TABLE 4

In vitro intrinsic clearance data for drugs in pooled human liver cytosol and S-9 fractions

The cytosol reaction values are an average of n = 4; therefore, an average %CV of 4% was observed.

DrugCytosol In Vitro t1/2aS-9 In Vitro t1/2aScaled Cytosol CL′intScaled S-9 CL′int
minminml/(min · kg)ml/(min · kg)
O6-Benzylguanine33153647
Carbazeran3.61.1323611
DACA111011169
6-Deoxypenciclovir415.829122
Methotrexate480120<2.5<5.9
PF-94586334193536
PF-42179035301192.25.9
RS-8359165247.129
XK-469480120<2.5<5.9
Zaleplon194936.17.6
Zoniporide31223732
  • CV, coefficient of variation.

  • a The S-9 values are an average of n = 2, and, on average, the replicates were within 8.5% of the mean t1/2 value.