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The objective of the current study is to investigate safety, tolerability, and pharmacokinetics of BI 201335 ZW following administration of single rising doses from 5 mg to 1500 mg. In addition Two stage intra-subject bioavailability comparison of 600 mg BI 201335 ZW as a liquid formulation given with and without food.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| BI 201335 ZW - single rising dose | Experimental |
| |
| Placebo | Placebo Comparator |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| BI 201335 ZW - single rising dose | Drug |
| ||
| Placebo |
| Measure | Description | Time Frame |
|---|---|---|
| Number of patients with abnormal findings in physical examination | Baseline, day 3 of each treatment period, within 8 days after last administration | |
| Number of patients with clinically significant changes in vital signs | Baseline, day 1-3 of each treatment period, within 8 days after last administration | |
| Number of patients with clinically significant changes in 12-lead ECG (electrocardiogram) | Baseline, day 1, 2 in treatment period, within 8 days after last administration | |
| Number of patients with abnormal changes in laboratory parameters | Baseline, day 1-3 of each treatment period, within 8 days after last administration | |
| Number of patients with adverse events | up to 13 days | |
| Assessment of tolerability by investigator on a 4-point scale | on day 3 of each treatment period |
| Measure | Description | Time Frame |
|---|---|---|
| Cmax (maximum concentration of the analyte in plasma) | pre-dose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 15, 24, 30, 36 and 48 hours post-dose | |
| tmax (time from dosing to maximum concentration) | pre-dose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 15, 24, 30, 36 and 48 hours post-dose |
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Inclusion Criteria:
Exclusion Criteria:
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| Drug |
|
| AUC0-∞ (area under the concentration time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity) | pre-dose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 15, 24, 30, 36 and 48 hours post-dose |
| AUC0-tz (area under the concentration-time curve of the analyte in plasma over the time interval from 0 to the last quantifiable data point) | pre-dose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 15, 24, 30, 36 and 48 hours post-dose |
| λz (terminal elimination rate constant in plasma) | pre-dose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 15, 24, 30, 36 and 48 hours post-dose |
| t1/2 (terminal half-life of the analyte in plasma) | pre-dose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 15, 24, 30, 36 and 48 hours post-dose |
| MRTpo (Mean residence time of the analyte in the body after oral administration) | pre-dose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 15, 24, 30, 36 and 48 hours post-dose |
| CL/F (apparent clearance of the analyte in the plasma after oral administration) | pre-dose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 15, 24, 30, 36 and 48 hours post-dose |
| Vz/F (apparent volume of distribution during the terminal phase λz following an oral dose) | pre-dose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 15, 24, 30, 36 and 48 hours post-dose |