Healthy
Conditions
Brief summary
Study to assess pharmacokinetics incl. dose proportionality, safety and tolerability of 4 different dosage strengths of BIBW 2992 tablets (final formulation of 20 mg, 30 mg, 40 mg, 50 mg) administered as single doses to healthy male volunteers
Interventions
DRUGBIBW 2992 MA2 - single rising dose
Sponsors
Boehringer Ingelheim
Study design
Allocation
NA
Intervention model
SINGLE_GROUP
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 (blood pressure, pulse rate), 12-lead Electrocardiogram (ECG), 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 (GCP) and the local legislation
Exclusion criteria
* Any finding of the medical examination (including Blood Pressure (BP), Puse Rate (PR) and Electrocardiogram (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 1 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 administration of the trial drug 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) * 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 30 g/day) * Drug abuse * Blood donation (more than 100 mL within 4 weeks prior to administration of the trial drug or during the trial) * Excessive physical activities (within 1 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 |
|---|---|
| Cmax (maximum measured concentration of the analyte in plasma) | predose, up to120 h after drug administration |
| AUC0-tz (area under the concentration-time curve of the analyte in plasma over the time interval from 0 to the time of the last quantifiable data point) | predose, up to 120 h after drug administration |
| AUC0-∞ (area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity) | predose, up to 120 h after drug administration |
Secondary
| Measure | Time frame |
|---|---|
| λz (terminal rate constant of the analyte in plasma) | predose, up to 120 h after drug administration |
| t1/2 (terminal half-life of the analyte in plasma) | predose, up to 120 h days after drug administration |
| MRTpo (mean residence time of the analyte in the body after oral administration) | predose, up to 120 h after drug administration |
| CL/F (apparent clearance of the analyte in plasma after extravascular administration) | predose, up to 120 h after drug administration |
| Vz/F (apparent volume of distribution during the terminal phase λz following an extravascular dose) | predose, up to 120 h after drug administration |
| %AUCtz-∞ (percentage of the AUCtz-∞ obtained by extrapolation from the last quantifiable data point to infinity) | predose, up to 120 h after drug administration |
| Number of patients with clinically significant changes in vital signs (blood pressure, pulse rate) | Screening, up to 20 days after drug administration |
| Number of patients with abnormal changes in laboratory parameters | Screening, up to 20 days after drug administration |
| Number of patients with adverse events | up to 41 days |
| Assessment of tolerability by investigator on a 4-point scale | up to 20 days after drug administration |
| Number of patients with abnormal changes in 12-lead electrocardiogram (ECG) | Screening, up to 20 days after drug administration |
| Number of patients with abnormal findings in physical examination | Screening, up to 20 days after drug administration |
| AUC0-24 (area under the concentration-time curve of the analyte in plasma over the time interval from 0 [predose] to 24 h) | predose, up to 120 h after drug administration |
| tmax (time from dosing to the maximum concentration of the analyte in plasma) | predose, up to 120 h after drug administration |
Outcome results
None listed