RR et al. "Effects of once-weekly exenatide on cardiovascular outcomes (EXSCEL)." N Engl J Med. 2017;377:1228-1239

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