Dose
(mg)
|
thalf
(h)
±
SD
|
Cmax
(ng/mL) ± SD
|
Tmax
(h) ± SD
|
AUC(0-inf)
(ng/mL) ± SD
|
SAD |
|
|
|
|
0.3 mg (n=5)* |
7.4 ± 3.1 |
15.3 ± 2.7 |
1.4 ± 1.1 |
117 ±
13.3 |
1 mg (n=4) |
7.1 ± 0.9 |
43.7 ± 8.8 |
1.5 ± 0.4 |
351 ±
61.1 |
3 mg (n=4) |
16.2 ± 8.6 |
136 ± 53.7 |
2.3 ± 1.2 |
1060 ±
307 |
10 mg (n=3) |
9.0 ± 2.0 |
413 ± 221 |
0.7 ± 0.3 |
2660 ±
1830 |
30 mg (n=4) |
8.9 ± 2.2 |
1520 ± 68.3 |
1.0 ± 0.0 |
11600 ±
1740 |
60 mg (n=6) |
9.5 ± 0.7 |
2700 ± 4.0 |
0.9 ± 0.6 |
16100 ±
3840 |
100 mg (n=5) |
10.0 ± 4.1 |
5110 ± 744 |
1.3 ± 1.0 |
35700 ±
6190 |
200 mg (n=5) |
10.9 ± 1.6 |
6760 ± 1750 |
1.0 ± 0.4 |
43500 ±
14200 |
400 mg (n=6) |
9.3 ± 1.0 |
12600 ± 3430 |
1.5 ± 0.8 |
85200 ±
16300 |
600 mg (n=6) |
14.6 ± 12.7 |
14600 ± 4480 |
1.3 ± 0.6 |
96700 ±
17300 |
Food effect |
|
|
|
|
100 mg, fasted (n=6) |
12.6 ± 7.1 |
4490 ±949 |
1.6 ± 0.4 |
32900 ±
8060 |
100 mg, fed (n=6) |
9.5 ± 0.6 |
3810 ± 967 |
3.3 ± 1.0 |
33300 ±
7430 |
Gender differences |
|
|
|
|
100 mg, females (n=6) |
15.1 ± 6.3 |
5390 ± 2140 |
1.3 ± 0.7 |
33100 ±
11800 |
100 mg, males (n=11) ** |
11.4 ± 5.8 |
4774 ± 891 |
1.5 ± 0.7 |
31129 ±
11474 |
MAD |
|
|
|
|
30 mg (n=8) |
8.9 ± 1.8 |
1680 ± 380 |
1.0 ± 0.5 |
8000 ±
2060 |
70 mg (n=8) |
13.6 ± 6.6 |
3000 ± 327 |
0.8 ± 0.4 |
14000 ±
1690 |
150 mg (n=8) |
11.6 ± 2.6 |
5810 ± 1630 |
1.8 ± 0.6 |
33600 ±
12100 |