Tirzepatide: difference between revisions
Diff·revision 2 → 3·20:38, 27 Jun 2024
Difference between revision 2 and revision 3 of Tirzepatide. 6 lines changed; the page grew by 793 bytes.
| Revision 2 — 11:07, 16 Jun 2024 DulaglutideDug (talk) add the excipient list from the labelling 1,388 bytes ±0 | Revision 3 — 20:38, 27 Jun 2024 CategoryBot (talk) bot: repair redlinked category 2,181 bytes +793 | ||
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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 | == 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}} | |
| + | 15 | ||
| + | 16 | Reported potency at the GIP receptor approaches that of native GIP, while potency at the GLP-1 receptor is roughly an order of magnitude below that of native GLP-1. The molecule is therefore not a balanced dual agonist, and the term "GIP-biased" is used in that sense. It also shows signalling bias at the GLP-1 receptor, favouring cAMP accumulation over β-arrestin recruitment; whether this contributes to the clinical effect is unresolved. See [[Receptor bias]]. | |
| + | 17 | ||
| 13 | == References == | 18 | == References == |
| 14 | {{reflist}} | 19 | {{reflist}} |
| ⋮ | ⋮ | ||
| 18 | [[Category:Dual and triple agonists]] | 23 | [[Category:Dual and triple agonists]] |
| 19 | [[Category:Peptide drugs]] | 24 | [[Category:Peptide drugs]] |
| + | 25 | [[Category:Pharmacokinetics]] | |
| 20 | 26 |