Table 1

Michaelis-Menten kinetic parameters of sertraline N-demethylation in microsomes of human B-lymphoblastoid cells expressing CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4, the contents of five CYP isoforms in pooled human liver microsomes, and the estimated Vmax/KM of each CYP isoform in human liver microsomes

MicrosomesKMVmaxVmax/KMContents of CYP in Human Liver MicrosomesEstimatedVmax/KM in Human Liver Microsomes
μM pmol/min/pmol CYP μl/min/pmol CYP pmol CYP/mg of protein μl/min/mg of protein
CYP2B630.7  ± 1.21-a 2.04  ± 0.361-a 0.067  ± 0.0121-a 411-b 2.71-c  (14%)1-d
CYP2C930.3  ± 5.31.73  ± 0.280.057  ± 0.006965.5  (29%)
CYP2C199.0  ± 1.71.11  ± 0.220.124  ± 0.016192.4  (13%)
CYP2D62.6  ± 0.30.79  ± 0.050.309  ± 0.022226.8  (35%)
CYP3A445.3  ± 8.50.57  ± 0.060.013  ± 0.0021421.8  (9%)
  • 1-a The values are expressed as the mean ± S.D. from three different experiments.

  • 1-b Provided in data sheets by the manufacturer.

  • 1-c Estimated from theVmax/KM values of cDNA-expressed CYP isoforms and their contents in pooled human liver microsomes.

  • 1-d Numbers in parentheses represent the estimatedVmax/KM as a percentage of the total Vmax/KM values of five CYP isoforms (CYP2B6, CYP2C9, CYP2C19, CYP2D6, and CYP3A4).