TABLE 2

Binding to ∆(2–50)CYP46A1 of the structural analogs of POS and VOR

The order of the azoles reflects the increasing size/length of the varying functionality. The results represent the average of triplicate measurements ± S.D.

DrugKd
μMa
VOR and Its Analogs
 Fluconazole5.2 ± 0.3
 VOR0.22 ± 0.02
 Albaconazole2.0 ± 0.2
 Ravuconazole0.11 ± 0.01b
POS and Its Analogs
 Ketoconazole2.3 ± 0.2
 ItraconazoleNSRc
 POS0.03 ± 0.01
  • a All azoles, except itraconazole and ravuconazole, induced in CYP46A1 a type II spectral response.

  • b Type I spectral response.

  • c NSR, nondetectable spectral response (<0.002 absorbance units).