Inhibition of P450 activities by bortezomib, major metabolites M1–M4, and known P450 inhibitors in human liver microsomes
IC50 | |||||||
|---|---|---|---|---|---|---|---|
| P450 | 1A2 | 2C9 | 2C19 | 2D6 | 3A4a | 3A4b | |
| Bortezomib | >30 | >30 | 18.0 | >30 | >30 | >30 | |
| M1 | >30 | 11.5 | 10.0 | >30 | >30 | >30 | |
| M2 | >30 | >30 | 13.2 | >30 | >30 | >30 | |
| M3 | >30 | >30 | >30 | >30 | >30 | >30 | |
| M4 | >30 | >30 | >30 | >30 | >30 | >30 | |
| Furafylline | 3.2 | ||||||
| Sulfaphenazole | 0.15 | ||||||
| Omeprazole | 3.3 | ||||||
| Quinidine | 0.09 | ||||||
| Ketoconazole |
|
|
|
| 0.10 | 0.15 | |