Estimations of percentage contribution of human cytochrome P450 enzymes to sertraline N-demethylation
Microsomes | CYP2B6 | CYP2C9 | CYP2C19 | CYP2D6 | CYP3A |
|---|---|---|---|---|---|
| From inhibition data | |||||
| HH8 (high CYP3A) | 40 | 10 | 9 | 19 | 22 |
| HH75 (high CYP2B6) | 65 | 10 | 11 | 7 | 8 |
| HH80 (high CYP2D6) | 42 | 7 | 10 | 31 | 10 |
| HH91 (high CYP2C9) | 36 | 26 | 13 | 9 | 16 |
| HH100 (high CYP2C19) | 15 | 19 | 42 | 14 | 10 |
| Average | 40 | 14 | 17 | 16 | 15 |
| Pooled (HL-MIX-101) | 59 | 11 | 15 | 0 | 16 |
| From rP450s using the relative activity factor approach | |||||
| [Sertraline] = 0.5 μM | 36 | 4 | 22 | 16 | 18 |
| [Sertraline] = 50 μM | 16 | 21 | 16 | 5 | 18 |