Table 5.
Mean (coefficient of variation) pharmacokinetic parameters for cycle 1 of R(+)XK469
| Dose level | N | Cmax (μg/ml) | AUC0→T (h μg/ml) | AUC0→∞ (h μg/ml) | t½ (h) | Cl (ml/h) | Vss (L) | |||
|---|---|---|---|---|---|---|---|---|---|---|
| Day 1 | Day 3 | Day 1 | Day 3 | Day 1 | Day 3 | Day 1 | Day 1 | Day 1 | ||
| Schedule A (mg) | ||||||||||
| 15 | 2 | 1.2 (0.03) | 24 (0.10) | 106 (0.72) | 66 (0.75) | 191 (0.72) | 13 (0.50) | |||
| 30 | 2 | 4.1 (0.29) | 41 (0.18) | 162 (0.30) | 57 (0.11) | 194 (0.30) | 15 (0.19) | |||
| 60 | 2 | 8.8 (0.02) | 92 (0.19) | 223 (0.44) | 31 (0.33) | 297 (0.44) | 12 (0.10) | |||
| 120 | 1 | 14.3 | 148 | 347 | 30 | 345 | 15 | |||
| 240 | 4 | 27.9 (0.14) | 335 (0.10) | 1.285 (0.54) | 56 (0.60) | 244 (0.64) | 14 (0.16) | |||
| Schedule B (mg) | ||||||||||
| 360 | 3 | 58.0 (0.31) | 79.9 (0.18) | 1.177 (0.14) | 1.885 (0.24) | 2.577 (0.25) | 4.091 (0.37) | 54 (0.36) | 147 (0.29) | 11 (0.22) |
| 540 | 6 | 71.5 (0.20) | 89.6 (0.32) | 1.469 (0.20) | 2.010 (0.28) | 5.002 (0.77) | 5.564 (0.74) | 90 (0.85) | 152 (0.51) | 14 (0.20) |
| 675 | 5 | 86.2 (0.18) | 104.2 (0.14) | 1.581 (0.12) | 2.195 (0.22) | 3.033 (0.18) | 4.335 (0.30) | 61 (0.71) | 220 (0.23) | 13 (0.24) |
| 850 | 7 | 105.1 (0.17) | 127.1 (0.15) | 2.270 (0.24) | 3.307 (0.29) | 5.161 (0.59) | 7.748 (0.53) | 43 (0.55) | 216 (0.56) | 13 (0.14) |
| 1100 | 20 | 146.3 (0.22) | 166.5 (0.21) | 3.067 (0.26) | 4.489 (0.28) | 7.903 (0.49) | 10.531 (0.43) | 55 (0.41) | 169 (0.45) | 14 (0.31) |
| 1400 | 1 | 173.1 | 177.7 | 4.571 | 6.718 | 16.473 | 35.930 | 107 | 84 | 13 |
| Schedule C (mg) | ||||||||||
| 1600 | 5 | 172.0 (0.21) | 4.607 (0.28) | 13.785 (0.55) | 75 (0.47) | 144 (0.51) | 14 (0.32) | |||
| 2000 | 3 | 247.6 (0.22) | 5.704 (0.12) | 11.204 (0.19) | 47 (0.10) | 183 (0.18) | 12 (0.09) | |||
| 2500 | 14 | 293.9 (0.19) | 7.125 (0.30) | 13.905 (0.52) | 42 (0.33) | 215 (0.39) | 11 (0.16) | |||
| 3200 | 5a | 292.3 (0.20) | 8.155 (0.21) | 16.445 (0.21) | 49 (0.08) | 193 (0.24) | 13 (0.22) | |||
a
One patient had blood levels drawn at significantly insufficient time points.