Table 4.
Gemcitabine (dFdC) and metabolite (dFdU) plasma pharmacokinetic parameters, mean (standard deviation).
| dFdC | dFdC | dFdC | dFdC | dFdC | dFdU | dFdU | dFdU | dFdU/dFdC | dFdU/dFdC | ||
|---|---|---|---|---|---|---|---|---|---|---|---|
|
| |||||||||||
| Gemcitabine (mg/m2) |
Veliparib (mg) |
Cmax (µg/mL) |
t½ (min) |
AUC0-inf1 (µg/mL•h) |
Cl (L/h/m2) |
Vss (L/m2) |
Cmax (µg/mL) |
t½ (h) |
AUC0-48 (µg/mL•h) |
Cmax | AUC2 |
| 500 (N=5) | 10 | 9.36 (5.72) | 25.7 (4.3) | 5.68 (3.45) | 109 (46) | 57.1 (31.3) | 16.1 (3.6) | 27.6 (9.5) | 216 (82) | 2.3 (1.3) | 41 (25) |
| 500 (N=3) | 20 | 7.17 (0.88) | 17.3 (5.8) | 4.07 (0.40) | 124 (12) | 53.8 (9.4) | 20.7 (3.8) | 130 (161) | 257 (43) | 2.9 (0.5) | 64 (17) |
| 750 (N=3) | 10 | 11.5 (0.3) | 22.9 (9.0) | 7.07 (0.73) | 107 (10) | 47.0 (1.4) | 18.4 (1.0) | 28.3 (15.1) | 186 (81) | 1.6 (0.1) | 26 (8) |
| 750 (N=13) | 20 | 13.4 (4.0) | 23.6 (5.6) | 8.22 (2.12) | 99 (35) | 46.5 (19.6) | 22.0 (2.6) | 58.1 (36.8) | 236 (62) | 1.7 (0.6) | 29 (7) |
| 750 (N=3) | 40 | 17.6 (14.6) | 54.4 (13.8) | 9.17 (5.51) | 100 (44) | 46.7 (24.1) | 18.7 (5.0) | 29.3 (5.8) | 188 (33) | 1.4 (0.7) | 24 (8) |
|
| |||||||||||
| All (N=27) | - | 26.6 (12.1) | - | 105 (34) | 49.4 (20.0) | - | 53.8 (60.9) | - | 1.9 (0.8) | 35 (17) | |
1
The extrapolated portion was less than 0.37%.
2
Calculated as dFdU-AUC0–48h / dFdC-AUC0-inf.