Table 7.
Mean pharmacokinetic parameters on days 1 and 15 after oral administration of bosutinib 400, 500, and 600 mg
| Dose | Day | Measure | Cmax, ng/mL | Tmax, h* | T1/2, h | AUC, ng·h/mL |
|---|---|---|---|---|---|---|
| 400 mg | 1 | No. | 3 | 3 | 3 | 3 |
| Mean | 77.2 | 3.0 (3-4) | NA | 1487 | ||
| CV% | 76.3 | 17.3 | 109.4 | 72.2 | ||
| 15 | No. | 3 | 3 | 2 | 3 | |
| Mean | 157.3 | 6.0 (6-24) | 22.6 | 2851 | ||
| CV% | 17.6 | 86.6 | 24.4 | 16.6 | ||
| 500 mg | 1 | No. | 3 | 3 | 3 | 3 |
| Mean | 100.9 | 6.0 (6-6) | 22.1 | 2064 | ||
| CV% | 35.3 | 0 | 10.1 | 24.8 | ||
| 15 | No. | 3 | 3 | 2 | 3 | |
| Mean | 200.3 | 6.0 (4-8) | 21.9 | 3660 | ||
| CV% | 6.0 | 33.3 | 27.9 | 11.4 | ||
| 600 mg | 1 | No. | 12 | 12 | 11 | 12 |
| Mean | 119.9 | 4.0 (2-48) | 24.7 | 2074 | ||
| CV% | 33.5 | 159.0 | 54.1 | 20.0 | ||
| 15 | No. | 10 | 10 | 6 | 10 | |
| Mean | 208.2 | 6.0 (3-8) | 27.0 | 3360 | ||
| CV% | 35.2 | 30.4 | 100.8 | 43.5 |
AUC indicates area under the curve; Cmax, maximum concentration; CV%, coefficient of variation; NA, not available; Tmax, time to maximum concentration; and T1/2, elimination half life.
*
For Tmax, median (range) values are shown instead of mean values.