TABLE 1

Summary of in vitro parameters for E7766 estimated from the sandwich-cultured human hepatocytes

Test ArticleTarget Conc. (µmol/l)TemperatureTime (min)Uptake CLint,T (µl/min per 106 cells)Efflux CLint,T (µl/min per 106 cells)BEI %
E77660.337°C17.69 ± 0.47
53.83 ± 0.26
103.12 ± 0.26
20Not determined2.05 ± 0.0785.2 ± 1.7
4°C100.13 ± 0.00
1.037°C15.46 ± 0.10
52.70 ± 0.14
101.85 ± 0.13
20Not determined1.42 ± 0.0886.2 ± 0.40
4°C100.14 ± 0.02
10.037°C11.22 ± 0.11
50.47 ± 0.02
100.33 ± 0.01
20Not determined0.15 ± 0.0170.9 ± 1.3
4°C100.58 ± 0.73
d8-TCA537°C1014.2 ± 0.8211.0 ± 1.7472.6 ± 5.8
4°C0.27 ± 0.02
Rosuvastatin1037°C106.22 ± 0.312.23 ± 0.3842.7 ± 5.8
4°C0.21 ± 0.04
  • Efflux CLint,T, intrinsic biliary efflux clearance; uptake CLint,T, intrinsic hepatic uptake clearance. Values represent the mean ± S.D. (n = 3).