Table 5.
Summary of pharmacokinetic parameters for AZD9164 after single dose and after last dose (400 μg, 1000 and 2800 μg)
| |
First dose |
Last dose |
||||
|---|---|---|---|---|---|---|
|
Geometric mean (CV%) | ||||||
|
PK parameters AZD9164 |
400 μg |
1000 μg |
2800 μg |
400 μg |
1000 μg |
2800 μg |
| (n = 6) | (n = 6) | (n = 6) | (n = 6) | (n = 6) | (n = 5) | |
|
GMAD Study healthy subjects | ||||||
| Cmax (nmol/L) |
1.32 (52.9) |
3.93 (64.9) |
13.3 (136.0) |
1.95 (36.2) |
7.47 (50.5) |
16.0 (140.0) |
| tmax (min)a |
10.0 (5–31) |
10.0 (5–16) |
5.0 (5–15) |
11.0 (5–31) |
5.0 (5–16) |
5.0 (5–6) |
| t½ (h) |
95.1 (19.5) |
137 (41.1) |
72.3 (58.5) |
189 (62.4) |
179 (86.1) |
131.0 (55.9) |
| AUCb |
11.8 (30.1) |
41.3 (62.1) |
54.5 (113) |
12.1 (25.0) |
39.4 (42.2) |
58.6 (87.8) |
| Cmax/dose(10-3/L) |
1.53 (52.9) |
1.83 (64.9) |
2.21 (136.0) |
2.28 (36.2) |
3.47 (50.5) |
2.67 (140.0) |
| AUC/Doseb |
0.0138 (30.1) |
0.0193 (62.1) |
0.0092 (113) |
0.0141 (25.0) |
0.0184 (42.2) |
0.0098 (87.8) |
| Rac |
- |
- |
- |
3.23 (22.1) |
3.52 (48.4) |
2.47 (30.0) |
|
JMAD Study healthy subjects | ||||||
| Cmax (nmol/L) |
1.14 (30.8) |
7.27 (47.6) |
- |
1.83 (33.2) |
6.30 (31.8) |
- |
| tmax (min)a |
15 (5–60) |
5 (5–5) |
- |
15 (5–90) |
5 (5–15) |
- |
| t½ (h) |
88.1 (29.7) |
71.3 (11.9) |
- |
107.3 (26.2) |
130.2 (56.9) |
- |
| AUCb |
12.5 (23.0) |
29.4 (49.3) |
- |
15.6 (18.7) |
28.6 (40.9) |
- |
| Cmax/dose(10-3/L) |
1.33 (30.8) |
3.39 (47.6) |
- |
2.13 (33.2) |
2.93 (31.8) |
- |
| AUC/Doseb |
0.0145 (23.0) |
0.0137 (49.3) |
- |
0.0182 (18.7) |
0.0133 (40.9) |
- |
| Rac | - | - | - | 3.69 (24.4) | 2.08 (25.1) | - |
aMedian (minimum to maximum).
bZero to infinity for single dose; 0–24 for last dose.