TABLE 1

Demographic information and kinetic parameters derived from 4-OH-ATX formation in 21 individual human liver microsomal preparations of varying CYP2D6 genotype and activity score

HLM #CYP2D6 GenotypeActivity ScoreM/FAgeRace§KmVmaxClint
µMpmol/min/mg proteinµl/min/mg protein
H0033*4/*50M44C79.220.00.253
H0486*4/*50F49C59.1*4.64*NA
H0446*4/*410.5M21C5.3530.95.78
H0439*1/*41F78C0.930406437
H0455*1/*41F37C0.945436461
H0028*2/*31F20C1.32251190
H0157*2/*41F50C1.33188141
H0021*1/*41M19C0.737123167
H0025*1/*41F30C1.07131122
H0115*2/*41F48C2.4028.011.7
H0138*2/*41F70C1.3071.755.2
H0153*1/*12F63C1.01352348
H0155*1/*12M46H1.65360218
H0059*1/*22M9C1.33791595
H0485*1/*22M10C1.50479319
H0120*1/*22F57C1.34141105
H0268*1/*12M0C1.81417230
H0493*1/*12F64C1.33289217
H0134*2/*22F61C4.5925255.0
H0099*1/*2x23M6C1.711600936
H0289*1/*2x23F60C1.941220629
Average5.64379262
  • * Clint was not calculated for HLM H0486 because there were not enough points above the limit of quantitation to provide accurate estimates of Km.

  • M = male, F = female

  • § C = Caucasian, H = Hispanic