IC50 and maximum percent inhibition values for the inhibition of P450 isoforms by imetelstat and positive control inhibitors in pooled cryopreserved human hepatocytes
| Enzyme | Substrate | IC50 | Maximum Inhibition | Positive Control Inhibitor (Concentration) | Positive Control Inhibition |
|---|---|---|---|---|---|
| μM | % | % | |||
| CYP1A2 | Phenacetin | >100 | <10 | α-Naphthoflavone (1 μM) | 90 |
| CYP2B6 | Bupropion | >100 | <10 | Ticlopidine (10 μM) | 84 |
| CYP2C8 | Amodiaquine | >100 | 49 | Montelukast (50 μM) | 88 |
| CYP2C9 | Tolbutamide | >100 | <10 | Sulfaphenazole (5 μM) | 99 |
| CYP2C19 | S-Mephenytoin | >100 | <10 | N-3-Benzylphenobarbital (4 μM) | 96 |
| CYP2D6 | Dextromethorphan | >100 | 14 | Quinidine (5 μM) | 99 |
| CYP2E1 | Chlorzoxazone | >100 | 10 | 4-Methylpyrazole (10 μM) | 92 |
| CYP3A4 | Midazolam | >100 | 18 | Ketoconazole (4 μM) | 98 |