Retatrutide
Retatrutide
Overview
Retatrutide is a first-in-class triple agonist targeting GIP GLP-1 and glucagon receptors simultaneously developed by Eli Lilly. Phase 2 trial data published in 2023 showed average weight loss of 24% of body weight at 48 weeks — the highest weight loss ever reported for a pharmacological intervention in a clinical trial. Retatrutide represents the frontier of metabolic peptide therapeutics combining three complementary receptor agonist mechanisms for unprecedented efficacy in obesity treatment.
Mechanism of Action
Retatrutide simultaneously activates three receptors involved in energy metabolism. GLP-1 receptor agonism provides incretin effects appetite suppression and gastric emptying delay. GIP receptor agonism complements GLP-1 signaling in the pancreas and adipose tissue improving insulin sensitivity and lipid metabolism. Glucagon receptor agonism adds a third mechanism — stimulating hepatic fat burning and increasing energy expenditure through thermogenic effects. The glucagon component is particularly important for differentiating retatrutide from dual GIP/GLP-1 agonists like tirzepatide — glucagon receptor activation directly increases metabolic rate and fat oxidation producing weight loss through both reduced intake and increased expenditure. The combination of all three mechanisms produces the remarkable efficacy observed in trials.
Dosage Information
Typical Dose
1-12 mg weekly (Phase 2 trial doses)
Frequency
Once weekly
Administration
Subcutaneous injection
Notes
Currently in Phase 3 clinical trials. Not yet FDA approved. This entry documents the research context for this highly anticipated compound.
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Evidence Score
0.75
Compound Data
Molecular Formula
C221H342N46O68
Molecular Weight
4731.00 g/mol
IUPAC Name
20-[[(1S)-4-[2-[2-[2-[[(5S)-5-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-5-amino-2-[[2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-2-methylpropanoyl]amino]-5-oxopentanoyl]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]-2,4-dimethylpentanoyl]amino]-4-methylpentanoyl]amino]-3-carboxypropanoyl]amino]hexanoyl]amino]-6-[[(2S)-1-[[(2S)-5-amino-1-[[1-[[(2S)-1-[[(2S)-1-[[(3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-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]-4-carboxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxopropan-2-yl]amino]-2-methyl-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-6-oxohexyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-20-oxoicosanoic acid
PubChem CID
171390338Potential Side Effects
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Quick Facts
- Administration
- Subcutaneous injection
- Typical Dose
- 1-12 mg weekly (Phase 2 trial doses)
- Frequency
- Once weekly
- References
- 0 curated + 43 from PubMed
- Clinical Trials
- 32 registered
- Evidence Score
- 0.8 / 100