Table 1

Enzyme kinetic analyses of the formation of 4-hydroxyatomoxetine by human liver microsomes or expressed P450s

SampleKMVmaxCLint (Vmax/KM)
μM pmol/min/mg μl/min/mg
Human Liver Microsomes
 HLC2.3  ± 0.11-a 115  ± 2 50
 HLM2.2  ± 0.1340  ± 6155
 HLK1-b 153  ± 1317  ± 10.1
 HLN1-b 144  ± 937  ± 10.3
Expressed P450s
 CYP1A2399  ± 404.6  ± 1.2 N.D.1-c
 CYP2B629  ± 12.6  ± 0.1N.D.
 CYP2C1996  ± 73.0  ± 0.1N.D.
 CYP2E15.0  ± 0.92.1  ± 0.1N.D.

  • ↵1-a  Parameter estimate ± standard error of the parameter estimate.

  • ↵1-b  Human liver deficient in CYP2D6.

  • ↵1-c  N.D., not determined.