TABLE 3

Emax in mRNA for CYP3A4, 3A5, 2B6, 2C9, and 2C19 for 21 compounds in cryopreserved human hepatocytes

DrugsFold-Increases in mRNA LevelRatios
CYP3A4CYP2B6CYP2C9CYP2C19CYP3A53A4/2B63A4/2C93A4/2C193A4/3A5
Aprepitant16.01.61.11.02.61015166.2
Avasimibe5.32.21.01.03.82.45.35.31.4
Bosentan547.71.91.11.97.0295129
Carbamazepine7.63.53.11.43.52.22.45.52.2
CITCO173.12.41.21.45.67.11412
Efavirenz162.81.11.01.35.7151612
Modafinil7.02.91.71.42.32.54.15.03.0
Nafcillin6.13.31.91.01.61.93.26.13.9
Nevirapine213.72.11.33.75.69.9165.6
Nifedipine307.61.71.87.74.018173.9
Oxcarbazepine7.92.91.51.02.02.75.37.94.0
Phenobarbital31232.83.53.91.3118.88.0
Phenytoin105.55.54.14.11.971010
Pioglitazone408.23.81.03.44.9104012
Pleconaril583.82.41.04.715245813
Rifabutin467.63.52.53.16.0131815
Rifampin475.61.91.04.08.4254712
Rosiglitazone407.92.41.64.95.017258.2
Sulfinpyrazone385.62.41.03.06.7163813
Topiramate5.91.91.31.01.73.24.55.93.5
Troglitazone22153.82.25.01.55.8104.4
Averages5.012208.6
  • CITCO, 6-(4-chlorophenyl)imidazo[2,1-b][1,3]thiazole-5-carbaldehyde O-(3,4-dichlorobenzyl)oxime.