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Tirzepatide (revision 1)

Old revision·12:42, 15 Jun 2024·MolarMassMaeve

This is an old revision of this page, as it stood at 12:42, 15 Jun 2024, saved by MolarMassMaeve 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.
Tirzepatide
INNtirzepatide
ClassDual incretin agonist (GIP/GLP-1)
RouteSubcutaneous, weekly
First approval2022 (type 2 diabetes)
Compound infobox · conventions

Tirzepatide is a 39-residue synthetic peptide that activates both the receptor for Glucose-dependent insulinotropic polypeptide and the GLP-1 receptor, making it the first dual incretin agonist to reach the market. Its backbone is derived from GIP rather than from GLP-1, and it is described in the literature as GIP-biased, with greater potency at the GIP receptor than at the GLP-1 receptor.[1]

Half-life extension follows the same logic as semaglutide: α-aminoisobutyric acid at positions 2 and 13 confers protease resistance, and a C-20 fatty diacid at Lys20 confers albumin binding. The resulting half-life of about five days supports weekly administration.[1]

References

  1. ^ a b Coskun T, Sloop KW, Loghin C, et al. "LY3298176, a novel dual GIP and GLP-1 receptor agonist for the treatment of type 2 diabetes mellitus." Molecular Metabolism 18:3–14 (2018). DOI:10.1016/j.molmet.2018.09.009. PMID 30473097.