Table 2.
Input parameters for the azole inhibitors used in Simcyp simulations. Values for ka are Simcyp defaults, where CYP3A4 Ki and fup data for fluconazole and ketoconazole were from [1] and itraconazole and hydroxy-itraconazole from [25]
Inhibitor | Ki (CYP3A4) (µm) | fup | ka (h−1) |
---|---|---|---|
Fluconazole | 11.9 | 0.890 | 1.28 |
Ketoconazole | 0.0420 | 0.017 | 1.90 |
Itraconazole | 0.0013 | 0.036 | 0.62 |
Hydroxy-itraconazole | 0.0144 | 0.0045 | – |