Table 5.
Pharmacokinetic parameters of SJG-136 following daily × 3 intravenous administration of 20, 25, 30 or 35 µg/m2/day SJG-136 (Schedule B).
| SJG-136 Dose Level (µg/m2/day) |
|||||
|---|---|---|---|---|---|
| 20 (n=3) | 25 (n=3) | 30 (n=5) | 35 (n=2) | ||
|
Cmax (ng/mL) |
C1D1 | 6.41 (1.10) | 5.97 (1.76) | 9.51 (2.09) | 13.63 |
| C1D3 | 6.12 (2.47) | 5.52 (2.24) | 7.84 (3.57) | 9.85 | |
| C2D1 | 7.68 (3.70) | 6.45 (0.80) | 9.61 (2.59) | 14.17 | |
| C2D3 | 6.92 (3.68) | 4.60 (0.46) | 6.91 (1.48) | 9.23 | |
|
AUCinf (ng•min/mL) |
C1D1 | 254 (116) | 303 (73) | 439 (140) | 575 |
| C1D3 | 273 (169) | 306 (155) | 372 (152) | 450 | |
| C2D1 | 426 (247) | 335 (48) | 455 (213) | 641 | |
| C2D3 | 376 (255) | 244 (39) | 319 (120) | 402 | |
|
Half-life (min) |
C1D1 | 74.3 (17.4) | 99.5 (24.0) | 85.5 (17.4) | 65.3 |
| C1D3 | 48.5 (20.4) | 91.9 (10.4) | 96.9 (16.3) | 77.2 | |
| C2D1 | 77.3 (24.6) | 81.7 (17.8) | 82.3 (11.5) | 69.2 | |
| C2D3 | 87.8 (28.9) | 94.3 (7.1) | 76.9 (10.5) | 74.5 | |
|
CL (mL/min/m2) |
C1D1 | 88.7 (32.9) | 86.1 (23.5) | 73.2 (19.8) | 61.9 |
| C1D3 | 91.7 (46.0) | 95.2 (40.7) | 92.3 (38.3) | 78.1 | |
| C2D1 | 57.0 (26.9) | 75.7 (11.6) | 75.5 (27.2) | 55.7 | |
| C2D3 | 69.1 (36.1) | 103.9 (15.1) | 104.5 (35.3) | 89.3 | |
|
Vss (mL/m2) |
C1D1 | 4730 (553) | 7630 (2590) | 4860 (911) | 3120 |
| C1D3 | 3920 (1930) | 8070 (3700) | 7370 (2720) | 5020 | |
| C2D1 | 4540 (3180) | 6050 (1300) | 5060 (1510) | 3170 | |
| C2D3 | 5600 (3990) | 8760 (1180) | 6810 (2240) | 5570 | |