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). 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.

Chemistry

The drug is a peptide with amino acid sequence 

YA¹QGTFTSDYSIL²LDKK⁴AQA¹AFIEYLLEGGPSSGAPPPS³

where 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.

References


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