TABLE 2

Clinical parameters for CYP3A4/5 inhibitors used in clinical DDI studies: dose, Cmax and fraction unbound

PerpetratorMolecular Weight (g/mol)Dose and RegimenCmax (ยตM)ReferenceFraction Unbound (fu)Reference
Ketoconazole (high-dose)531.431400 mg qd 4 days2.82(Olkkola et al., 1994)0.032(Kuroha et al., 2002)
Clarithromycin (high-dose)747.953500 mg bid 7 days3.12(Calabresi et al., 2004)0.28(Davey, 1991)
Ritonavir (low-dose)720.946100 mg bid 15 days3.50(Reddy et al., 2007)0.02(Lee et al., 2004)
Itraconazole (capsules)705.64100 mg bid 4 days4.34(Jaakkola et al., 2005)0.036(Templeton et al., 2008)
Itraconazole (oral solution)705.64100 mg qd 7 days1.15(Templeton et al., 2008)
Hydroxy-itraconazole721.630.6080.005
Keto-itraconazole719.620.0230.053
N-Desalkyl-itraconazole649.530.0220.0012