Fractional cross-inhibition of P450 enzymes by P450-selective inhibitors in HLMs
Bold values represent the fractional inhibition of enzymes by their corresponding selective inhibitor. Data shown are mean ± S.D. of three independent experiments with each experiment conducted in triplicate.
| Inhibitor | Selective Probe | |||
|---|---|---|---|---|
| 4-OH-DCL | 6β-OH-TES | 4-OH-MEP | DXO | |
| P450 Enzyme | CYP2C9 | CYP3A | CYP2C19 | CYP2D6 |
| Sulfaphenazole (10 μM) | 0.99 ± 0.00 | 0.28 ± 0.12 | 0.02 ± 0.07 | 0.18 ± 0.17 |
| Itraconazole (2 μM) | 0.44 ± 0.12 | 0.98 ± 0.00 | 0.13 ± 0.07 | 0.27 ± 0.18 |
| Omeprazole (30 μM) | 0.75 ± 0.01 | 0.68 ± 0.07 | 0.82 ± 0.07 | 0.27 ± 0.16 |
| Quinidine (1 μM) | 0.13 ± 0.05 | 0.12 ± 0.19 | −0.33 ± 0.26 | 0.90 ± 0.03 |
DXO, dextrorphan; 4-OH-DCL, 4-OH-diclofenac; 4-OH-MEP, 4-OH-mephenytoin; 6β-OH-TES, 6β-OH-testosterone.