Table 2.
Pharmacokinetics of barasertib and barasertib-hQPA in plasma and urine
| Sample (n) | Parametera | Barasertib | Barasertib-hQPA |
|---|---|---|---|
| Plasma (4)b | AUC, ng.h/mLc | NC | 40,400 (0.4) |
| AUC(0–t), ng.h/mLc | 13,840 (0.4) | 40,080 (0.4) | |
| AUC(0–192 h), ng.h/mLc | NC | 38,230 (0.4) | |
| CSS, ng/mLc | 85.6 (0.5) | 226.8 (0.4) | |
| CL, L/h | NC | 31.4 (11.3) | |
| t½, h | NC | 66.3 (36.1) | |
| λZ, h–1 | NC | 0.02 (0.02) | |
| VSS, L | NC | 669.1 (344.9) | |
| VZ, L | NC | 2805 (1708) | |
| Urine (5) | Ae, mg | NC | 96.9 (47.2) |
| CLR, L/h | NC | 2.85 (1.6) | |
| fe % | NC | 8.1 (3.9) |
AUC, area under plasma concentration–time curve; C SS, steady-state drug concentration; CL, total clearance; t ½, terminal half-life; λ Z, slowest disposition rate constant; V SS, volume of distribution (apparent) at steady state; V Z, volume of distribution (apparent) during terminal (λZ) phase; Ae, cumulative amount of unchanged drug excreted; CL R, renal clearance of drug from plasma; fe, fraction of drug excreted into urine; NC, not calculable
aAll values are arithmetic mean (standard deviation) except where indicated. b Due to sampling issues, plasma concentration data were excluded for one patient. c Values indicate geometric mean (coefficient of variation)