Peptides›Metabolic›Exenatide

Exenatide

/ Synthetic version of exendin-4 (Gila monster saliva); GLP-1 receptor agonist

TIER 1 · ClinicalN = 0 · TESTING PENDINGLAST REVIEW 2026·04·20

ALIAS · Byetta · Bydureon

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Pass rate

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Research use onlyAny dose figures below describe what specific cited studies used, reported factually. Nothing on this page is guidance for human use.READ FIRST →

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§ A · Identity

Primary sequence— sequence not captured —

MW · —CLASS · Synthetic version of exendin-4 (Gila monster saliva); GLP-1 receptor agonistCATEGORY · Metabolic

FDA-approved for type 2 diabetes (Byetta twice-daily 2005; Bydureon extended-release 2012). First GLP-1 agonist ever approved.

§ B · Mechanism of action

Exenatide is a synthetic version of exendin-4, a peptide originally isolated from the saliva of Heloderma suspectum (Gila monster) that shares ~53% sequence identity with human GLP-1 but is resistant to DPP-4 degradation. Twice-daily Byetta has a ~2.4-hour half-life; the extended-release Bydureon formulation enables once-weekly dosing.

§ C · Human clinical evidence

Extensive. Multiple registrational trials supported approvals for glycemic control in type 2 diabetes. EXSCEL cardiovascular outcomes trial showed non-inferiority but not superiority versus placebo for MACE.

§ D · Primary literature

PubMed28910237Holman RR et al. — Effects of Once-Weekly Exenatide on Cardiovascular Outcomes in Type 2 Diabetes · The New England Journal of Medicine · human-phase-4Once-weekly exenatide did not significantly reduce major adverse cardiovascular events versus placebo in 14,752 patients with T2DM over 3.2 years.Limitations: Pragmatic open-label design; modest placebo separation.2017

PubMed15504997Buse JB et al. — Effects of exenatide (exendin-4) on glycemic control over 30 weeks in sulfonylurea-treated patients with type 2 diabetes · Diabetes Care · human-phase-3-rctExenatide reduced HbA1c by 0.86% and produced weight loss in sulfonylurea-treated T2DM versus placebo over 30 weeks; supported FDA approval.Limitations: 30-week duration; sulfonylurea-only background therapy.2004

§ F · Safety signal

Class GLP-1 profile. Notable for injection-site nodules with the extended-release formulation. Boxed warning for thyroid C-cell tumors. Pancreatitis signal.

§ H · Regulatory status

Regulatory status

FDA status:: FDA-approved
Compounding:: Not eligible for compounding (approved, not in shortage)