Peptide reference
Exenatide
Byetta ·Bydureon ·Bydureon BCise ·Exendin-4 ·AC2993
What cited sources report about exenatide
Exenatide is a synthetic 39-amino-acid peptide whose sequence is identical to exendin-4, a salivary peptide originally isolated from the Gila monster (Heloderma suspectum). It shares roughly 53% sequence identity with human GLP-1(7-37) and is resistant to dipeptidyl peptidase-4 (DPP-4) cleavage. Two formulations are marketed in the United States: Byetta (twice-daily immediate-release) and Bydureon / Bydureon BCise (once-weekly microsphere extended-release). Byetta was the first GLP-1 receptor agonist approved by the FDA, on 28 April 2005. Exenatide is approved by the FDA, EMA, Health Canada, and TGA, and has not been nominated to the FDA Pharmacy Compounding Advisory Committee. The summaries below report what individual cited sources state.
FDA Drug Label — Byetta (revised September 2, 2025)
The DailyMed structured product label for Byetta (AstraZeneca) indicates the product as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. The label describes the mechanism as glucose-dependent enhancement of insulin secretion from pancreatic beta cells, suppression of elevated glucagon, and slowed gastric emptying.
BYETTA is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.
Knop, Brønden, and Vilsbøll (2017) — Expert Opinion on Pharmacotherapy
A 2017 review from the Center for Diabetes Research at Gentofte Hospital surveyed pharmacokinetic and clinical data for both the immediate-release (Byetta, twice daily) and extended-release (Bydureon, once weekly) formulations of exenatide. The authors observed that the once-weekly microsphere formulation produced steadier plasma concentrations than the twice-daily injection and reported that both formulations lowered HbA1c and body weight in patients with type 2 diabetes, with gastrointestinal events as the most common adverse-event class.
PubChem CID 45588096 — National Center for Biotechnology Information
The PubChem compound record for exenatide lists molecular formula C184H282N50O60S, consistent with a 39-amino-acid synthetic peptide identical in sequence to exendin-4. PubChem aggregates synonyms (including AC2993) and links to the underlying chemical and patent literature.
DrugBank DB01276 — Exenatide
The DrugBank record describes the molecule, its origin from Heloderma suspectum exendin-4, and the regulatory history of the immediate-release Byetta formulation (FDA approval 28 April 2005 — the first GLP-1 receptor agonist approved in the United States) and the once-weekly extended-release Bydureon and Bydureon BCise products. The record notes that exenatide is renally cleared and is contraindicated in severe renal impairment.
Coverage notes
Exenatide is the prototype GLP-1 receptor agonist and the first FDA-approved drug in the class. The EXSCEL cardiovascular outcomes trial (2017) of once-weekly exenatide reported a neutral primary cardiovascular endpoint, in contrast to the positive results later observed for liraglutide (LEADER), semaglutide (SUSTAIN-6, SELECT), and dulaglutide (REWIND). Exenatide has gradually lost market share to longer-acting once-weekly products with cardiovascular labelling.