Table 5.
MLN8237 pharmacokinetic parameters for QD dosing
| Dose (mg/m2/dose) | Age (y) | BSA (m2) | Cmax (μmol/L) | Tmax (h) | AUC0–24 (μmol/L·h) | T1/2 (h) | CL/F (mL/min/m2) |
|---|---|---|---|---|---|---|---|
| 30 | 7 | 0.87 | 1.1 | 2.1 | 11.4 | 9 | 67.7 |
| 20 | 1.54 | 2.1 | 3.3 | 22.0 | 6.8 | 32.6 | |
| 6 | 0.84 | 2.4 | 2.0 | 9.2 | 3.1 | 68.9 | |
| Mean | 1.8 | 3 | 14.2 | 6.3 | 56.4 | ||
| SD | 0.7 | 2.5 | 6.9 | 3 | 20.6 | ||
| 40 | 11 | 1.4 | 2.7 | 3.1 | 32.7 | 9 | 30.8 |
| 9 | 1.1 | 2.3 | 3.0 | 33.2 | 8.3 | 31.3 | |
| Mean | 2.5 | 3.1 | 32.9 | 8.6 | 31 | ||
| SD | 0.3 | 0.1 | 0.4 | 0.5 | 0.3 | ||
| 45 | 11 | 1.15 | 8.1 | 1.1 | 80.5 | 6.1 | 16.3 |
| 60 | 15 | 1.52 | 4.2 | 3.1 | 36.5 | 5.5 | 52.3 |
| 14 | 1.62 | 2.2 | 3.1 | 23.9 | 7.1 | 74.5 | |
| 19 | 1.97 | 9.6 | 4.1 | 118 | 8.2 | 14.8 | |
| Mean | 5.3 | 3.4 | 49.5 | 6.9 | 47.2 | ||
| SD | 3.8 | 0.6 | 51.2 | 1.3 | 30.2 | ||
| 80 | 12 | 1.25 | 7.5 | 1.0 | 65.7 | 8.8 | 35.5 |
| 15 | 2.1 | 7.6 | 3.0 | 84.7 | 7.8 | 24.2 | |
| Mean | 7.5 | 2.0 | 75.2 | 8.3 | 29.9 | ||
| SD | 0.1 | 1.4 | 13.5 | 0.7 | 8.0 | ||
| 100 | 9 | 1.5 | 8.2 | 2.0 | 65.3 | 8.1 | 44.4 |
| 13 | 1.2 | 7.8 | 3.2 | 95.2 | 6.4 | 28.6 | |
| Mean | 8.0 | 2.6 | 80.3 | 7.2 | 36.5 | ||
| SD | 0.3 | 0.8 | 21.2 | 1.3 | 11.2 |