Effects of PSC on the metabolism of characteristic CYP substrates and potentially coadministered compounds (IC50) in human liver microsomes or in S9 fractions
| Substrate | IC50/Ki | Pathway/Metabolite | Involved CYP |
|---|---|---|---|
| Phenacetin | No effect | O-Deethylation | CYP1A2 |
| Theophylline | No effect | Total | CYP1A2 |
| Paclitaxel | No effect | 6α-Hydroxypaclitaxel | CYP2C8 |
| 2.4 ± 1.1/1.2 μM | p-Hydroxyphenyl-C3′-paclitaxel | CYP3A4 | |
| Tolbutamide | No effect | 4-Hydroxylation | CYP2C9 |
| (S)-Mephenytoin | No effect | 4-Hydroxylation | CYP2C19 |
| Bufuralol | 35% at 20 μM | 1-Hydroxylation | CYP2D6 |
| Dextromethorphan | 20% at 20 μM | O-Demethylation | CYP2D6 |
| Chlorzoxazone | No effect | 6-Hydroxylation | CYP2E1 |
| CSA | 6.5 μM | Hydroxylation | CYP3A |
| N-Demethylation | CYP3A4 | ||
| Doxorubicin | No effect | Doxorubicinol | Aldoketoreductase |
| Doxorubicinol | No effect | 7-Deoxyaglycon | CYP reductase |
| Tropisetron | 22 ± 12% at 20 μM3-a | 5,6,7-Hydroxylation | CYP2D6 |
| Ondansetron | 27 ± 12% at 20 μM3-a | 7,8-Hydroxylation | CYP1A2, CYP2D6, CYP3A4 |
| Glyburide | No effect | Cyclohexylhydroxylation | Unknown |
| 3 μM | Phenylethylhydroxylation | CYP3A | |
| 40% at 5 μM | Unknown | Partially CYP3A |
↵3-a Values represent mean ± range from two livers.