TABLE 2

Emax in CYP3A4 mRNA and testosterone 6β-hydroxylase activity for 15 clinical noninducers in three lots of cryopreserved human hepatocytes from different donors

DrugHu4026RCPHu8020
mRNAActivitymRNAActivitymRNAActivity
Fluconazole (0.1–20 μM)N.A.N.A.1.5<1N.A.N.A.
Leflunomide (0.1–20 μM)N.A.N.A.3.3<1N.A.N.A.
Roxithromycin (10–30 μM)1.7<11.4<1<1<1
Ranitidine (10–30 μM)3.5<11.51.11.51.4
Fluoxetine (5–10uM)2.2<11.1<11.8<1
Acetyl acetic acid (10–30 μM)2.6<1<1<11.71.2
Fluvoxamine (10–30 μM)6.8<16.61.73.81.1
Flumazenil (10–30 μM)1.41.01.31.01.71.2
Nitrendipine (10–30 μM)3.45.342112223
Gatifloxacin (10–30 μM)0.81.01.61.13.11.4
Pioglitazone (1–100 μM)4025205.32015
Nifedipine (1–100 μM)337.6103234616
Rosiglitazone (1–100 μM)5.44.940253926
Omeprazole (1–50 μM)5.21.53.52.15.22.2
Dexamethasone (50–100 μM)1214.2115.39.17.0
  • N.A., not available.