Tirzepatide
Tirzepatide
Overview
Tirzepatide is a first-in-class dual GIP/GLP-1 receptor agonist approved by the FDA under the brand name Mounjaro for type 2 diabetes and Zepbound for obesity. It simultaneously activates both glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptors, producing greater weight loss and glycemic control than GLP-1 receptor agonists alone. Phase 3 SURMOUNT trials demonstrated average weight loss of 20-22% of body weight — the greatest ever seen in a pharmaceutical weight management trial — positioning tirzepatide as the most effective approved pharmacological weight loss intervention available.
Compound Data
Molecular Formula
C225H348N48O68
Molecular Weight
4813.00 g/mol
IUPAC Name
20-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(5S)-5-[[(2S)-5-amino-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-methylpentanoyl]amino]-2-methylpropanoyl]amino]-4-methylpentanoyl]amino]-3-carboxypropanoyl]amino]hexanoyl]amino]-3-methylpentanoyl]amino]propanoyl]amino]-5-oxopentanoyl]amino]-6-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[2-[[2-[(2S)-2-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[(2S)-2-[(2S)-2-[(2S)-2-[[(2S)-1-amino-3-hydroxy-1-oxopropan-2-yl]carbamoyl]pyrrolidine-1-carbonyl]pyrrolidine-1-carbonyl]pyrrolidin-1-yl]-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxopropan-2-yl]amino]-6-oxohexyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-20-oxoicosanoic acid
PubChem CID
166567236Where does Tirzepatide sit?
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Mechanism of Action
Tirzepatide is a 39-amino-acid synthetic peptide that acts as an agonist at both GIP receptors and GLP-1 receptors simultaneously. GIP receptor activation in adipose tissue enhances insulin sensitivity and lipid metabolism, while GLP-1 receptor activation provides the incretin, appetite-suppressing, and gastric emptying effects established for that receptor class. The dual agonism appears synergistic — GIP potentiates GLP-1 receptor signaling and adds complementary metabolic effects that single GLP-1 agonists cannot achieve. In the brain, combined GIP and GLP-1 receptor activation produces stronger appetite suppression than either alone. The result is superior weight loss efficacy compared to selective GLP-1 agonists, with comparable or better tolerability.
Dosage Information
Typical Dose
2.5-15 mg weekly
Frequency
Once weekly
Administration
Subcutaneous injection
Notes
Titrated over 20 weeks from 2.5mg to maximum 15mg. Requires medical supervision. Supply shortages have been a significant issue since approval.
Potential Side Effects
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Quick Facts
- Administration
- Subcutaneous injection
- Typical Dose
- 2.5-15 mg weekly
- Frequency
- Once weekly
- References
- 0 curated + 19 from PubMed
- Clinical Trials
- 39 registered
- Evidence Score
- 59.5 / 100