Safety/Tolerability, Pharmacokinetics, and Pharmacodynamics of BIBB 1464 MS in Healthy Male Subjects, Combined With Preliminary Evaluation of Relative Bioavailability and Effect of Food
Phase 1
Completed
- Conditions
- Healthy
- Interventions
- Drug: BIBB 1464 MS tabletDrug: BIBB 1464 MS solutionDrug: BIBB 1464 MS placeboOther: Standard dinner
- Registration Number
- NCT02229838
- Lead Sponsor
- Boehringer Ingelheim
- Brief Summary
Safety, pharmacodynamics and pharmacokinetics of 0.25, 0.75, 2.0, 6.0, and 10 mg BIBB 1464 p.o once daily in a rising dose group-comparison (placebo controlled, double blind, randomized per dose level).
Relative Bioavailability of 0.75 mg or 2 mg or 6 mg ( tablet vs. solution, intraindividual comparison), preliminary assessment of food effects (interindividual comparison)
Two-stage Trial Design With Randomised Double Blind Placebo Controlled Rising Dose Phase and Subsequent Randomised, Open Parallel Group Phase).
MS (Tablet) in Healthy Male Subjects, Combined With Preliminary Evaluation of Relative Bioavailability and Effect of Food of the Dose of 0.75 mg or 2 mg or 6 mg (Two-stage Trial Design With Randomised Double Blind Placebo Controlled Rising Dose Phase and Subsequent Randomised, Open Parallel Group Phase).
- Detailed Description
Not available
Recruitment & Eligibility
- Status
- COMPLETED
- Sex
- Male
- Target Recruitment
- 73
Inclusion Criteria
- Healthy subjects as determined by results of screening
- Signed written informed consent in accordance with good clinical practice (GCP) and local legislation
- Age > 18 and < 55 years
- Broca > - 20% and < + 20%
Exclusion Criteria
- Any findings of the medical examination (including blood pressure, pulse rate and ECG) deviating from normal and of clinical relevance.
- Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal (including thyroid) disorder
- Surgery of the gastro-intestinal tract (except appendectomy)
- Disease of the central nervous system (such as epilepsy) or psychiatric 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) (<= 1 month prior to administration or during the trial)
- Use of any drugs which might influence the result of the trial (<= 10 days prior to administration or during the trial)
- Participation in another trial with an investigational drug (<= 2 month prior to administration or during the trial)
- Smoker (> 10 cigarettes or > 3 cigars or >3 pipes/day)
- Inability to refrain from smoking during the period of the study
- Known alcohol (>60 g/day) or drug abuse
- Blood donation (<=1 month prior to administration)
- Excessive physical activities (<5 days prior to administration)
- Any laboratory value outside the normal range of clinical relevance
- History of hemorrhagic diatheses
- History of gastro-intestinal ulcer, perforation or bleeding
- History of bronchial asthma
Study & Design
- Study Type
- INTERVENTIONAL
- Study Design
- PARALLEL
- Arm && Interventions
Group Intervention Description BIBB 1464 MS single rising dose fed BIBB 1464 MS tablet - BIBB 1464 MS tablet fasted BIBB 1464 MS tablet - BIBB 1464 MS solution fasted BIBB 1464 MS solution - BIBB 1464 MS single rising dose fed Standard dinner - BIBB 1464 MS placebo BIBB 1464 MS placebo -
- Primary Outcome Measures
Name Time Method Maximum drug plasma concentration (Cmax) Up to 38 hours after drug administration Time to reach the maximum concentration of the analyte in plasma (tmax) Up to 38 hours after drug administration Total area under the plasma drug concentration-time curve (AUC) Up to 38 hours after drug administration Apparent terminal half-life of the analyte in plasma (t1/2) Up to 38 hours after drug administration Total plasma clearance divided by the systemic availability factor (CL/f) Up to 38 hours after drug administration Dose normalized AUC0-38h ( NAUC0-38h) Up to 38 h after drug administration Mean residence time, total (MRTtot) Up to 38 hours after drug administration Number of patients with adverse events Up to 72 hours after last drug administration Number of patients with clinical significant findings in vital signs Up to 38 hours after drug administration Number of patients with clinical significant findings in electrocardiogram (ECG) Up to 38 hours after drug administration Number of patients with clinical significant findings in physical examination Up to 38 hours after drug administration Investigator assessed tolerability on a 4 point scale Up to 38 hours after drug administration Monoepoxysqualene (MES) plasma concentration Up to 38 hours after drug administration Amount of drug excreted in urine Up to 38 h after drug administration
- Secondary Outcome Measures
Name Time Method