Disposition and metabolism of the G protein-coupled receptor 40 agonist TAK-875 (fasiglifam) in rats, dogs, and humans
| Autor: | Tomoaki Higuchi, Yuu Moriya, Liping Pan, Ronald D. Lee, Akifumi Kogame, Masami Nonaka, Yoshihiko Tagawa, Miyako Sudo |
|---|---|
| Rok vydání: | 2018 |
| Předmět: |
Adult
Male Glucuronosyltransferase Health Toxicology and Mutagenesis Metabolite Glucuronidation Administration Oral Pharmacology Toxicology 030226 pharmacology & pharmacy Biochemistry Receptors G-Protein-Coupled Excretion Rats Sprague-Dawley 03 medical and health sciences chemistry.chemical_compound Feces 0302 clinical medicine Dogs Pharmacokinetics Animals Bile Humans Sulfones Benzofurans biology CYP3A4 Dose-Response Relationship Drug Cytochrome P450 General Medicine Middle Aged Radioactivity chemistry Liver 030220 oncology & carcinogenesis biology.protein Metabolome Administration Intravenous Glucuronide Metabolic Networks and Pathways |
| Zdroj: | Xenobiotica; the fate of foreign compounds in biological systems. 49(4) |
| ISSN: | 1366-5928 |
| Popis: | The absorption, distribution, metabolism, and excretion of fasiglifam were investigated in rats, dogs, and humans. The absolute oral bioavailability of fasiglifam was high in all species (>76.0%). After oral administration of [14C]fasiglifam, the administered radioactivity was quantitatively recovered and the major route of excretion of radioactivity was via feces in all species. Fasiglifam was a major component in the plasma and feces in all species. Its oxidative metabolite (M-I) was observed as a minor metabolite in rat and human plasma ( |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|