TABLE 1

Michaelis-Menten kinetic parameters for BILR 355 metabolism as measured by compound depletion in human liver microsomes (n = 2)

HLM LotTestosterone 6β-Hydroxylase ActivitiesHLM Protein Conc.Apparent KmVmaxCLint, in vitroCLint, in vivoCLhCLh/Qh
nmol · min1 · mg1mg/mlμMpmol · min1 · mg1 HLM proteinml · min1 · mg1 HLM proteinml · min1 · kg1 b.wt.%
10280.720.7346.50.063773.716.278.1
10131.821.1435.00.030735.513.163.2
10084.610.641330.20824019.192.1
10037.90.50.632300.36542219.795.3
Mean ± S.D.0.79 ± 0.24111 ± 910.167 ± 0.153193 ± 17717.0 ± 3.082.2 ± 14.7