Dual incretin agonist: difference between revisions
Diff·revision 11 → 12·07:03, 30 Nov 2024
Difference between revision 11 and revision 12 of Dual incretin agonist. 8 lines changed; the page grew by 982 bytes.
| Revision 11 — 11:11, 17 Nov 2024 GroupBuyGalen (talk) move the trade-name history out of the lead and into §Regulatory history 3,465 bytes +113 | Revision 12 — 07:03, 30 Nov 2024 IncretinIvo (talk) add the molecular formula to the infobox 4,447 bytes +982 | ||
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| 1 | {{Infobox concept | 1 | {{Infobox concept |
| 2 | | name = Dual incretin agonist | 2 | | name = Dual incretin agonist |
| + | 3 | | subtitle = Drug class | |
| 3 | | image = receptor.svg | 4 | | image = receptor.svg |
| 4 | | caption = One peptide, two class B receptors, one fixed intramolecular potency ratio. | 5 | | caption = One peptide, two class B receptors, one fixed intramolecular potency ratio. |
| ⋮ | ⋮ | ||
| 21 | 22 | ||
| 22 | Reported potency ratios are assay-dependent — cell line, readout, incubation time and receptor expression level all move them — and cross-publication comparison of ratios is unreliable. A ratio quoted without its assay system is not a meaningful number. | 23 | Reported potency ratios are assay-dependent — cell line, readout, incubation time and receptor expression level all move them — and cross-publication comparison of ratios is unreliable. A ratio quoted without its assay system is not a meaningful number. |
| + | 24 | ||
| + | 25 | == Why dual agonism might work == | |
| + | 26 | Three explanations circulate, and they are not mutually exclusive. | |
| + | 27 | ||
| + | 28 | # ''Adipose GIP action''. GIP receptors are expressed on adipocytes, where GIP promotes triglyceride storage. Whether the clinical benefit arises from agonism or from functional antagonism through receptor desensitisation is genuinely disputed, and — awkwardly for the field — GIP-receptor antagonists have also produced weight loss in early studies. | |
| + | 29 | # ''Improved tolerability''. If GIP-receptor agonism in the area postrema reduces nausea, a dual agonist can be escalated to a total exposure that a GLP-1 agonist alone could not reach. On this account the benefit is not a new mechanism but a higher tolerable dose. | |
| + | 30 | # ''Restored beta-cell responsiveness''. Beta-cell responsiveness to GIP is impaired in type 2 diabetes but is partly restored when glycaemia improves, so a dual agonist may create the conditions for its own GIP component to work. | |
| 23 | 31 | ||
| 24 | == References == | 32 | == References == |