Healthy
Conditions
Brief summary
The objective of the current study was to investigate the safety, tolerability, and pharmacokinetics of BILB 1941 ZW following the administration of single rising doses from 5 mg to 300 mg. In addition the bioavailability of the 60 mg dose given fasted and after a high-fat breakfast was to be be investigated
Interventions
DRUGBILB 1941 ZW - single rising dose part
DRUGPlacebo
DRUGBILB 1941 ZW - solution
DRUGBILB 1941 ZW - tablet
Sponsors
Boehringer Ingelheim
Study design
Allocation
RANDOMIZED
Intervention model
PARALLEL
Primary purpose
TREATMENT
Masking
DOUBLE
Eligibility
Sex/Gender
MALE
Age
18 Years to 50 Years
Healthy volunteers
Yes
Inclusion criteria
1. Healthy males according to the following criteria based upon a complete medical history, including the physical examination, vital signs (BP, PR), 12-lead ECG, clinical laboratory tests: 1.1 No finding deviating from normal and of clinical relevance 1.2 No evidence of a clinically relevant concomitant disease 2. Age ≥18 and Age ≤50 years, BMI ≥18.5 and BMI ≤29.9 kg/m2 (Body Mass Index) 3. Signed and dated written informed consent prior to admission to the study in accordance with Good Clinical Practice (GCP) and the local legislation
Exclusion criteria
* Any finding of the medical examination (including blood pressure, pulse rate and ECG) deviating from normal and of clinical relevance * 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 1 month 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 of more than 100 mL 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 | Description |
|---|---|---|
| Number of subjects with abnormal findings in physical examination | up to 48 hours following drug administration | — |
| Number of subjects with abnormal changes in laboratory parameters | up to 48 hours following drug administration | — |
| Number of subjects with clinically significant changes in vital signs | up to 48 hours following drug administration | Blood pressure, Pulse Rate |
| Number of subjects with adverse events | up to 48 hours following drug administration | — |
| Number of subjects with clinically significant changes in 12-lead ECG (electrocardiogram) | up to 48 hours following drug administration | — |
| Assessment of tolerability by investigator on a 4-point scale | after 48 hours following drug administration | — |
Secondary
| Measure | Time frame |
|---|---|
| MRT (Mean time of residence of drug molecules in the body after intravascular administration) | up to 48 hours following drug administration |
| Cmax (maximum concentration of the analyte in plasma) | up to 48 hours following drug administration |
| Vz/F (Apparent volume of distribution during the terminal phase after extravascular administration) | up to 48 hours following drug administration |
| tmax (time from dosing to maximum concentration) | up to 48 hours following drug administration |
| AUC0-∞ (area under the concentration time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity) | up to 48 hours following drug administration |
| 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) | up to 48 hours following drug administration |
| λz (terminal rate constant in plasma) | up to 48 hours following drug administration |
| t1/2 (terminal half-life of the analyte in plasma) | up to 48 hours following drug administration |
Outcome results
None listed