Healthy
Conditions
Brief summary
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.
Interventions
DRUGBI 201335 ZW - single rising dose
DRUGPlacebo
Sponsors
Boehringer Ingelheim
Study design
Allocation
RANDOMIZED
Intervention model
PARALLEL
Primary purpose
TREATMENT
Masking
DOUBLE
Eligibility
Sex/Gender
MALE
Age
18 Years to 55 Years
Healthy volunteers
Yes
Inclusion criteria
* Healthy males according to the following criteria based upon a complete medical history, including the physical examination, vital signs ((blood pressure (BP), pulse rate (HR)), 12-lead electrocardiogram (ECG), clinical laboratory tests * Age ≥18 and Age ≤55 years * BMI ≥18.5 and BMI ≤29.9 kg/m2 (Body Mass Index) * Signed and dated written informed consent prior to admission to the study in accordance with Good Clinical Practice (GCP) and the local legislation * Willingness to abstain from alcohol from screening period until conclusion visit
Exclusion criteria
* Any finding of the medical examination (including blood pressure, pulse rate and ECG) deviating from normal and of clinical relevance * Any evidence of a clinically relevant concomitant disease * History or current gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunologic, hormonal disorders, including a clinical history of viral hepatitis, or serological evidence of active Hepatitis B or Hepatitis C infection * History of orthostatic hypotension, fainting spells and blackouts * Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or neurological disorders * Chronic or relevant acute infections * History of allergy/hypersensitivity (including drug allergy) which is deemed relevant to the trial as judged by the investigator * Intake of drugs with a long half-life (\> 24 hours) within 1 month prior to administration * Use of any drugs which might influence the results of the trial within 10 days prior to administration or during the trial * Participation in another trial with an investigational drug within 2 months prior to administration or during the trial * Smoker (\> 10 cigarettes or 3 cigars or 3 pipes/day) or inability to refrain from smoking on trial days * Alcohol abuse (\> 60 g/day) * Drug abuse * Blood donation within 1 month prior to administration or during the trial * Excessive physical activities within 5 days prior to administration or during the trial * Any laboratory value outside the clinically accepted reference range and of clinical relevance * History of any familial bleeding disorder
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| 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 |
| 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 |
Secondary
| Measure | Time frame |
|---|---|
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
Outcome results
None listed