Absorption, distribution, metabolism and excretion of 14C-Emvododstat following a single oral dose in rats and dogs.
Xenobiotica
; 52(12): 1031-1040, 2022 Dec.
Article
in English
| MEDLINE | ID: covidwho-2242951
ABSTRACT
Emvododstat is a potent inhibitor of dihydroorotate dehydrogenase and is now in clinical development for the treatment of acute myeloid leukaemia and COVID-19.Following an oral dose administration in Long-Evans rats, 14C-emvododstat-derived radioactivity was widely distributed throughout the body, with the highest distribution in the endocrine, fatty, and secretory tissues and the lowest in central nervous system.Following a single oral dose of 14C-emvododstat in rats, 54.7% of the dose was recovered in faeces while less than 0.4% of dose was recovered in urine 7 days post-dose. Emvododstat was the dominant radioactive component in plasma and faeces.Following a single oral dose of 14C-emvododstat in dogs, 75.2% of the dose was recovered in faeces while 0.5% of dose was recovered in urine 8 days post-dose. Emvododstat was the dominant radioactive component in faeces, while emvododstat and its two metabolites (O-desmethyl emvododstat and emvododstat amide bond hydrolysis product) were the major circulating radioactivity in dog plasma.
Keywords
Full text:
Available
Collection:
International databases
Database:
MEDLINE
Main subject:
Body Fluids
/
COVID-19
Type of study:
Prognostic study
Limits:
Animals
Language:
English
Journal:
Xenobiotica
Year:
2022
Document Type:
Article
Affiliation country:
00498254.2023.2171925
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