Amylin receptor agonist (revision 1)
Old revision·09:00, 2 Oct 2024·TimelineTiernan
This is an old revision of this page, as it stood at 09:00, 2 Oct 2024, saved by TimelineTiernan with the summary start article on the compound. It may differ substantially from the current revision, and any error it contains may since have been corrected.
| Amylin receptor agonist | |
|---|---|
| Endogenous ligand | Amylin |
| Receptors | AMY1, AMY2, AMY3 (calcitonin receptor plus RAMP) |
| Design problem | Removing amyloidogenicity from the human sequence |
| Topic infobox · conventions | |
Amylin receptor agonists are engineered analogues of amylin designed to reproduce its actions on gastric emptying, glucagon secretion and food intake without the aggregation behaviour of the native human sequence.[1]
Two generations exist. Pramlintide, approved in 2005 as an adjunct to insulin, substitutes three prolines into the human sequence to disrupt β-sheet formation; its short half-life requires injection at each meal, which limited uptake. Cagrilintide is a long-acting analogue employing acylation for weekly dosing and is under development principally in combination with semaglutide as CagriSema.[2]
References
- ^ Hay DL, Chen S, Lutz TA, Parkes DG, Roth JD. "Amylin: pharmacology, physiology, and clinical potential." Pharmacological Reviews 67(3):564–600 (2015). PMID 26071095.
- ^ Lau DCW, Erichsen L, Francisco AM, et al. "Once-weekly cagrilintide for weight management in people with overweight and obesity: a multicentre, randomised, double-blind, placebo-controlled trial." The Lancet 398(10317):2160–2172 (2021). PMID 34798060.
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