Preclinical pharmacokinetics and biodistribution of the dual adenosine A2A/A2B inhibitor muvadenant (M1069) in rats.

Authors

Jonny Nachtigall, Christine K Maurer, Marc Lecomte, Kai Schiemann, Rinat Zaynagetdinov, Tanja Reuter, Holger Scheible

Published in

Xenobiotica; the fate of foreign compounds in biological systems. Pages 1-15. Sep 02, 2026. Epub Sep 02, 2026.

Abstract

Muvadenant is a selective, dual A2A/A2B adenosine receptor antagonist that demonstrated anti-tumour efficacy in preclinical in vitro and in vivo models.In rats, ¹⁴C-muvadenant related radioactivity was quickly and widely distributed throughout the body with highest exposure observed in metabolic/excretory and melanin containing tissues and the gastrointestinal tract and lowest in the central nervous system.Following single oral administration, 6.27% of the radioactive dose was excreted via urine and 90.3% via faeces with a total recovery of 97.6%. After single intravenous dosing, the amounts of radioactivity excreted via urine and faeces were 13.7% and 80.2%, respectively, with a total recovery of 94.6% within 7 days.Whereas the parent compound accounted for the majority of the circulating radioactivity (>50%), metabolism plays the dominant role in the elimination of muvadenant.Metabolite structures derived from in vivo profiles in rats and in vitro incubations across species revealed extensive phase 1 metabolism of muvadenant with comparable metabolic pathways in human and preclinical species.

PMID:
42686645
Bibliographic data and abstract were imported from PubMed on 03 Sep 2026.

Read full publication at:
Please sign in to see all details.

Stats

1-terrible, 9-excellent. How would you rate this publication? Sign in in to submit your rating.

Post a comment

You need to be signed in to post comments. You can sign in here.

Comments

There are no comments yet.