Calculated exposure of lixivaptan and metabolites in humans
Data are means ± S.D. Subjects were given a single 100-mg dose of lixivaptan for 7 days; exposure at day 7.
| Analyte | 14C Human Study | Simulated from14C Study | Nonradiolabeled Clinical Study | |||
|---|---|---|---|---|---|---|
| Cmax | AUC | Css | AUCss | Css | AUCss | |
| ng/ml | ng · h/ml | ng/ml | ng · h/ml | ng/ml | ng · h/ml | |
| Lixivaptan | 454 ± 114 | 1860 ± 305 | 575 ± 170 | 2440 ± 1000 | 514 ± 220 | 2960 ± 1060 |
| M3a | 716 ± 317 | 8100 ± 2470 | 942 ± 349 | 10700 ± 2450 | 112 ± 42.9 | 416 ± 167 |
| M5 | 290 ± 99 | 2680 ± 591 | 346 ± 108 | 3230 ± 589 | 454 ± 137 | 3040 ± 991 |
| M6 | 278 ± 103 | 5180 ± 2410 | 428 ± 160 | 8110 ± 4020 | 658 ± 201 | 6610 ± 2110 |
ss, steady state.
↵a Quantified with M1 and M2 in the 14C human AME study.