Concentrations of fasiglifam and its metabolites in pooled bile over 24 h after a single dose of [14C]fasiglifam
[14C]fasiglifam was administered intraduodenally to rats and orally to dogs. The individual measurements are presented in Supplemental Table 7.
| Dose | Compound | Concentration (n = 2) | Dog/Rat Fold Difference | |
|---|---|---|---|---|
| Rat | Dog | |||
| mg/kg | μg Eq/ml | μg Eq/ml | ||
| 2 | Fasiglifam | 1.80 | 18.2 | 10.1 |
| Fasiglifam-G | 12.4 | 66.6 | 5.4 | |
| Fasiglifam-tau | 4.83 | 7.65 | 1.6 | |
| M-I | <LOQ | <LOQ | NA | |
| 200 | Fasiglifam | 101 | 470 | 4.7 |
| Fasiglifam-G | 433 | 3341 | 7.7 | |
| Fasiglifam-tau | 231 | 16.0 | <1 | |
| M-I | 23.9 | <LOQ | <1 | |
<LOQ, below the lower limit of quantitation; M-I, 2ʹ,6ʹ-dimethyl-4ʹ-[3-(methylsulfonyl)propoxy]biphenyl-3-carboxylic acid; NA, not available.