TABLE 4

The inhibitor concentration to IC50 ratios for the two pairs of ITZ stereoisomers, calculated using peak and trough concentrations of the two enantiomeric pairs after a single dose administration (day 1) of a 100-mg oral solution of itraconazole and after multiple dose administration (100 mg/day) for 7 days



Day 1

Day 7

Cmax/IC50
Cmin/IC50
Cmax/IC50
Cmin/IC50
2R,4S-ITZ 23.4 0.6 130 12.1
2S,4R-ITZ
23.4
2.0
63.9
15.7