Clinical parameters for CYP3A4/5 inhibitors used in clinical DDI studies: dose, Cmax and fraction unbound
| Perpetrator | Molecular Weight (g/mol) | Dose and Regimen | Cmax (ยตM) | Reference | Fraction Unbound (fu) | Reference |
|---|---|---|---|---|---|---|
| Ketoconazole (high-dose) | 531.431 | 400 mg qd 4 days | 2.82 | (Olkkola et al., 1994) | 0.032 | (Kuroha et al., 2002) |
| Clarithromycin (high-dose) | 747.953 | 500 mg bid 7 days | 3.12 | (Calabresi et al., 2004) | 0.28 | (Davey, 1991) |
| Ritonavir (low-dose) | 720.946 | 100 mg bid 15 days | 3.50 | (Reddy et al., 2007) | 0.02 | (Lee et al., 2004) |
| Itraconazole (capsules) | 705.64 | 100 mg bid 4 days | 4.34 | (Jaakkola et al., 2005) | 0.036 | (Templeton et al., 2008) |
| Itraconazole (oral solution) | 705.64 | 100 mg qd 7 days | 1.15 | (Templeton et al., 2008) | ||
| Hydroxy-itraconazole | 721.63 | 0.608 | 0.005 | |||
| Keto-itraconazole | 719.62 | 0.023 | 0.053 | |||
| N-Desalkyl-itraconazole | 649.53 | 0.022 | 0.0012 |