Orforglipron: difference between revisions
Diff·revision 5 → 6·07:23, 10 Jan 2025
Difference between revision 5 and revision 6 of Orforglipron. 6 lines changed; the page grew by 434 bytes.
| Revision 5 — 05:46, 2 Jan 2025 DPP4_Dagmar (talk) expand §Reported clinical findings 2,903 bytes +548 | Revision 6 — 07:23, 10 Jan 2025 CategoryBot (talk) bot: expand DOI to full citation 3,337 bytes +434 | ||
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| 5 | | Route = Oral, once daily | 5 | | Route = Oral, once daily |
| 6 | | Status = Phase 3; not approved | 6 | | Status = Phase 3; not approved |
| + | 7 | <!-- Contrast with oral peptide --> | |
| + | 8 | | Bioavailability = Not limited by proteolysis | |
| + | 9 | | Food restriction = None required | |
| + | 10 | | Compare = [[Oral semaglutide]], ≈0.4–1% with fasting conditions | |
| 7 | }} | 11 | }} |
| 8 | 12 | ||
| ⋮ | ⋮ | ||
| 17 | 21 | ||
| 18 | A consequence is species selectivity. The pocket differs between human and rodent receptors sufficiently that activity does not translate, and preclinical work required humanised receptor models — a practical complication of small-molecule work at this target that peptide agonists do not face. | 22 | A consequence is species selectivity. The pocket differs between human and rodent receptors sufficiently that activity does not translate, and preclinical work required humanised receptor models — a practical complication of small-molecule work at this target that peptide agonists do not face. |
| + | 23 | ||
| + | 24 | Signalling profile differs from that of the peptide agonists, with a reported preference for cAMP accumulation over β-arrestin recruitment. Whether that difference has clinical consequences is unknown; see [[Receptor bias]].{{r|kawai2020}} | |
| 19 | 25 | ||
| 20 | == References == | 26 | == References == |