Effect of ERY on other CYP450 isoforms
For incubations with diazepam, riluzole, and risperidone, CLint values were derived from the average of two replicates using donor 1307. Tolbutamide CLint values were derived from the average of three replicates each for donors 1307 and ACR. APZ CLint values were derived from the average of two to five replicates each from donors 1307, 3121B, 4202, 4297, and ACR.
Probe Substrate | P450 Responsible for Metabolism | Percent Metabolized by Isoform | Expected Percent Inhibition by 30 µM ERY | Observed Percent Inhibition by 30 µM ERY |
Riluzole | CYP2D6 | >80 | 0 | 7.7 |
Tolbutamide | CYP2C9 | >85 | 0 | 26 |
Diazepam | CYP3A4/CYP2C19 | 60/40 | 60 | 74 |
Risperidone | CYP2D6 | >93 | 7 | 21 |
Alprazolam | CYP3A4 | >90 | 100 | 89 ± 11 |