TABLE 4.
Summary of pharmacokinetic parameters of KAF156 following oral administration of single ascending doses (part 1)a
| Dose (mg) | AUC0–24 (ng · h/ml) | AUClast (ng · h/ml) | AUCinf (ng · h/ml) | Cmax (ng/ml) | Tmax (h) | t1/2 (h) | CL/F (liters/h) | Vz/F (liters) |
|---|---|---|---|---|---|---|---|---|
| 10 (n = 3) | 83.0 ± 14.6 | 123 ± 16.2 | 7.6 ± 1.29 | 1.00 (1.00, 1.00) | ||||
| 60 (n = 3) | 679 ± 102 | 1,560 ± 205 | 1,710 ± 216 | 67.6 ± 9.79 | 1.02 (1.02, 4.00) | 47.1 ± 4.35 | 35.6 ± 4.81 | 2,410 ± 222 |
| 180 (n = 3) | 3,180 ± 1,240 | 7,550 ± 4,170 | 8,210 ± 4,830 | 275 ± 82.9 | 2.00 (2.00, 3.00) | 51.7 ± 9.14 | 26.8 ± 12.6 | 1,890 ± 640 |
| 400 (n = 8) | 7,570 ± 1,380 | 17,200 ± 4,890 | 18,700 ± 5,650 | 796 ± 177 | 3.00 (2.00, 6.00) | 55.6 ± 10.2 | 23.8 ± 9.52 | 1,820 ± 440 |
| 800 (n = 6) | 19,500 ± 2,340 | 43,700 ± 6,080 | 46,900 ± 6,870 | 2,050 ± 328 | 3.00 (2.00, 4.00) | 48.0 ± 5.83 | 17.4 ± 2.51 | 1,200 ± 176 |
| 1,200 (n = 6) | 31,200 ± 7,200 | 78,800 ± 24,800 | 80,300 ± 25,400 | 2,720 ± 949 | 4.00 (3.00, 6.00) | 70.7 ± 9.78 | 16.0 ± 4.24 | 1,610 ± 381 |
a
All values are means ± standard deviations except Tmax, which are medians (ranges). PK parameters that could not be adequately characterized were excluded.