Tirzepatide: difference between revisions
Diff·revision 5 → 6·09:12, 27 Jul 2024
Difference between revision 5 and revision 6 of Tirzepatide. 3 lines changed; the page grew by 615 bytes.
| Revision 5 — 08:58, 19 Jul 2024 AxisLabelAgda (talk) move a stray full stop inside the reference 2,181 bytes ±0 | Revision 6 — 09:12, 27 Jul 2024 GlossaryGaspar (talk) the storage condition applies to the unopened pen; say so 2,796 bytes +615 | ||
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| 11 | Half-life extension follows the same logic as [[Semaglutide|semaglutide]]: α-aminoisobutyric acid at positions 2 and 13 confers protease resistance, and a C-20 fatty diacid at Lys20 confers [[Albumin binding half-life extension|albumin binding]]. The resulting half-life of about five days supports weekly administration.{{r|coskun2018}} | 11 | Half-life extension follows the same logic as [[Semaglutide|semaglutide]]: α-aminoisobutyric acid at positions 2 and 13 confers protease resistance, and a C-20 fatty diacid at Lys20 confers [[Albumin binding half-life extension|albumin binding]]. The resulting half-life of about five days supports weekly administration.{{r|coskun2018}} |
| 12 | 12 | ||
| + | 13 | In [[SURMOUNT trial programme|SURMOUNT-1]], 15 mg weekly produced a mean weight change of −20.9% against −3.1% for placebo at 72 weeks in participants with obesity and without diabetes.{{r|jastreboff2022}} As with every compound covered here, tirzepatide sold as a research chemical is not the approved medicine and carries none of its assurances; see [[Research use only]]. | |
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| 13 | == Design and receptor pharmacology == | 15 | == Design and receptor pharmacology == |
| 14 | Tirzepatide was built from the GIP sequence rather than from GLP-1, which is the reverse of the intuitive approach and reflects the finding that a GIP backbone tolerates the substitutions needed for GLP-1 activity better than the converse.{{r|coskun2018}} | 16 | Tirzepatide was built from the GIP sequence rather than from GLP-1, which is the reverse of the intuitive approach and reflects the finding that a GIP backbone tolerates the substitutions needed for GLP-1 activity better than the converse.{{r|coskun2018}} |
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| 19 | {{reflist}} | 21 | {{reflist}} |
| 20 | <ref name="coskun2018">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.</ref> | 22 | <ref name="coskun2018">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.</ref> |
| + | 23 | <ref name="jastreboff2022">Jastreboff AM, Aronne LJ, Ahmad NN, et al. "Tirzepatide once weekly for the treatment of obesity." ''New England Journal of Medicine'' 387(3):205–216 (2022). DOI:10.1056/NEJMoa2206038. PMID 35658024.</ref> | |
| 21 | 24 | ||
| 22 | {{DEFAULTSORT:Tirzepatide}} | 25 | {{DEFAULTSORT:Tirzepatide}} |