Mazdutide — pharmacology
Molecular targets, mechanism of action, pharmacokinetics and interactions as characterised in humans.
§2Pharmacology
§2.1Molecular targets
Table 2. Molecular targets recorded for Mazdutide, with the character of the interaction and the potency where the Institute holds it.
| Target | Interaction | Note |
|---|---|---|
| GLP-1 receptor (GLP1R) | Agonist | Dominant arm |
| Glucagon receptor (GCGR) | Agonist | Lower relative potency than the GLP-1 arm |
§2.2Mechanism of action
Mazdutide reproduces the natural dual activity of oxyntomodulin with a pharmacokinetic profile suitable for weekly dosing. The glucagon arm contributes energy expenditure and hepatic lipid mobilisation; the GLP-1 arm supplies appetite suppression and glycaemic control.[1,2]
§2.3Pharmacokinetics
- Terminal half-life
- ≈5–6 days
- Time to maximum concentration
- approximately 24–36 h
- Volume of distribution
- not published
- Plasma protein binding
- high
- Clearance
- not published
- Bioavailability
- not published
Assumed proteolytic with beta-oxidation.
§2.4Interactions
- Not fully characterised
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.
- Ji L, Jiang H, Bi Y, Li X, Ning G, Qu S, Wu Y, Yang J, Chen L, Li L, Zhang M, Qian L. Efficacy and safety of mazdutide in Chinese participants with overweight or obesity: a randomised, double-blind, placebo-controlled phase 2 trial. Diabetes, Obesity and Metabolism 2023;25(12):3691–3700. doi:10.1111/dom.15264
- Müller TD, Finan B, Bloom SR, D’Alessio D, Drucker DJ, Flatt PR, Fritsche A, Gribble F, Grill HJ, Habener JF, Holst JJ, Langhans W, Meier JJ, Nauck MA, Perez-Tilve D, Pocai A, Reimann F, Sandoval DA, Schwartz TW, Seeley RJ. Glucagon-like peptide 1 (GLP-1). Molecular Metabolism 2019;30:72–130. doi:10.1016/j.molmet.2019.09.010 · PMID 31767182
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.