Clinical trials used in the analyses
Total of 23 trials and 18 victim CYP3A4 substrate/perpetrator inducer compound pairs for the set of 15 test inducer compounds. Fup is the fraction unbound in plasma and Fuhep is the fraction unbound in the in vitro hepatocyte model of each of the test inducer compounds.
| Perpetrator | Victim | No. of Trials | Reference (Supplemental Data) | AUC Ratio Observed | Fup | Fuhep |
|---|---|---|---|---|---|---|
| Carbamazepine | Simvastatin | 1 | 1 | 0.26 | 0.25 | 0.52 |
| Nifedipine | Midazolam | 1 | 2 | 1 | 0.05 | 0.90 |
| Phenytoin | Midazolam | 1 | 3 | 0.06 | 0.80 | 0.83 |
| Phenytoin | Quetiapine | 1 | 4 | 0.2 | 0.80 | 0.83 |
| SARA | Midazolam | 1 | 5 | 0.82 | 0.01 | 0.07 |
| SARB | Midazolam | 1 | 6 | 0.73 | 0.08 | 0.89 |
| Pioglitazone | Midazolam | 1 | 7 | 0.74 | 0.01 | 0.80 |
| Pioglitazone | Simvastatin | 1 | 8 | 0.98 | 0.01 | 0.80 |
| Rifampicin | Midazolam | 1 | 9 | 0.08 | 0.25 | 0.42 |
| Rifampicin | Simvastatin | 1 | 10 | 0.1 | 0.25 | 0.42 |
| Rifapentine (4 doses) | Midazolam | 4 | 11 | 0.07; 0.07; 0.07; 0.07 | 0.01 | 0.57 |
| Phenobarbital | Nifedipine | 1 | 12 | 0.39 | 0.50 | 1.00 |
| Troglitazone | Midazolam | 1 | 13 | 0.33 | 0.01 | 0.22 |
| Rosiglitazone | Nifedipine | 1 | 14 | 1 | 0.01 | 0.87 |
| SARC (3 doses) | Midazolam | 3 | 15 | 0.67; 0.57; 0.33 | 0.01 | 0.68 |
| SARD | Midazolam | 1 | 16 | 0.2 | 0.01 | 0.94 |
| Pleconaril | Midazolam | 1 | 17 | 0.65 | 0.01 | 0.13 |
| Aprepitant | Midazolam | 1 | 18 | 0.78 | 0.01 | 0.09 |