Accuracy of extrapolation of P450 contributions using ISEF determined by different methods and substrates
Average Fold Error (rhP450-ISEF Extrapolated/Directly Measured in HLM) | |||
---|---|---|---|
CYP2C9 Contribution (n = 7 Compounds) | CYP2D6 Contribution (n = 7 Compounds) | CYP3A4 Contribution (n = 17 Compounds) | |
ISEF determined using different methods | |||
ISEF-CLint | 1.03 | 1.05 | 1.05 |
VISEF | 1.15 | 1.10 | 1.17 |
CLISEF | 1.96 | 1.03 | 1.16 |
ISEF-CLint determined using different substrates | |||
CYP2C9 | |||
Diclofenac | 1.55 | ||
S-Warfarin | 1.14 | ||
Tolbutamide | 1.11 | ||
CYP2D6 | |||
Bufuralol | 1.19 | ||
Dextromethorphan | 1.08 | ||
CYP3A4 | |||
Midazolam | 1.03 | ||
Testosterone | 1.14 | ||
Nifedipine | 1.24 |