Metabolic•Dual Agonist

⚖️Tirzepatide

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 acids
39
Mol. weight
4813.5 Da
Half-life
~5 days
Availability
On inquiry
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.

Frequently Asked Questions

Is tirzepatide the same as semaglutide?

No — semaglutide is a single (GLP-1-only) receptor agonist, while tirzepatide is a dual agonist activating both GIP and GLP-1 receptors. The added GIP mechanism underlies tirzepatide's larger weight-loss effect sizes in head-to-head trial data.

What's the difference between Mounjaro and Zepbound?

Both are tirzepatide — the same molecule under different brand names for different approved indications (Mounjaro for type 2 diabetes, Zepbound for chronic weight management), similar to the Ozempic/Wegovy relationship for semaglutide.

How does tirzepatide compare to retatrutide mechanistically?

Tirzepatide combines GIP + GLP-1 agonism; retatrutide adds a third receptor (glucagon, GCGR) on top of that same dual mechanism, which is the basis for retatrutide's investigational higher weight-loss ceiling in Phase 2 data.