TABLE 3

TDI kinetic parameters generated in human hepatocytes and human liver microsomes

ParametersHuman Hepatocyte: Add MethodHuman Hepatocyte: Dilution MethodHuman Hepatocyte: Add Method (Mean)Human Hepatocyte: Dilution Method (Mean)HLMa (Mean ± S.D.)
Assay 1Assay 2Assay 1Assay 2
Diltiazem
    KI6.66.010.57.46.38.91.53 ± 0.565
    kinact0.01620.02190.02340.02220.0190.02280.024 ± 0.011
    kinact/KI0.00240.00370.00220.0030.00310.00260.016 ± 0.001
Erythromycin
    KI61.358.767.168.660.067.95.33 ± 2.57
    kinact0.08560.07600.08680.07120.0810.0790.061 ± 0.002
    kinact/KI0.00140.00130.00130.00100.00130.00120.013 ± 0.005
Verapamil
    KI2.41.42.22.11.92.13.19 ± 0.251
    kinact0.020.02030.02490.02950.020.02720.076 ± 0.004
    kinact/KI0.00830.01490.01130.01410.01160.01270.024 ± 0.003
TAO
    KI2.73.33.73.23.03.40.440 ± 0.140
    kinact0.2370.2380.3560.3820.2380.3690.078 ± 0.053
    kinact/KI0.0880.0720.0980.1190.07980.10810.205 ± 0.180
  • a Mean values are from at least three assays collected from historical data.