TABLE 4.
Summary of prexasertib pharmacokinetics in pediatric patients with recurrent or refractory solid and CNS tumorsa
| Dose Level (mg/m2) | 80 | 100 | 125 | 150 | All Patients |
|---|---|---|---|---|---|
| No. of Patients | 6 | 6 | 5 | 12 | 29 |
| Cmax (ng/ml) | 858 ± 311 | 984 ± 289 | 1227± 212 | 1697 ± 822 | ———— |
| Tmax (hrs) | 1.4 ± 0.9 | 1.1 ± 0.2 | 1.1 ± 0.1 | 1.2 ± 0.5 | 1.2 ± 0.5 |
| T1/2 (hrs) | 7.6 ± 2.3 | 10.0 ± 3.9 | 8.5 ± 4.5 | 9.2 ± 3.5 | 8.9 ± 3.4 |
| AUC0–24h (ng•hr/ml) | 1624 ± 358 | 2011 ± 416 | 2462 ± 545 | 3359 ± 898 | ———— |
| AUC0−∞ (ng•hr/ml) | 1726 ± 387 | 2381 ± 712 | 2638 ± 632 | 3681 ± 1059 | ———— |
| Vss (L/m2) | 245 ± 67 | 332 ± 85 | 292 ± 169 | 257 ± 98 | 276 ± 102 |
| CLp (L/hr/m2) | 48.2 ± 11.5 | 45.1 ± 12.6 | 49.3 ± 10.3 | 44.4 ± 13.5 | 46.1 ± 12.0 |
Abbreviations: AUC= area under the concentration versus time curve; CLp= plasma clearance; Cmax= peak plasma concentration; CNS= central nervous system; hr= hour; No.= number; PK= pharmacokinetic; Tmax= amount of time that a drug is present at the maximum concentration in serum; T1/2= half-life; Vss= volume of distribution at steady state
a
Shown as median (range)