Retatrutide: difference between revisions
Diff·revision 6 → 7·18:08, 19 Aug 2024
Difference between revision 6 and revision 7 of Retatrutide. 2 lines changed; the page grew by 484 bytes.
| Revision 6 — 09:36, 7 Aug 2024 EscalationEira (talk) reorder the analogues chronologically rather than alphabetically 2,722 bytes +278 | Revision 7 — 18:08, 19 Aug 2024 GMP_Gita (talk) add CAS number, sourced 3,206 bytes +484 | ||
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| 11 | The rationale for adding glucagon-receptor agonism to a dual incretin agonist is that glucagon increases resting energy expenditure and hepatic fatty-acid oxidation. The obvious objection — that glucagon raises blood glucose — is addressed by dosing the GLP-1 component sufficiently to dominate the net glycaemic effect, making the intramolecular potency ratio the central design problem.{{r|jastreboff2023}} | 11 | The rationale for adding glucagon-receptor agonism to a dual incretin agonist is that glucagon increases resting energy expenditure and hepatic fatty-acid oxidation. The obvious objection — that glucagon raises blood glucose — is addressed by dosing the GLP-1 component sufficiently to dominate the net glycaemic effect, making the intramolecular potency ratio the central design problem.{{r|jastreboff2023}} |
| 12 | 12 | ||
| + | 13 | In a 48-week phase 2 trial in adults with obesity and without diabetes, the highest dose studied produced a mean weight change of −24.2% against −2.1% for placebo.{{r|jastreboff2023}} That figure comes from a phase 2 trial and should be read with the caution that phase 2 effect sizes in this field have not always been reproduced at phase 3 scale. Material sold as retatrutide by research-chemical suppliers is an unapproved investigational compound; see [[Research use only]]. | |
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| 13 | == Design == | 15 | == Design == |
| 14 | Retatrutide shares its GIP-derived architecture with [[Tirzepatide|tirzepatide]] and adds substitutions that restore appreciable activity at the glucagon receptor. Because the three receptors are evolutionarily related and their ligands derive from a common precursor family — see [[Proglucagon]] — the sequence space in which all three activities coexist is real but narrow.{{r|coskun2022}} | 16 | Retatrutide shares its GIP-derived architecture with [[Tirzepatide|tirzepatide]] and adds substitutions that restore appreciable activity at the glucagon receptor. Because the three receptors are evolutionarily related and their ligands derive from a common precursor family — see [[Proglucagon]] — the sequence space in which all three activities coexist is real but narrow.{{r|coskun2022}} |