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Triple agonist (revision 1)

Old revision·07:20, 23 Sep 2024·MazdutideMads

This is an old revision of this page, as it stood at 07:20, 23 Sep 2024, saved by MazdutideMads with the summary start article on the compound. It may differ substantially from the current revision, and any error it contains may since have been corrected.
Triple agonist
Usual receptorsGIP, GLP-1 and glucagon
Leading exampleRetatrutide
Design constraintA fixed three-way potency ratio
Topic infobox · conventions

A triple agonist is a single engineered peptide that activates three receptors of the glucagon-secretin family — conventionally the receptors for GIP, GLP-1 and glucagon. Retatrutide is the most advanced example and is investigational.[1]

The design extends the logic of the dual agonists by one receptor, and multiplies the constraints accordingly: the sequence must retain activity at three targets in a ratio fixed by chemistry, and that ratio must remain appropriate across the whole dose range.[1]

References

  1. ^ a b Coskun T, Urva S, Roell WC, et al. "LY3437943, a novel triple glucagon, GIP, and GLP-1 receptor agonist." Cell Metabolism 34(9):1234–1247 (2022). PMID 35985340.