Table VI.
Enzyme | Treatment | IND24
|
IND81
|
||||||
---|---|---|---|---|---|---|---|---|---|
Measured Conc. (μM) | Disappearance
|
CYP? | Measured Conc. (μM) | Disappearance
|
CYP? | ||||
% | % Δa | % | % Δa | ||||||
Irreversible incubation condition | |||||||||
Negative Control | No NADPH/No Inhibitor | 0.622 | 0.899 | 0 | |||||
Maximum Metabolism | NADPH/No Inhibitor | 0.733 | 0 (−18) | 0 | 0.143 | 84 | 0 | ||
CYP1A2 | NADPH + Furafylline | 0.766 | 0 (−23) | 0 | Unlikely | 0.534 | 41 | 43 | Unlikely |
Reversible incubation condition | |||||||||
Negative Control | No NADPH/No Inhibitor | 0.654 | 0 | 0.664 | 0 | ||||
Maximum Metabolism | NADPH/No Inhibitor | 0.655 | 0 | 0 | 0.226 | 66 | 0 | ||
CYP2C9 | NADPH + Sulphaphenazol | 0.566 | 14 | 0 (−14) | Unlikely | 0.238 | 64 | 1.8 | Unlikely |
CYP2C19 | NADPH + N-3-B | 0.537 | 18 | 0 (−18) | Unlikely | 0.283 | 57 | 8.5 | Possible |
CYP2D6 | NADPH + Quinidine | 0.555 | 15 | 0 (−15) | Unlikely | 0.300 | 55 | 11 | Likely |
CYP3A4 | NADPH + Ketoconazole | 0.557 | 15 | 0 (−15) | Unlikely | 0.324 | 51 | 15 | Likely |
The involvement of the CYP considered unlikely for values <5; possible for values 5–10; and likely for values >10