In vitro determined CYP3A4 and CYP2B6 DDI kinetic parameters
| Precipitant | CYP3A4 | CYP2B6 | Ratio Emax CYP3A4/CYP2B6 | Ratio EC50 CYP3A4/CYP2B6 | Ratio Emax/EC50 CYP3A4/CYP2B6 | ||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Ki | KI | kinact | Emax | EC50 | Ki | Emax | EC50 | ||||
| µM | µM | min−1 | µM | µM | µM | ||||||
| Carbamazepine | 100 | NA | NA | 24.7 | 43.3 | 100 | 14.8 | 35.4 | 1.7 | 1.2 | 1.4 |
| Cimetidine | 100 | NA | NA | NA | NA | 100 | NA | NA | NA | NA | NA |
| Efavirenz | 20.6 | NA | NA | 19.6 | 4.59 | 2.7 | 10.8 | 1.62 | 1.8 | 2.8 | 0.64 |
| Ezetimibe | 3.3 | 1.1 | 0.06 | 4.90 | 10.2 | 5.5 | 3.48 | 6.68 | 1.4 | 1.5 | 0.92 |
| Indinavir | 0.4 | NA | NA | 8.30 | 16.5 | 40.0 | 2.29 | 15.2 | 3.6 | 1.1 | 3.3 |
| Itraconazole | 0.10 | NA | NA | NA | NA | 2.00 | NA | NA | NA | NA | NA |
| Nelfinavir | 0.9 | 2.3 | 0.10 | 15 | 1.51 | 6.5 | 4.14 | 1.43 | 3.7 | 1.1 | 3.4 |
| Nevirapine | 100 | NA | NA | 27 | 86.3 | 100 | 12.2 | 35.9 | 2.2 | 2.4 | 0.92 |
| Rifampin | 100 | NA | NA | 38 | 0.66 | 100 | 8.26 | 1.26 | 4.5 | 0.5 | 8.8 |
| Ritonavir | 0.004 | 0.07 | 0.21 | 20 | 1.40 | 2.3 | 5.73 | 0.87 | 3.5 | 1.6 | 2.2 |
| Saquinavir | 1.3 | 7.7 | 0.09 | 12 | 2.82 | 40.0 | 3.04 | 0.63 | 3.9 | 4.5 | 0.88 |
| Teriflunomide | 100 | NA | NA | 4.13 | 10.3 | 100 | 3.03 | 4.97 | 1.4 | 2.1 | 0.66 |
| Phenobarbital | NA | NA | NA | 21.1 | 347 | NA | 13.9 | 347 | 1.5 | 1.0 | 1.5 |
| Phenytoin | NA | NA | NA | 25.1 | 36 | NA | 14.9 | 14.3 | 1.7 | 2.5 | 0.67 |
Ratios of CYP3A4/CYP2B6 are based on the mean values of data generated from various lots. NA, not applicable.