Table 4.
Imatinib plasma pharmacokinetic parameters
| DL | N (d1/d3) | Ima (mg) | Pac (mg/m2) | Cmax d1 (SD) (μg/mL) | Cmax d3 (SD) (μg/mL) | Tmax d1 (SD) (h) | Tmax d3 (SD) (h) | T½ d1 (SD) (h) | T½ d3 (SD) (h) | Cl/F d1 (SD) (L/h) | Cl/F d3 (SD) (L/h) |
|---|---|---|---|---|---|---|---|---|---|---|---|
| 1 | 7/6 | 400 QD | 60 | 3.00 (1.55) | 2.77 (1.18) | 2.6 (1.0) | 4.1 (1.4) | 12.7 (4.1) | 23.8 (14.0) | 8.93 (5.59) | 7.40 (3.33) |
| −1 | 7/7 | 300 QD | 60 | 2.45 (1.61) | 1.84 (1.18) | 2.6 (0.7) | 6.1 (1.5) | 11.7 (2.1) | 18.3 (11.7) | 9.98 (5.40) | 11.2 (5.7) |
| 1A | 3/3 | 400 QD | 60 | 3.76 (2.43) | 3.83 (2.27) | 3.7 (0.6) | 5.7 (2.3) | 14.6 (5.3) | 12.5 (2.1) | 6.24 (2.47) | 8.22 (2.48) |
| 2A | 3/3 | 400 QD | 80 | 3.15 (0.96) | 2.73 (2.01) | 3.7 (0.6) | 3.3 (0.6) | 11.0 (4.4) | 12.9 (4.8) | 8.40 (4.46) | 24.1 (31.3) |
| 3A | 2/3 | 300 BID | 80 | 4.06 (2.50) | 4.91 (2.28) | 2.8 (1.8) | 3.0 (0) | 5.9 (0.1) | 35.4 (32.7) | 8.75 (5.45) | 5.13 (3.34) |
| 4A | 6/3 | 300 BID | 100 | 2.15 (0.83) | 2.24 (0.47) | 2.9 (0.8) | 3.7 (0.6) | 3.5 (16.8) | 22.5 (3.2) | 10.6 (9.30) | 14.7 (4.7) |
| 5A | 8/6 | 400 BID | 100 | 5.15 (2.13) | 6.65 (2.47) | 3.0 (1.0) | 3.7 (0.5) | 10.2 (3.7) | 19.5 (5.8) | 5.72 (2.38) | 9.13 (3.3) |
| P value | (N = 30) | 0.256 | 8.0 E-6 | 1.4 E-6 | 0.136 |
Differences between imatinib parameters on day 1 and day 3 were tested with a two-tailed Wilcoxon exact rank test, whereby a P value <0.05 was considered significant
DL dose level