Healthy
Conditions
Brief summary
The primary objective of the study was to investigate the relative bioavailability and pharmacokinetics of 20 mg BIBW 2992 administered as film-coated immediate release tablet (final formulation, i.e. phase III/to-be-marketed formulation) to healthy subjects in comparison with the drinking solution and in comparison with the trial formulation II tablet, which was administered in phase II clinical trials and also partly in phase I trials.
Interventions
DRUGBIBW 2992 MA2
film-coated immediate release tablet - final formulation
Sponsors
Boehringer Ingelheim
Study design
Allocation
RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
TREATMENT
Masking
NONE
Eligibility
Sex/Gender
MALE
Age
21 Years to 55 Years
Healthy volunteers
Yes
Inclusion criteria
* Healthy males according to a complete medical history, including a physical examination, vital signs (BP (blood pressure), PR (pulse rate)), 12-lead ECG (electrocardiogram), and clinical laboratory tests * Age 21 to 55 years, inclusive * Body mass index 18.5 to 29.9 kg/m2, inclusive * Signed and dated written informed consent prior to admission to the study in accordance with Good Clinical Practice and the local legislation
Exclusion criteria
* Any finding of the medical examination (including BP, PR and ECG) deviating from normal and of clinical relevance * Any evidence of a clinically relevant concomitant disease * Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders * Surgery of the gastrointestinal tract (except appendectomy) * Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or neurological disorders * History of relevant orthostatic hypotension, fainting spells or blackouts * Chronic or relevant acute infections * History of relevant allergy/hypersensitivity (including drug allergy or its excipients) * Intake of drugs with a long half-life (\> 24 hours) within one month prior to administration of the trial drug or during the trial * Use of any drugs (including herbal preparations, vitamins and nutrient supplements) within 10 days prior to first administration of the trial drug or during the trial * Participation in another trial with an investigational drug within two months prior to administration or during the trial * Smoker (\> 10 cigarettes or \> 3 cigars or \> 3 pipes/day) * Inability to refrain from smoking within the in-house periods from 12 hours before until 25 hours after each administration of the trial drug * Alcohol abuse (more than 60 g/day) * Drug abuse * Blood donation (more than 100 mL within four weeks prior to administration of the trial drug or during the trial) * Excessive physical activities (within one week prior to administration of the trial drug or during the trial) * Any laboratory value outside the reference range that is of clinical relevance * Inability to comply with dietary regimen of trial site * A marked baseline prolongation of QT/QTc interval (e.g., repeated demonstration of a QTc interval \>450 ms) * A history of additional risk factors for Torsades de Points, e.g., heart failure, hypokalemia, family history of Long QT Syndrome
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| AUC0-∞ (area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity) | up to 96 hours after drug administration |
| Cmax (maximum measured concentration of the analyte in plasma) | up to 96 hours after drug administration |
Secondary
| Measure | Time frame |
|---|---|
| tmax (time from dosing to the maximum concentration of the analyte in plasma) | up to 96 hours after drug administration |
| λz (terminal rate constant in plasma) | up to 96 hours after drug administration |
| t1/2 (terminal half-life of the analyte in plasma) | up to 96 hours after drug administration |
| MRTpo (mean residence time of the analyte in the body after oral administration) | up to 96 hours after drug administration |
| AUC (area under the concentration-time curve of the analyte in plasma) for several time points | up to 96 hours after drug administration |
| Vz/F (apparent volume of distribution during the terminal phase λz following an extravascular dose) | up to 96 hours after drug administration |
| Number of patients with adverse events | up to 88 days |
| Assessment of tolerability by the investigator on a 4-point scale | Day 5 of each treatment period |
| CL/F (apparent clearance of the analyte in the plasma after extravascular administration) | up to 96 hours after drug administration |
| %AUCtz-∞ (percentage of the AUCtz-∞ that is obtained by extrapolation from the last quantifiable data point to infinity) | up to 96 hours after drug administration |
Outcome results
None listed