TABLE 3.
Summary of main PK parameters of dimdazenil following single-dose administration.
| Parameter | 1.5 mg | 2.5 mg fasted | 2.5 mg fed | 5 mg | Day 1 in 2.5 mg multiple dose |
|---|---|---|---|---|---|
| N = 12 | N = 12 | N = 12 | N = 12 | N = 13 | |
| Cmax (ng/mL) | |||||
| Mean (SD) | 23.54 (6.76) | 37.43 (9.30) | 28.22 (6.31) | 70.37 (17.37) | 30.24 (6.38) |
| GM (CV%) | 22.82 (25.4) | 36.35 (26.1) | 27.57 (22.8) | 68.41 (25.4) | 29.63 (21.2) |
| AUC0-t (h*ng/mL) | |||||
| Mean (SD) | 130.84 (86.34) | 224.90 (84.34) | 221.32 (91.39) | 461.04 (166.65) | 191.46 (52.13) |
| GM (CV%) | 113.69 (54.8) | 210.88 (39.3) | 206.93 (38.8) | 429.39 (43.1) | 184.74 (28.7) |
| AUC0-∞ (h*ng/mL) | |||||
| Mean (SD) | 132.88 (86.24) | 227.05 (83.95) | 224.30 (92.08) | 462.44 (167.16) | 194.47 (54.83) |
| GM (CV%) | 115.99 (53.7) | 213.42 (38.4) | 209.97 (38.3) | 430.71 (43.0) | 187.21 (29.6) |
| AUC0-24h (h*ng/mL) | |||||
| Mean (SD) | 128.02 (77.55) | 220.20 (75.22) | 214.36 (76.04) | 443.92 (151.22) | 191.70 (52.32) |
| GM (CV%) | 113.50 (50.4) | 208.51 (36.1) | 203.31 (34.6) | 416.74 (40.4) | 184.94 (28.8) |
| Tmax (h) | |||||
| Median (range) | 0.75 (0.5–2) | 0.75 (0.5–3.5) | 2.50 (1.5–5) | 0.50 (0.5–5) | 1.50 (0.5–3.52) |
| t1/2z (h) | |||||
| Mean (SD) | 3.80 (1.40) | 3.99 (1.16) | 4.14 (1.26) | 4.32 (1.19) | 3.50 (0.62) |
| Vz (L) | |||||
| Mean (SD) | 67.93 (11.69) | 65.33 (8.78) | 69.04 (8.98) | 71.10 (14.80) | 67.69 (13.15) |
| CLz (L/h) | |||||
| Mean (SD) | 14.26 (5.70) | 12.48 (4.78) | 12.64 (4.48) | 12.61 (5.69) | 13.89 (4.08) |
Data are expressed as arithmetic mean with standard deviation (SD) and geometric mean (GM) with coefficient of variation (CV), except for Tmax which is expressed as median (range).
Cmax: maximum observed concentration; AUC: area under the concentration–time curve; AUC0-t: AUC, from time of administration to the last measurable concentration; AUC0-∞: AUC, from time of administration to infinity; AUC0–24h: AUC, from time of administration to 24 h; Tmax: time to reach the maximum observed concentration; t1/2z: apparent terminal elimination half-life; CLz, apparent clearance; Vz: apparent volume of distribution.