Table 3.
Venetoclax plasma PK parameters (geometric mean (geometric standard deviation)).
| D1 | D15 | D29 | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
|
| |||||||||||
| Dose (mg) | Cmax (μg/L) | Cmax/Dose (μg/L/mg) | Tmax (h) | t½ (h) | AUC0-last (mg/L·h) | AUC0-infa (mg/L·h) | Cl/F (L/h) | Cmin (μg/L) | Cmaxb (μg/L) | AUC0–24b (mg/L·h) | Ratioc D29/D1 |
|
| |||||||||||
| 400 (N=3) | 658 (1.29) | 1.64 (1.29) | 5.2 (1.3) | 11 (1.2) | 8.02 (1.21) | 11.1 (1.27) | 36.2 (1.27) | 180 (1.72) | 968 (1.67) | 10.5 (1.65) | 0.95 (1.99) |
| 600 (N=3) | 1172 (1.79) | 1.95 (1.79) | 5.6 (1.5) | 6.6 (1.4) | 12.2 (1.65) | 14.6 (1.65) | 41.2 (1.65) | 214 (2.30) | 554 (4.89) | 9.11 (4.1) | 0.62 (5.32) |
| 800 (N=4) | 979 (1.50) | 1.22 (1.50) | 6.9 (1.2) | 9.4 (1.8) | 8.76 (1.54) | 16.6 (2.31) | 48.1 (2.31) | 177 (2.89) | 1000 (-) | 8.87 | 0.79 |
|
| |||||||||||
| Total (N=10) | 917 (1.57) | 1.54 (1.54) | 6.0 (1.3) | 8.9 (1.6) | - | - | 42.1 (1.76) | 188 (2.17) | 765 (2.74) | 0.77 (2.90) | |
a
AUC0-inf extrapolated beyond the last time point sampled was geometric mean 20% (range 4.9–84%).
b
N=3, 3, and 1 respectively for the 400, 600, and 800 mg dose.
c
Ratio of day 29 AUC0–24 over day 1 AUC0-inf.