Exenatide
/ Synthetic version of exendin-4 (Gila monster saliva); GLP-1 receptor agonistALIAS · Byetta · Bydureon
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FDA-approved for type 2 diabetes (Byetta twice-daily 2005; Bydureon extended-release 2012). First GLP-1 agonist ever approved.
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.
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.
Class GLP-1 profile. Notable for injection-site nodules with the extended-release formulation. Boxed warning for thyroid C-cell tumors. Pancreatitis signal.
Regulatory status
- FDA status:
- FDA-approved
- Compounding:
- Not eligible for compounding (approved, not in shortage)