Table 3.
Pharmakokinetic profile of anle138b: Geometric Mean (CV%) key pharmacokinetic parameters of anle138b in healthy volunteers following single oral administration of anle138b in capsule form. For Tmax Median (range) is shown. Abbreviations: Tmax: Time to maximum peak; Cmax: Maximum concentration; AUC: Area under the curve (= exposure); T1/2: Plasma half-life; h: Hour; ng: Nanogram; ml: Millilitre; NA: Not applicable.
| Treatment | Sampling day | Tmax* (h) | Cmax (ng/mL) | AUC(0-24) (ng·h/mL) | T1/2 (h) |
|---|---|---|---|---|---|
| Single Ascending Dose Study | |||||
|
Cohort A 50 mg |
Dosing day | 1·00 (0·50–2·00) |
54·3 (58·5) |
113 (66·0) |
3·9 (201·3) |
|
Cohort B 100 mg |
Dosing day | 1·50 (0·50–2·00) |
156 (30·5) |
366 (23·4) |
10·8 (57·6) |
|
Cohort C 200 mg |
Dosing day | 1·50 (1·00–2·00) |
458 (56·3) |
1090 (55·8) |
10·3, 15·8 [N=2] |
|
Cohort D 300 mg |
Dosing day | 1·50 (1·50–2·00) |
704 (49·5) |
1650 (48·6) |
16·2 (32·3) |
| Multiple Ascending Dose Study | |||||
|
Cohort A 100 mg |
Dosing day 1 | 1·00 (1·00–1·50) |
135 (38·9) |
261 (42·5) |
NA |
| Dosing day 7 | 1·25 (1·00–1·50) |
70·9 (55·4) |
141 (40·7) |
4·2 (119·6) [N=4] |
|
|
Cohort B 200 mg |
Dosing day 1 | 1·50 (1·00–2·02) |
447 (58·0) |
905 (60·7) |
NA |
| Dosing day 7 | 1·00 (1·00–1·50) |
128 (55·5) |
308 (34·1) |
9·5 (78·8)[N=5] |
|
|
Cohort C 300 mg |
Dosing day 1 | 1·50 (1·50–2·00) |
910 (94·9) |
2210 (81·1) |
NA |
| Dosing day 7 | 1·50 (1·00–1·50) |
307 (55·9) |
633 (37·3) |
6·06, 6·07 [N=2] | |
| Food Effect Study | |||||
| 150 mg fasted | Dosing day | 1·25 (1·00–2·00) |
442 (58·7) |
896 (54·7) |
11·3 (17·4)[N=3] |
| 150 mg fed | Dosing day | 3·00 (1·50–3·08) |
196 (48·6) |
641 (49·0) |
15·2 (28·3)[N=7] |