Retatrutide – (2381089-83-2)

Retatrutide (LY-3437943) is an experimental drug developed by Eli Lilly for the treatment of obesity. It is a triple agonist targeting the glucagon receptor (GCGR), glucose-dependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R).

In a phase 2 trial, retatrutide demonstrated a mean weight reduction of over 17.5% in adults with obesity or preobesity without diabetes. The drug is a peptide with a specific amino acid sequence and unique chemical modifications, including 2-aminoisobutyric acid, alpha-methyl leucine, and a modified lysine tail.

Retatrutide has shown efficacy in improving glucose tolerance and causing significant body weight loss through glucagon receptor activation. It is currently being investigated in phase 3 clinical trials, with results indicating its potential to outperform existing obesity treatments in terms of total weight loss.

The drug’s safety profile is similar to other GLP-1 and GIP-GLP-1 receptor agonists, with mostly mild to moderate gastrointestinal adverse events reported during dose escalation. Retatrutide’s ability to achieve substantial weight reduction and improve cardiometabolic measures makes it a promising candidate for obesity treatment.

The above information is displayed for information purpose only, and has not been reviewed by EON nor does EON attests or validates the accuracy nor does it constitutes a recommendation or validation.

Retatrutide (LY-3437943) is an experimental drug developed by Eli Lilly for the treatment of obesity. It is a triple agonist targeting the glucagon receptor (GCGR), glucose-dependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R).

In a phase 2 trial, retatrutide demonstrated a mean weight reduction of over 17.5% in adults with obesity or preobesity without diabetes. The drug is a peptide with a specific amino acid sequence and unique chemical modifications, including 2-aminoisobutyric acid, alpha-methyl leucine, and a modified lysine tail.

Retatrutide has shown efficacy in improving glucose tolerance and causing significant body weight loss through glucagon receptor activation. It is currently being investigated in phase 3 clinical trials, with results indicating its potential to outperform existing obesity treatments in terms of total weight loss.

The drug’s safety profile is similar to other GLP-1 and GIP-GLP-1 receptor agonists, with mostly mild to moderate gastrointestinal adverse events reported during dose escalation. Retatrutide’s ability to achieve substantial weight reduction and improve cardiometabolic measures makes it a promising candidate for obesity treatment.

The above information is displayed for information purpose only, and has not been reviewed by EON nor does EON attests or validates the accuracy nor does it constitutes a recommendation or validation.
Sources:
https://en.wikipedia.org/wiki/Retatrutide
https://pubchem.ncbi.nlm.nih.gov/compound/171390338
https://www.medchemexpress.com/retatrutide.html
https://www.nejm.org/doi/full/10.1056/NEJMoa2301972#:~:text=Retatrutide
https://www.sciencedirect.com/science/article/abs/pii/S0014299924007854
https://www.nature.com/articles/s41591-024-03018-2
Other Names

EX-A7826E

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

CAS

2381089-83-2

Molecular Weight

4731

Molecular Formula

C221H342N46O68

SMILES

CC[C@H](C)C(C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC1=CC=C(C=C1)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)NCC(=O)NCC(=O)N2CCC[C@H]2C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N3CCC[C@H]3C(=O)N4CCC[C@H]4C(=O)N5CCC[C@H]5C(=O)N[C@@H](CO)C(=O)N)NC(=O)[C@H](CC6=CC=CC=C6)NC(=O)[C@H](C)NC(=O)C(C)(C)NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](C)NC(=O)[C@H](CCCCNC(=O)COCCOCCNC(=O)CC[C@@H](C(=O)O)NC(=O)CCCCCCCCCCCCCCCCCCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@](C)(CC(C)C)NC(=O)C([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](CC7=CC=C(C=C7)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC8=CC=CC=C8)NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(=O)N)NC(=O)C(C)(C)NC(=O)[C@H](CC9=CC=C(C=C9)O)N

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