Summary of the PK of KAE609 in human plasma
Blood samples were collected at selected time intervals from each subject. Plasma samples were prepared by centrifugation. Total radioactivity in blood and plasma was determined by scintillation counting. After extraction, plasma samples were analyzed by validated LC-MS/MS analysis. PK parameters were calculated using Phoenix (WinNonlin, version 6.2).
| Subject ID | tmax | Cmax | AUC0–24 h | AUClast | AUCinf | t1/2 | CL/F | Vz/F |
|---|---|---|---|---|---|---|---|---|
| h | ng/ml | mg⋅h/ml | h | l/h | liters | |||
| 5101 | 8.00 | 2310 | 37.8 | 96.4 | 96.6 | 34.2 | 3.11 | 153 |
| 5102 | 3.00 | 2290 | 30.9 | 96.5 | 97.0 | 39.6 | 3.09 | 177 |
| 5103 | 6.00 | 1520 | 22.8 | 55.3 | 55.4 | 27.8 | 5.42 | 217 |
| 5104 | 3.00 | 2330 | 28.0 | 60.0 | 60.0 | 30.5 | 5.00 | 220 |
| 5105 | 3.00 | 623 | 11.3 | 38.6 | 38.8 | 36.4 | 7.73 | 406 |
| 5106 | 4.00 | 1590 | 23.3 | 53.5 | 53.9 | 32.1 | 5.57 | 258 |
| Mean | NA | 1780 | 25.7 | 66.7 | 67.0 | 33.4 | 4.99 | 238 |
| SD | NA | 676 | 8.95 | 24.1 | 24.2 | 4.23 | 1.74 | 89.8 |
| %CV mean | NA | 38.0 | 34.8 | 36.1 | 36.1 | 12.7 | 35.0 | 37.7 |
| Geomean | NA | 1627 | 24.1 | 63.2 | 63.4 | 33.2 | 4.73 | 227 |
| %CV geomean | NA | 54.4 | 43.5 | 37.2 | 37.2 | 12.7 | 37.2 | 34.9 |
| Median | 3.50 | 1940 | 25.7 | 57.7 | 57.7 | 33.2 | 5.21 | 219 |
| Minimum | 3.00 | 623 | 11.3 | 38.6 | 38.8 | 27.8 | 3.09 | 153 |
| Maximum | 8.00 | 2330 | 37.8 | 96.5 | 97.0 | 39.6 | 7.73 | 406 |
NA, not applicable (only the median and range are presented for tmax).