Table 5.
Plasma pharmacokinetic parameters
| Cmax (μM) | Tmax (h) | AUCINF (μM·h) | T1/2 (h) | Cl (L/h) | V (L) | |
|---|---|---|---|---|---|---|
| Belinostat | ||||||
| 800 mg/m2 | 124.8 ± 30.9 (6) | 0.4 (0.4–0.4; 6) | 66.7 ± 11.5 (6) | 0.77 ± 0.43 (6) | 38.6 ± 6.5 | 14.5 ± 5.1 |
| 1000 mg/m2 | 157.0 ± 36.9 (4) | 0.4 (0.4–0.4; 4) | 77.9, 81.7 (2) | 0.7, 1.89 (2) | 39.4 ± 1.3 | 13.9 ± 0.3 |
| Belinostat glucuronide | ||||||
| 800 mg/m2 | 148.9 ± 46.7 (6) | 0.8 (0.4–0.8; 6) | 396.0 ± 151.1 (6) | 3.51 ± 0.95 (6) | NR | NR |
| 1000 mg/m2 | 126.4 ± 24.5 (5) | 0.8 (0.8–1.0; 5) | 668.6 ± 452.2 (4) | 4.41 ± 1.30 (4) | NR | NR |
| Cmax (nM) | Tmax (h) | AUCINF (nM·h) | T1/2 (h) | Cl/F (L/h) | V/F (L) | |
| Adavosertib | ||||||
| 225 mg | 652 ± 221 (10) | 3 (2–4; 10) | 7409 (1) | 9.70 ± 1.93 | 57.0 ± 13.6 | 784.6 ± 204.3 |
Data are presented in the table as mean ± SD (n). Tmax is presented as median (range; n). If n < 3, the actual values are reported
AUCINF, area under the plasma concentration–time curve to infinity; Cl, systemic clearance; Cl/F, apparent systemic clearance; Cmax, peak plasma concentration; NR, not reportable; Tmax, time to peak concentration; T1/2 half-life; V volume of distribution; V/F apparent volume of distribution