Summary of induction data (induction term fromeq. 9) for the compounds tested and the DDI-predicted AUC ratios The values used for [I] in vivo were estimated total systemic plasma concentration.
Precipitant | DDI (Observed) | EC50 | Emax | Predicted AUC′PO/AUCPO (induction) | GFEa |
|---|---|---|---|---|---|
| μM | |||||
| Avasimibe | 0.27 | 3.3 | 14.9 | 0.40 | 1.5 |
| Avasimibe | 0.06 | 3.3 | 14.9 | 0.22 | 3.6 |
| Bosentan | 0.66 | 3.4 | 38.8 | 0.07 | 9.3 |
| Carbamazepine | 0.26 | 56 | 34.3 | 0.09 | 2.9 |
| Ethinyl estradiol | 1.2 | 20 | 69 | 0.97 | 1.2 |
| Fluoxetine | 0.87 | 0.5 | 2.1 | 0.60 | 1.4 |
| Fluoxetine | 1.0 | 0.5 | 2.1 | 0.60 | 1.7 |
| Mibefradil | 8.9 | 4.1 | 6.5 | 0.46 | 19 |
| Mibefradil | 8.4 | 4.1 | 6.5 | 0.46 | 18 |
| Modafinil | 0.42 | 26 | 8.9 | 0.18 | 2.3 |
| Nafcillin | 0.37 | 9.0 | 5.1 | 0.23 | 1.6 |
| Nelfinavir | 6.1 | 0.75 | 23.2 | 0.06 | 106 |
| Nifedipine | 1.0 | 18 | 34.3 | 0.70 | 1.5 |
| Phenobarbital | 0.39 | 159 | 49.1 | 0.10 | 4.1 |
| Phenytoin | 0.06 | 24 | 15.8 | 0.10 | 1.6 |
| Pioglitazone | 0.98 | 2.0 | 7.0 | 0.24 | 4.1 |
| Pleconaril | 0.65 | 16.5 | 51 | 0.17 | 3.9 |
| Rifampin | 0.03 | 1.9 | 14.9 | 0.09 | 3.2 |
| Rifampin | 0.08 | 1.9 | 14.9 | 0.09 | 1.1 |
| Rifampin | 0.12 | 1.9 | 14.9 | 0.09 | 1.3 |
| Rifampin | 0.05 | 1.9 | 14.9 | 0.09 | 1.8 |
| Ritonavir | 27 | 1.0 | 68.5 | 0.02 | 1378 |
| Rosiglitazone | 0.88 | 14 | 23.9 | 0.69 | 1.3 |
| Saquinavir | 5.2 | 0.87 | 34.6 | 0.10 | 52 |
| Troglitazone | 0.62 | 2.0 | 9.8 | 0.16 | 4.0 |
| Troleandomycin | 3.8 | 0.3 | 15.9 | 0.19 | 20 |
| Verapamil | 2.9 | 0.16 | 16.4 | 0.12 | 24 |
| Verapamil | 4.7 | 0.16 | 16.4 | 0.12 | 40 |
| Geometric mean fold error |
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61
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↵ a GFE is the geometric fold error in predicting DDI. Values highlighted in bold are above 2-fold