Table 1.
Summary of mean (standard deviation [SD]) plasma pharmacokinetic parameters for ampreloxetine: single-ascending dose study
| Dose level (mg) | Cmax (ng/mL) | Tmaxa (h) | Tlaga (h) | AUC0–24 (ng*h/mL) | AUC0–t (ng*h/mL) | t1/2 (h) | CL/F (L/h) | VZ/F (L) | |
|---|---|---|---|---|---|---|---|---|---|
| 2 | Mean | 0.925 | 12 | 1 | 15.8 | 36.3 | 29.5 | 56.4 | 2397 |
| SD | 0.335 | 8.00, 12.0 | 0.5, 1.5 | 5.6 | 11.1 | 4.6 | 22.3 | 916 | |
| n | 6 | 6 | 6 | 6 | 6 | 3 | 3 | 3 | |
| 4 | Mean | 2.09 | 8 | 1 | 32.8 | 87.6 | 36.0 | 38.7 | 1983 |
| SD | 0.34 | 8.00, 10.0 | 0.5, 1.0 | 4.3 | 11.4 | 6.4 | 6.4 | 353 | |
| n | 6 | 6 | 6 | 6 | 6 | 6 | 6 | 6 | |
| 8 | Mean | 5.02 | 12 | 0.50 | 85.6 | 231 | 34.5 | 38.2 | 1659 |
| SD | 1.4 | 8.05, 14.0 | 0, 1.0 | 22.5 | 98 | 12.8 | 17.4 | 386 | |
| n | 6 | 6 | 6 | 6 | 6 | 6 | 6 | 6 | |
| 20 | Mean | 8.59 | 12 | 0.5 | 142 | 445 | 41.0 | 52.2 | 2745 |
| SD | 2.45 | 8.00, 14.0 | 0, 2.0 | 43 | 195 | 12.2 | 33.8 | 1034 | |
| n | 6 | 6 | 6 | 6 | 6 | 6 | 6 | 6 | |
| 50 | Mean | 26.4 | 12 | 0.5 | 461 | 1430 | 40.9 | 39.9 | 2337 |
| SD | 5.7 | 8.00, 14.0 | 0, 1.0 | 105 | 530 | 8.8 | 15 | 1046 | |
| n | 6 | 6 | 6 | 6 | 6 | 5 | 5 | 5 |
In each cohort, 6 subjects were dosed with the active drug
AUC0–24 area under the concentration–time curve from time 0 to 24 h, AUC0–t area under the concentration–time curve from time 0 to the time of last quantifiable concentration, CL/F oral clearance, Cmax maximum concentration, t1/2 terminal elimination half-life, Tlag lag time, Tmax time to maximum concentration, VZ/F oral volume of distribution during terminal phase
aMedian (minimum, maximum)