TABLE 5

Comparison of enzyme inactivation kinetic parameters between INF and several clinically important MBI of CYP3A4 using testosterone 6β-hydroxylation as a marker reaction of CYP3A activity

CompoundKIkinactkinact/KIReference
μMmin−1min−1 mM−1
INF3.260.0278.4
Clarithromycin2.250.0417.8Polasek and Miners, 2006
Diltiazem0.50.0120.0Ma et al., 2000
Mibefradil2.30.4173.9Prueksaritanont et al., 1999