TABLE 6

Reliability of in vitro systems for metabolic clearance predictions

For each method, in vivo intrinsic clearance values were calculated using the parallel-tube model incorporating the free fraction in blood. In vitro intrinsic clearance values were adjusted for either microsomal or hepatocyte binding using the methods of Gertz and Hallifax.




Recombinant Enzymes

Microsomesa

Hepatocytesa
n 72 41 57
r 2 0.43 0.28 0.40
afe 1.53 2.32 5.21
rmse 1528 3501 3608
% Inside 2-fold error 32 29 18
% Inside 5-fold error
73
66
46