Exenatide

Category: peptide

Aliases: Byetta, Bydureon, Exendin-4, AC2993

Pharmacological Mechanism

Synthetic exendin-4 — 39-residue peptide from Heloderma suspectum (Gila monster) saliva with ~53% homology to mammalian GLP-1. Resists DPP-4 cleavage (Gly at position 2) giving a 2–3 h plasma t½ (vs GLP-1's 1.5 min). Activates GLP-1R → glucose-dependent insulin secretion, glucagon suppression, slowed gastric emptying, central satiety. LAR microspheres release drug over weeks; takes 6–10 weeks to reach steady state.

Half-Life (t½)

SC: 2.4h

Dosing Guidelines

Target Organ Systems