Table 2

Ki values for inhibition of (3S)-3-hydroxylation and N-oxidation

Drug/compoundKi
3-OH-QQ-N-OX
μM μM
Ketoconazole0.150.23
Bifonazole0.480.59
Itraconazole0.491.02-a
Fluconazole14.919.82-a
Astemizole5.733.9
Terfenadine10.121.6
Bromocriptine0.81.6
Dihydroergotamine1.21.0
Vinblastine4.75.9
Vincristine24.827.2
Paclitaxel58.52-a 54.82-a
Nitrendipine20.214.12-b
Nifedipine28.22-b 2-c
Felodipine83.82-b 2-c
Erythromycin28.435.2
Triacetyloleandomycin2.32.9
Ciclosporin A2.33.2
Midazolam4.37.2
Gestodene33.473.5
Ethinylestradiol107.6 2-c
Naringenin109.8103.22-b
Nefazodone1.91.9

Values for inhibition by 22 drugs/compounds. Values represent mean of values from three inhibition studies.

  • 2-a Ki value is mean ofKi values from two inhibition studies.

  • 2-b Ki value from one inhibition study.

  • 2-c No inhibition with inhibitor concentrations up to 125 μM.