Table 1

Average Ki values and inhibition type in human intestine and liver microsomes1-a

InhibitorInhibition TypeKi
Ketoconazole
 LiverNoncompetitive14.9  ± 6.7 nM
 IntestineNoncompetitive17.0  ± 7.9 nM
Fluconazole
 LiverNoncompetitive10.7  ± 4.2 μM
 IntestineNoncompetitive10.4  ± 2.9 μM
  • 1-a n = 3 for each Kidetermination (mean ± S.D.), using microsomes with no detectable CYP3A5.