TABLE 5

The effect of coincubation with inhibitor and 1-h preincubation with inactivator on CYP3A activities in cryopreserved human hepatocytes Values are mean (S.D.), n = 3 incubations.


Name

Coincubationa

Percentage of Control without Inhibitor

Preincubationb

Percentage of Control without Inhibitor
μM μM
Amprenavir 2.5 100 (3) 1 46 (2)
Diclofenac 50 97 (4) 100 102 (4)
Diltiazem 1 95 (10) 1 75 (4)
Erythromycin 10 97 (10) 10 65 (11)
Raloxifene 5 105 (4) 5 48 (2)
Troleandomycin 2.5 99 (4) 1.5 57 (7)
Ketoconazole
2
19 (1)


  • a Inhibitors were coincubated with midazolam

  • b Hepatocytes were preincubated with inactivators for 1 h before the incubation with midazolam