GLP-1 receptor agonist: difference between revisions
Diff·revision 11 → 12·18:54, 6 Oct 2024
Difference between revision 11 and revision 12 of GLP-1 receptor agonist. 3 lines changed; the page grew by 584 bytes.
| Revision 11 — 10:42, 20 Sep 2024 CiteBot (talk) bot: add drug-class category 5,536 bytes ±0 | Revision 12 — 18:54, 6 Oct 2024 EndpointEnid (talk) correct the molar mass — source gives the free-base figure, we had the salt 6,120 bytes +584 | ||
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| 38 | [[Albumin binding half-life extension|Albumin binding]] is the dominant approach because it is reversible: the bound fraction acts as a circulating depot from which free drug is released continuously, flattening the peak-to-trough ratio as well as extending exposure. The C-18 diacid used in semaglutide binds albumin more tightly than the C-16 monoacid used in liraglutide, which is the principal reason for the difference in dosing interval.{{r|knudsen2019}} | 38 | [[Albumin binding half-life extension|Albumin binding]] is the dominant approach because it is reversible: the bound fraction acts as a circulating depot from which free drug is released continuously, flattening the peak-to-trough ratio as well as extending exposure. The C-18 diacid used in semaglutide binds albumin more tightly than the C-16 monoacid used in liraglutide, which is the principal reason for the difference in dosing interval.{{r|knudsen2019}} |
| 39 | 39 | ||
| + | 40 | Small-molecule agonists such as [[Orforglipron|orforglipron]] achieve oral bioavailability by abandoning the peptide backbone entirely. They are not subject to proteolysis and do not require an absorption enhancer, but they engage a different portion of the receptor and their efficacy relative to injected peptides remains under evaluation.{{r|frias2023}} | |
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| 40 | == References == | 42 | == References == |
| 41 | {{reflist}} | 43 | {{reflist}} |
| ⋮ | ⋮ | ||
| 44 | <ref name="wilding2021">Wilding JPH, Batterham RL, Calanna S, et al. "Once-weekly semaglutide in adults with overweight or obesity." ''New England Journal of Medicine'' 384(11):989–1002 (2021). DOI:10.1056/NEJMoa2032183. PMID 33567185.</ref> | 46 | <ref name="wilding2021">Wilding JPH, Batterham RL, Calanna S, et al. "Once-weekly semaglutide in adults with overweight or obesity." ''New England Journal of Medicine'' 384(11):989–1002 (2021). DOI:10.1056/NEJMoa2032183. PMID 33567185.</ref> |
| 45 | <ref name="nauck2016">Nauck MA, Meier JJ. "The incretin effect in healthy individuals and those with type 2 diabetes: physiology, pathophysiology, and response to therapeutic interventions." ''The Lancet Diabetes & Endocrinology'' 4(6):525–536 (2016). PMID 26876794.</ref> | 47 | <ref name="nauck2016">Nauck MA, Meier JJ. "The incretin effect in healthy individuals and those with type 2 diabetes: physiology, pathophysiology, and response to therapeutic interventions." ''The Lancet Diabetes & Endocrinology'' 4(6):525–536 (2016). PMID 26876794.</ref> |
| + | 48 | <ref name="frias2023">Frías JP, Hsia S, Eyde S, et al. "Efficacy and safety of oral orforglipron in patients with type 2 diabetes: a phase 2 randomised trial." ''The Lancet'' 402(10400):472–483 (2023). PMID 37369232.</ref> | |
| 46 | 49 | ||
| 47 | {{DEFAULTSORT:GLP-1 receptor agonist}} | 50 | {{DEFAULTSORT:GLP-1 receptor agonist}} |