Table 2

Effect of CLI on the PK parameters of imatinib and on its binding to plasma proteins

PatientDay 4aDay 5f
Cmaxb (μg/ml)AUCc (μg/ml h)Clssd (liter/h)Vssd (liter)% boundFree imatinibe (μg/ml)Cmax (μg/ml)AUC (μg/ml h)Clss (liter/h)Vss (liter)% boundFree imatinib (μg/ml)
0018.0970.475.6884.799.50.041.7930.2013.25172.698.50.052
0022.9042.709.37185.297.40.06541.0414.3027.97585.393.80.0645
05033.0643.209.26152.399.20.02450.7316.5924.11434.994.60.0394
05027.0897.704.0986.399.50.03541.5720.0020.00519.595.50.0707
05012.4933.3811.98266.899.50.01251.0216.4024.39876.497.60.0245
Mean4.7257.498.08155.199.020.0351.4319.5021.94517.796.00.051
95% CI3.3023.152.7766.61.070.021.025.544.93223.12.410.019
  • a Day 4 refers to PK performed at SS.

  • b Cmax values were obtained from experimental data.

  • c AUCs were calculated by trapezoidal rule.

  • d Clearance (Clss) and the volume of distribution (Vss) were calculated as described in “Patients and Methods.”

  • e The percentage of free imatinib and free imatinib concentrations were experimentally measured by ultrafiltration and HPLC determination.

  • f Day 5 refers to PK performed during CLI infusion, 24 h after the day 4 PK.