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. |