Table 3.
PK analyses on Day 1
| Parameter (mean ± SD) | 0.7 mg/m2 (n = 3) | 1.0 mg/m2 (n = 3) | 1.4 mg/m2 (n = 6) | 2.0 mg/m2 (n = 3) |
|---|---|---|---|---|
| Plasma | ||||
| Cmax (ng/mL) | 288.5 ± 43.0 | 380.6 ± 52.9 | 519.4 ± 107.2 | 717.6 ± 104.3 |
| AUC0-inf (ng.h/mL) | 299.2 ± 124.5 | 379.6 ± 65.2 | 672.7 ± 113.7 | 1370.1 ± 282.2 |
| t½ (h) | 36.4 ± 11.2 | 42.9 ± 10.9 | 39.4 ± 8.3 | 59.9 ± 13.4 |
| CL (L/h/m2) | 2.31 ± 0.88 | 2.37 ± 0.39 | 1.89 ± 0.33 | 1.32 ± 0.25 |
| Vz (L/m2) | 117.3 ± 45.0 | 143.0 ± 14.4 | 105.6 ± 19.6 | 111.7 ± 13.0 |
| MRT (h) | 32.6 ± 9.1 | 40.8 ± 10.4 | 40.7 ± 10.1 | 67.5 ± 22.5 |
| Urine | ||||
| Ae (μg) | 51.9 ± 8.89 | 104.5 ± 31.9 | 238.1 ± 28.4 | 355.7 ± 98.7 |
| fe (%) | 5.01 ± 0.69 | 7.36 ± 2.47 | 11.52 ± 1.04 | 12.88 ± 3.95 |
| CLR (mL/h) | 220.5 ± 62.7 | 352.2 ± 127.2 | 454.4 ± 83.6 | 394.8 ± 94.2 |
| CL (mL/h) | 3808.8 ± 1295.4 | 3872.5 ± 807.0 | 3126.3 ± 416.0 | 2086.3 ± 441.7 |
Ae, amount of unchanged drug excreted in urine; AUC0-inf, area under the concentration-time curve from time zero to infinity; CL, total clearance; CLR, renal clearance; fe, fraction of the dose excreted unchanged in the urine; MRT, mean residence time; t½, final elimination half-life; Vz, volume of distribution at terminal phase