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Retatrutide-Obesity
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What is retatrutide?
Retatrutide is a novel synthetic molecule, which shows agonist action at the glucose-dependent insulinotropic polypeptide receptor (GIPR), glucagon-like peptide-1 receptor (GLP-1R), and glucagon receptor (GCGR).
Retatrutide Molecular Description
Retatrutide is a novel synthetic molecule, which is an agonist of the
- glucose-dependent insulinotropic polypeptide receptor (GIPR)
- glucagon-like peptide-1 receptor (GLP-1R), and
- glucagon receptor (GCGR).1
Retatrutide is an investigational molecule and is not currently approved in the United States.2
The structure of retatrutide is presented in Retatrutide Structure.
Receptor Activation
Retatrutide shows 8.9-fold greater potency than human GIP at the human GIPR, 2.9-fold less potency than human glucagon at the human GCGR, and 2.5-fold less potency than human GLP-1 at the human GLP-1R. In other words, retatrutide demonstrated potent agonist activity at the human GIPR and balanced activity at the human GCGR and GLP-1R.1
Half-Life
In a phase 1 study in healthy participants (baseline body mass index from 19 to 40 Kg/m2), the mean half-life was approximately 6 days, supporting once-weekly dosing.1
References
The published reference below is available by contacting 1-800-LillyRx (1-800-545-5979).
1Coskun T, Urva S, Roell WC, et al. LY3437943, a novel triple glucagon, GIP, and GLP-1 receptor agonist for glycemic control and weight loss: from discovery to clinical proof of concept. Cell Metab. 2022;34(9):1234-1247. https://doi.org/10.1016/j.cmet.2022.07.013
2Medicines in development. Eli Lilly and Company. Clinical Development Pipeline website. Accessed April 30, 2024. https://www.lilly.com/pipeline
3Data on file, Eli Lilly and Company and/or one of its subsidiaries.
Date of Last Review: March 18, 2024