Glucagon-like peptide-1 (GLP-1) receptor agonist; synthetic exendin-4

Exenatide

Approvedaka Byetta, Bydureon, exendin-4

Exenatide is an approved GLP-1 therapy for type 2 diabetes and was the first drug in its class. It is a synthetic form of exendin-4, a peptide originally identified in the saliva of the Gila monster, that shares partial sequence homology with human GLP-1. Immediate-release (Byetta) and once-weekly extended-release (Bydureon) formulations lower HbA1c and body weight; the EXSCEL cardiovascular outcomes trial found it did not increase cardiovascular risk. In recent years the originator has discontinued supply of some exenatide formulations in certain markets.

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Mechanism

In plain terms, exenatide mimics a gut-hormone-like peptide that lowers blood sugar and reduces appetite. Technically, it is a synthetic exendin-4 that agonizes the GLP-1 receptor while resisting degradation by the enzyme DPP-4, stimulating glucose-dependent insulin secretion, suppressing glucagon, slowing gastric emptying, and promoting satiety. The extended-release formulation encapsulates exenatide in biodegradable microspheres to allow once-weekly dosing.

Regulatory Status by Region

  • United States (FDA)Approved. Byetta (exenatide twice daily) for type 2 diabetes (2005), the first GLP-1 receptor agonist approved, and Bydureon (extended-release, once weekly) (2012).
  • Australia (TGA)Registered on the ARTG for type 2 diabetes, available on prescription.
  • European Union (EMA)Authorized: Byetta (2006) and Bydureon (2011) for type 2 diabetes.
  • WADANot prohibited. GLP-1 receptor agonists are not on the WADA Prohibited List and are not banned substances.

See the full regulatory status matrix

Key Studies

Related Clinical Trials

Latest research

See all recent Exenatide research

Common Questions

What is Exenatide?
Exenatide is a GLP-1 receptor agonist and a synthetic version of exendin-4, marketed as Byetta (twice daily) and Bydureon (extended-release, once weekly) for type 2 diabetes. It was the first GLP-1 receptor agonist approved (FDA 2005) and is EMA-authorized and TGA-registered; its cardiovascular safety was evaluated in the EXSCEL trial. It is a prescription medicine.
Is Exenatide approved for medical use?
Exenatide is approved for one or more medical uses in at least one major jurisdiction. United States (FDA): Approved. Byetta (exenatide twice daily) for type 2 diabetes (2005), the first GLP-1 receptor agonist approved, and Bydureon (extended-release, once weekly) (2012). European Union (EMA): Authorized: Byetta (2006) and Bydureon (2011) for type 2 diabetes. Australia (TGA): Registered on the ARTG for type 2 diabetes, available on prescription.
How does Exenatide work?
In plain terms, exenatide mimics a gut-hormone-like peptide that lowers blood sugar and reduces appetite. Technically, it is a synthetic exendin-4 that agonizes the GLP-1 receptor while resisting degradation by the enzyme DPP-4, stimulating glucose-dependent insulin secretion, suppressing glucagon, slowing gastric emptying, and promoting satiety.
Is Exenatide legal in Australia?
Exenatide in Australia (TGA): Registered on the ARTG for type 2 diabetes, available on prescription.
Is Exenatide banned in sport?
Exenatide under the World Anti-Doping Agency (WADA) code: Not prohibited. GLP-1 receptor agonists are not on the WADA Prohibited List and are not banned substances.