Emax in mRNA for CYP3A4, 3A5, 2B6, 2C9, and 2C19 for 21 compounds in cryopreserved human hepatocytes
| Drugs | Fold-Increases in mRNA Level | Ratios | |||||||
|---|---|---|---|---|---|---|---|---|---|
| CYP3A4 | CYP2B6 | CYP2C9 | CYP2C19 | CYP3A5 | 3A4/2B6 | 3A4/2C9 | 3A4/2C19 | 3A4/3A5 | |
| Aprepitant | 16.0 | 1.6 | 1.1 | 1.0 | 2.6 | 10 | 15 | 16 | 6.2 |
| Avasimibe | 5.3 | 2.2 | 1.0 | 1.0 | 3.8 | 2.4 | 5.3 | 5.3 | 1.4 |
| Bosentan | 54 | 7.7 | 1.9 | 1.1 | 1.9 | 7.0 | 29 | 51 | 29 |
| Carbamazepine | 7.6 | 3.5 | 3.1 | 1.4 | 3.5 | 2.2 | 2.4 | 5.5 | 2.2 |
| CITCO | 17 | 3.1 | 2.4 | 1.2 | 1.4 | 5.6 | 7.1 | 14 | 12 |
| Efavirenz | 16 | 2.8 | 1.1 | 1.0 | 1.3 | 5.7 | 15 | 16 | 12 |
| Modafinil | 7.0 | 2.9 | 1.7 | 1.4 | 2.3 | 2.5 | 4.1 | 5.0 | 3.0 |
| Nafcillin | 6.1 | 3.3 | 1.9 | 1.0 | 1.6 | 1.9 | 3.2 | 6.1 | 3.9 |
| Nevirapine | 21 | 3.7 | 2.1 | 1.3 | 3.7 | 5.6 | 9.9 | 16 | 5.6 |
| Nifedipine | 30 | 7.6 | 1.7 | 1.8 | 7.7 | 4.0 | 18 | 17 | 3.9 |
| Oxcarbazepine | 7.9 | 2.9 | 1.5 | 1.0 | 2.0 | 2.7 | 5.3 | 7.9 | 4.0 |
| Phenobarbital | 31 | 23 | 2.8 | 3.5 | 3.9 | 1.3 | 11 | 8.8 | 8.0 |
| Phenytoin | 10 | 5.5 | 5.5 | 4.1 | 4.1 | 1.9 | 7 | 10 | 10 |
| Pioglitazone | 40 | 8.2 | 3.8 | 1.0 | 3.4 | 4.9 | 10 | 40 | 12 |
| Pleconaril | 58 | 3.8 | 2.4 | 1.0 | 4.7 | 15 | 24 | 58 | 13 |
| Rifabutin | 46 | 7.6 | 3.5 | 2.5 | 3.1 | 6.0 | 13 | 18 | 15 |
| Rifampin | 47 | 5.6 | 1.9 | 1.0 | 4.0 | 8.4 | 25 | 47 | 12 |
| Rosiglitazone | 40 | 7.9 | 2.4 | 1.6 | 4.9 | 5.0 | 17 | 25 | 8.2 |
| Sulfinpyrazone | 38 | 5.6 | 2.4 | 1.0 | 3.0 | 6.7 | 16 | 38 | 13 |
| Topiramate | 5.9 | 1.9 | 1.3 | 1.0 | 1.7 | 3.2 | 4.5 | 5.9 | 3.5 |
| Troglitazone | 22 | 15 | 3.8 | 2.2 | 5.0 | 1.5 | 5.8 | 10 | 4.4 |
| Averages | 5.0 | 12 | 20 | 8.6 | |||||
CITCO, 6-(4-chlorophenyl)imidazo[2,1-b][1,3]thiazole-5-carbaldehyde O-(3,4-dichlorobenzyl)oxime.