TABLE 2

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.

CompoundPercentage of Administered Dose
DogRat
2 mg/kg200 mg/kg2 mg/kg200 mg/kg
Total radioactivity78.2 (100.0)42.0 (100.0)81.4 (100.0)54.1 (100.0)
Fasiglifam10.8 (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-G39.4 (50.4)33.1 (78.8)38.8 (47.7)22.5 (41.6)
Fasiglifam-Tau4.5 (5.8)0.2 (0.5)15.2 (18.7)12.2 (22.6)
Others23.5 (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.