TABLE 5

Summary table of Km and Ki values in HLM and rUGT1A4 and physicochemical properties (pKa and clogP)

CompoundHLMrUGTpKaclogP
KmKiKmKi
TriazolesμM
    Alprazolam158N.A.261N.A.2.371.92
    Fluconazole2691N.A.UGT2B7 substrateUGT2B7 substrate2.440.45
    Itraconazole8.4421No dataNo data2.944.99
    Posaconazole27.9aN.A.15.9aN.A.2.754.67
    Voriconazole550N.A.1130N.A.2.721.21
Imidazoles
    Midazolam46b58b64b79b6.033.8
    Tioconazole14.81701242456.664.28
    Ketoconazole23.33267 (n = 2)941 (n = 2)6.884.04
    Econazole302861151926.684.48
    Miconazole3351758.74756.644.97
    Bifonazole847228476.554.69
    Sulconazole144371352906.554.36

  • ↵a Data from Ghosal et al. (2004).

  • ↵b Data from Hyland et al. (2009).