TABLE 1

Fold-induction of CYP1A2, CYP2B6, CYP2C9, and CYP3A4 for test azole and reference compounds

CompoundsFold-inductionRatio
CYP1A2CYP2B6CYP2C9CYP3A4(3A4/2B6)
Azoles
 Bifonazole11.355.421.126.891.27
 Climbazole4.086.791.6512.131.79
 Clotrimazole4.448.261.8417.052.06
 Econazole8.116.441.355.450.85
 Fenbuconazole3.147.361.967.421.01
 Fluconazole0.971.571.201.591.01
 Hexaconazole3.216.251.856.761.08
 Imazalil6.319.041.669.811.09
 Isoconazole3.308.452.1411.991.42
 Lanoconazole7.9112.351.137.620.62
 Luliconazole9.329.201.375.230.57
 Miconazole6.417.521.7413.901.85
 Metabolite of miconazole1.403.821.022.890.76
 Myclobutanil1.908.061.726.960.86
 Oxiconazole9.296.341.278.121.28
 Propiconazole3.747.002.056.830.98
 Tebuconazole3.495.291.695.991.13
 Tioconazole3.127.751.344.450.57
 Triflumizole3.385.621.205.841.04
 Uniconazole5.5211.222.008.330.74
 Voriconazole1.272.721.263.601.32
 Metabolite of voriconazole1.041.420.921.060.75
Reference compounds
 Rifampicin (10 μM)0.879.782.7932.203.29
 Phenobarbital (750 μM)1.4015.782.8321.561.37
 3-MC (1 μM)16.402.141.290.720.34
 CITCO (1 μM)0.927.431.073.430.46
 Probenecid (10 μM)1.101.711.281.891.11
  • Each fold-induction value represents the mean (n = 3–6; n refers to the number of wells in a single hepatocyte experiment).