Cagrilintide — pharmacology
Molecular targets, mechanism of action, pharmacokinetics and interactions as characterised in humans.
§2Pharmacology
§2.1Molecular targets
Table 2. Molecular targets recorded for Cagrilintide, with the character of the interaction and the potency where the Institute holds it.
| Target | Interaction | Note |
|---|---|---|
| Amylin receptors (AMY1–AMY3, calcitonin receptor with RAMP co-expression) | Agonist | Non-selective across the amylin receptor family |
| Calcitonin receptor (CTR) | Agonist | Contributes to the pharmacology; relevance to the weight effect is debated |
§2.2Mechanism of action
Amylin is co-secreted with insulin and acts at the area postrema to promote meal-related satiation, and separately reduces gastric emptying and glucagon secretion. Cagrilintide reproduces this signalling with a pharmacokinetic profile permitting weekly administration. The mechanism is complementary rather than redundant to GLP-1 receptor agonism, which is the rationale for the fixed-combination programme with semaglutide.[1,2]
§2.3Pharmacokinetics
- Terminal half-life
- ≈7–8 days
- Time to maximum concentration
- approximately 24–72 h
- Volume of distribution
- not published
- Plasma protein binding
- high
- Clearance
- not published
- Bioavailability
- not published
Assumed proteolytic with beta-oxidation of the lipid chain. Human mass-balance data have not been published.
§2.4Interactions
- Insulin — hypoglycaemia risk
- Concomitant medicines with narrow absorption windows may be affected by delayed gastric emptying
References cited on this page
References are numbered in order of first citation in this document. Each superscript in the text links to its entry below.
- Lau DCW, Erichsen L, Francisco AM, Satylganova A, le Roux CW, McGowan B, Pedersen SD, Pietiläinen KH, Rubino DM, Batterham RL. Once-weekly cagrilintide for weight management in people with overweight and obesity: a multicentre, randomised, double-blind, placebo-controlled and active-controlled, dose-finding phase 2 trial. The Lancet 2021;398(10317):2160–2172. doi:10.1016/S0140-6736(21)01751-7 · PMID 34798060
- Frías JP, Deenadayalan S, Erichsen L, Knop FK, Lingvay I, Macura S, Mathieu C, Pedersen SD, Davies M. Efficacy and safety of co-administered once-weekly cagrilintide 2·4 mg with once-weekly semaglutide 2·4 mg in type 2 diabetes: a multicentre, randomised, double-blind, active-controlled, phase 2 trial. The Lancet 2023;402(10403):720–730. doi:10.1016/S0140-6736(23)01163-7 · PMID 37364591
Identifiers are reproduced only where the Institute holds them. Where a digital object identifier or PubMed identifier is not shown, the Institute has recorded the journal and year and has not constructed an identifier.