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.
Drug | Cytosol In Vitro t1/2a | S-9 In Vitro t1/2a | Scaled Cytosol CL′int | Scaled S-9 CL′int |
---|---|---|---|---|
min | min | ml/(min · kg) | ml/(min · kg) | |
O6-Benzylguanine | 33 | 15 | 36 | 47 |
Carbazeran | 3.6 | 1.1 | 323 | 611 |
DACA | 11 | 10 | 111 | 69 |
6-Deoxypenciclovir | 41 | 5.8 | 29 | 122 |
Methotrexate | 480 | 120 | <2.5 | <5.9 |
PF-945863 | 34 | 19 | 35 | 36 |
PF-4217903 | 530 | 119 | 2.2 | 5.9 |
RS-8359 | 165 | 24 | 7.1 | 29 |
XK-469 | 480 | 120 | <2.5 | <5.9 |
Zaleplon | 194 | 93 | 6.1 | 7.6 |
Zoniporide | 31 | 22 | 37 | 32 |
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.