Retatrutide Explained

Retatrutide (LY-3437943) is an experimental drug for obesity developed by American pharmaceutical company Eli Lilly and Company. It is a triple glucagon hormone receptor agonist (GLP-1, GIP, and GCGR receptors).[1] It has been shown to achieve a more than 17.5% mean weight reduction in adults without diabetes but with obesity or preobesity (overweight) during a phase 2 trial.[2] [3] [4]

Chemistry

The drug is a peptide with amino acid sequence[5] YA¹QGTFTSDYSIL²LDKK⁴AQA¹AFIEYLLEGGPSSGAPPPS³where superscript numbers refer to unique chemical modifications:

  1. "A¹" refers to 2-aminoisobutyric acid (AiB) instead of alanine.
  2. "L²" refers to alpha-methyl added to leucine (MeL, 2-methylleucine).
  3. "S³" refers to addition of an amino group to the C-terminal serine.
  4. "K⁴" refers to a modification group attached to the lysine's tail amine, specifically (AEEA)-gamma-Glu-C20 diacid.

Notes and References

  1. Coskun T, Urva S, Roell WC, Qu H, Loghin C, Moyers JS, O'Farrell LS, Briere DA, Sloop KW, Thomas MK, Pirro V, Wainscott DB, Willard FS, Abernathy M, Morford L, Du Y, Benson C, Gimeno RE, Haupt A, Milicevic Z . 3 . LY3437943, a novel triple glucagon, GIP, and GLP-1 receptor agonist for glycemic control and weight loss: From discovery to clinical proof of concept . . 34 . 9 . 1234–1247.e9 . September 2022 . 35985340 . 10.1016/j.cmet.2022.07.013. free. 251675508 .
  2. Lilly's phase 2 retatrutide results published in The New England Journal of Medicine show the investigational molecule achieved up to 17.5% mean weight reduction at 24 weeks in adults with obesity and overweight . Eli Lilly. investor.lilly.com. 26 June 2023. 3 July 2023.
  3. News: Eli Lilly experimental obesity drug could beat rivals in total weight loss for patients. Annika Kim. Constantino. CNBC.com . 26 June 2023. 3 July 2023.
  4. Jastreboff AM, Kaplan LM, Frías JP, Wu Q, Du Y, Gurbuz S, Coskun T, Haupt A, Milicevic Z, Hartman ML . Triple-Hormone-Receptor Agonist Retatrutide for Obesity - A Phase 2 Trial . . June 2023 . 3. 389 . 6 . 514–526 . 37366315 . 10.1056/NEJMoa2301972. 259260926 . Free access subject to registration.
  5. Web site: Compound Report Card . n.d.. ebi.ac.uk. European Bioinformatics Institute, European Molecular Biology Laboratory. August 5, 2024.

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Retatrutide".

Except where otherwise indicated, Everything.Explained.Today is © Copyright 2009-2024, A B Cryer, All Rights Reserved. Cookie policy.