TABLE 2

Data for human hepatocyte incubations conducted in the presence of fetal calf serum corrected for both binding to hepatocytes (fuinc) and fub


Compound

Chemical Class

fub

CLint, ub, in vivo

CLh
Predicted
Observed
Predicted
Observed
ml/min/kg ml/min/kg
Antipyrinea N 0.94 0.23 0.60 0.212 0.55
Bosentana A 0.02 0.67 42.1 0.0134 3.65
Caffeinea N 0.83 0.37 1.40 0.303 1.05
Diazepama N 0.012 3.44 42.78 0.040 0.5
Diltiazema B 0.22 8.45 205.44 1.70 13.35
Felodipineb N 0.004 72.08 6111.11 0.28 11
Lorazepama N 0.094 1.24 16.71 0.12 1.45
Mibefradilb B 0.005 41.3 4888.9 0.20 11
Midazolama N 0.04 25.74 599.04 0.98 10.9
Oxazepama N 0.03 1.52 36.94 0.046 1.05
Propranolola B 0.1 21.67 388.75 1.96 13.2
Theophyllinea N 0.4 0.35 1.55 0.141 0.6
Tolcaponea A 0.0018 6.41 1650.32 0.074 2.65
Warfarinc
A
0.018
0.34
6.02
0.006
0.12
  • A, acid; B, base; N, neutral.

  • a-c Data were obtained from a mean data (see Table 4); b Schneider et al. (1999); c Lave et al. (1997a,b).