Absorption, distribution, metabolism and excretion of14C-Emvododstat following a single oral dose in rats and dogs / Jiyuan Ma, Qing Ye, Valerie Northcutt, John Babiak, Ronald Kong
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, 14 C-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 14 C-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 14 C-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.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2022 |
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| Erschienen: |
2022 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:52 |
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| Enthalten in: |
Xenobiotica - 52(2022), 12, Seite 1031-1040 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Ma, Jiyuan [VerfasserIn] |
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| Links: |
FID Access [lizenzpflichtig] |
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| Themen: |
Absorption |
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| Umfang: |
1 Online-Ressource (10 p) |
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| doi: |
10.1080/00498254.2023.2171925 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| 245 | 1 | 0 | |a Absorption, distribution, metabolism and excretion of14C-Emvododstat following a single oral dose in rats and dogs |c Jiyuan Ma, Qing Ye, Valerie Northcutt, John Babiak, Ronald Kong |
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| 520 | |a 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, 14 C-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 14 C-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 14 C-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 | ||
| 653 | |a Emvododstat | ||
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| 653 | |a distribution | ||
| 653 | |a metabolism | ||
| 653 | |a excretion | ||
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| 700 | 1 | |a Kong, Ronald |e verfasserin |4 aut | |
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