CagriSema (cagrilintide with semaglutide) — pharmacology
Molecular targets, mechanism of action, pharmacokinetics and interactions as characterised in humans.
§2Pharmacology
§2.1Molecular targets
Table 2. Molecular targets recorded for CagriSema (cagrilintide with semaglutide), with the character of the interaction and the potency where the Institute holds it.
| Target | Interaction | Note |
|---|---|---|
| GLP-1 receptor (GLP1R) | Full agonist (semaglutide component) | See semaglutide monograph |
| Amylin and calcitonin receptors | Agonist (cagrilintide component) | See cagrilintide monograph |
§2.2Mechanism of action
The combination pairs two complementary satiation mechanisms: GLP-1 receptor agonism acting on hypothalamic and hindbrain appetite circuits, and amylin receptor agonism acting principally at the area postrema to promote meal termination. Preclinical and early clinical data suggest additive rather than merely overlapping effects on energy intake.[1,2]
§2.3Pharmacokinetics
- Terminal half-life
- ≈7 days for both components
- Time to maximum concentration
- 1–3 days
- Volume of distribution
- as for each component
- Plasma protein binding
- >99 % for both
- Clearance
- as for each component
- Bioavailability
- as for each component
Each component follows its own route; no clinically significant pharmacokinetic interaction between the two has been reported.
§2.4Interactions
- As for each component
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.
- 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
- 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
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.