Clinical trial NCT02229838: Safety/Tolerability, Pharmacokinetics, and Pharmacodynamics of BIBB 1464 MS in Healthy Male Subjects, Combined With Preliminary Evaluation of Relative Bioavailability and Effect of Food
Official title: Safety/Tolerability, Pharmacokinetics, and Pharmacodynamics of Single Oral Doses of 0.25 mg, 0.75 mg, 2 mg, 6 mg, and 10 mg BIBB 1464 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)
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Healthy
Lead sponsor: Boehringer Ingelheim
Sponsor class: INDUSTRY
First posted: 2014-09-01
Enrollment: 73
Sex: MALE
Minimum age (years): 19
Maximum age (years): 54
Standard ages: ADULT
Accepts healthy volunteers: yes
Allocation: RANDOMIZED
Intervention model: PARALLEL
Primary purpose: TREATMENT

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).


Eligibility criteria: 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

Primary outcomes:
measure: Maximum drug plasma concentration (Cmax)
timeFrame: Up to 38 hours after drug administration
measure: Time to reach the maximum concentration of the analyte in plasma (tmax)
timeFrame: Up to 38 hours after drug administration
measure: Total area under the plasma drug concentration-time curve (AUC)
timeFrame: Up to 38 hours after drug administration
measure: Apparent terminal half-life of the analyte in plasma (t1/2)
timeFrame: Up to 38 hours after drug administration
measure: Total plasma clearance divided by the systemic availability factor (CL/f)
timeFrame: Up to 38 hours after drug administration
measure: Dose normalized AUC0-38h ( NAUC0-38h)
timeFrame: Up to 38 h after drug administration
measure: Mean residence time, total (MRTtot)
timeFrame: Up to 38 hours after drug administration
measure: Number of patients with adverse events
timeFrame: Up to 72 hours after last drug administration
measure: Number of patients with clinical significant findings in vital signs
timeFrame: Up to 38 hours after drug administration
measure: Number of patients with clinical significant findings in electrocardiogram (ECG)
timeFrame: Up to 38 hours after drug administration
measure: Number of patients with clinical significant findings in physical examination
timeFrame: Up to 38 hours after drug administration
measure: Investigator assessed tolerability on a 4 point scale
timeFrame: Up to 38 hours after drug administration
measure: Monoepoxysqualene (MES) plasma concentration
timeFrame: Up to 38 hours after drug administration
measure: Amount of drug excreted in urine
timeFrame: Up to 38 h after drug administration
Secondary outcomes:
Other outcomes:
Locations:
Study officials:
References: