Mean levels (percentages in parentheses) of fasiglifam and its metabolites in the bile of rats and dogs during 0–24 h following a single dose of [14C]fasiglifam
Each value represents an average of two animals. Numbers in parentheses represent proportions to the total radioactivity (%). The individual measurements are presented in Supplemental Table 5.
| Compound | Percentage of Administered Dose | |||
|---|---|---|---|---|
| Dog | Rat | |||
| 2 mg/kg | 200 mg/kg | 2 mg/kg | 200 mg/kg | |
| Total radioactivity | 78.2 (100.0) | 42.0 (100.0) | 81.4 (100.0) | 54.1 (100.0) |
| Fasiglifam | 10.8 (13.8) | 4.6 (11.0) | 5.7 (7.0) | 5.3 (9.8) |
| M-I | <LOQ (0.0) | <LOQ (0.0) | <LOQ (0.0) | 1.3 (2.4) |
| Fasiglifam-G | 39.4 (50.4) | 33.1 (78.8) | 38.8 (47.7) | 22.5 (41.6) |
| Fasiglifam-Tau | 4.5 (5.8) | 0.2 (0.5) | 15.2 (18.7) | 12.2 (22.6) |
| Others | 23.5 (30.0) | 4.2 (9.7) | 21.9 (26.6) | 13.0 (23.6) |
<LOQ, below the lower limit of quantitation; M-I, 2ʹ,6ʹ-dimethyl-4ʹ-[3-(methylsulfonyl)propoxy]biphenyl-3-carboxylic acid.