Tirzepatide

Category: peptide

Aliases: Mounjaro, Zepbound, LY3298176

Pharmacological Mechanism

Synthetic 39-residue dual agonist at GLP-1R + GIP-R. Aib substitutions at positions 2 and 13 block DPP-4; C-20 fatty diacid on Lys-20 binds albumin → ~5-day t½. Biased toward GIP-R cAMP signalling over β-arrestin recruitment. SURMOUNT-1: −20.9% weight loss at 72 weeks (15 mg) — largest weight-loss magnitude of any approved pharmacotherapy at trial time.

Half-Life (t½)

SC: 116h

Dosing Guidelines

Target Organ Systems