TABLE 2

Prediction of CLint ub in vivo using human hepatocytes for five marketed drugs

CLint values were determined using a media loss incubation via an initial disappearance approach and represent the mean ± S.D. from three individual human hepatocyte preparations. CLint values for estrone-3-sulfate were determined via an appearance into cells approach.


Compound

Mean CLint

CLint ub in vivo
Predicted
Observed
μl/min/106 cells ml/min/kg
Montelukast 360 ± 250 1100 2700a
Prazosin 12 ± 1.2 36 50a
Pravastatin 2.1 ± 1.4 6.6 23b
Atorvastatin 100 ± 19 320 910c
Bosentan 38 ± 6.5 120 340a
Estrone-3-sulfate
80 ± 54
N.A.
N.A.
  • N.A., not applicable.

  • a As reported in Riley et al. (2005).

  • b As reported in Lennernäs (2003) and Schachter (2005).

  • c As reported in Pan et al. (1987).