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Metabolic

Tirzepatide

Dual Agonist

FDA-approved dual GIP/GLP-1 receptor agonist (Mounjaro/Zepbound). Up to 22.5% weight loss in SURMOUNT-1 trial. Currently the most effective approved anti-obesity medication.

Amino Acids39
Mol. Weight4813.5 Da
Half-Life~5 days
Availability 🔔 By Request
Amino Acid Sequence GIP/GLP-1 dual agonist

What Is Tirzepatide?

Tirzepatide (LY3298176) is a dual GIP/GLP-1 receptor agonist developed by Eli Lilly. FDA-approved as Mounjaro (T2D, 2022) and Zepbound (obesity, 2023). The SURMOUNT-1 trial demonstrated 22.5% body weight reduction at 72 weeks at 15mg — the highest for any approved pharmacological agent at the time.

Key Mechanisms

  • GLP-1R agonism — appetite suppression and gastric emptying delay
  • GIPR agonism — synergistically amplifies GLP-1R-mediated weight loss; adipose tissue effects
  • Metabolic parameter improvement — HbA1c, triglycerides, blood pressure, HDL

Key References

  1. Jastreboff AM et al. “Tirzepatide once weekly for the treatment of obesity.” N Engl J Med, 2022;387:205–216.
  2. Rosenstock J et al. “Efficacy and Safety of a Novel Dual GIP and GLP-1 Receptor Agonist Tirzepatide in T2DM.” Lancet, 2021;398:143–155.
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