Clinical trial NCT02184338: Safety, Tolerability, and Pharmacokinetics of Single Rising Oral Doses of BIRB 1017 BS as a Solution in PEG 400 / 26% Ethanol Administered to Healthy Male Subjects
Official title: Safety, Tolerability, and Pharmacokinetics of Single Rising Oral Doses of BIRB 1017 BS (5, 25, 100, 250, 500, and 800 mg) as a Solution in PEG 400 / 26% Ethanol Administered to Healthy Male Subjects. Placebo Controlled and Blinded at Each Dose Level
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Healthy
Lead sponsor: Boehringer Ingelheim
Sponsor class: INDUSTRY
First posted: 2014-07-09
Enrollment: 48
Sex: MALE
Minimum age (years): 18
Maximum age (years): 50
Standard ages: ADULT
Accepts healthy volunteers: yes
Allocation: RANDOMIZED
Intervention model: PARALLEL
Primary purpose: TREATMENT

Brief summary: Study to assess safety, tolerability and pharmacokinetics of BIRB 1017 BS in single rising oral doses of 5 to 800 mg in a polyethylene glycol 400 (PEG 400) / 26% ethanol solution in healthy male subjects


Eligibility criteria: Inclusion Criteria:

* Healthy male subjects as determined by results of screening
* Signed written informed consent in accordance with Good Clinical Practice (GCP) and local legislation
* Age \>= 18 and \<= 50 years
* BMI \>18.5 and \<29.9 kg/m2 (Body Mass Index)

Exclusion Criteria:

* Any finding of the medical examination (including blood pressure, pulse rate, and electrocardiogram) deviating from normal and of clinical relevance
* Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunologic, haematological, oncological or hormonal disorders
* Surgery of gastrointestinal tract (except appendectomy)
* Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or neurological disorders
* Relevant history of orthostatic hypotension, fainting spells or blackouts
* 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 results of the trial (\< 10 days prior to study drug administration or expected during the trial)
* Participation in another trial with an investigational drug (\< 2 months prior to administration or expected during trial)
* Smoker (\> 10 cigarettes or \>3 cigars or \>3 pipes/day)
* Inability to refrain from smoking on trial days
* Alcohol abuse (\> 60 g/day)
* Drug abuse
* Blood donation or loss \> 400 mL, \< 1 month prior to administration or expected during the trial
* Excessive physical activities (within 5 days prior to administration or during the trial)
* Clinically relevant laboratory abnormalities
* Any electrocardiogram value outside of the reference range and of clinical relevance including, but not limited to QRS interval \> 110 ms or QTcB \> 450 ms or QT \>500 ms
* Known hypersensitivity to the drug or its excipients
* Inability to comply with dietary regimen of study centre
* Inability to comply with investigator's instructions

Primary outcomes:
measure: Assessment of safety and tolerability by the investigator on a 4-point scale
timeFrame: at day 5-10
measure: Number of patients with adverse events
timeFrame: up to 25 days
measure: Number of patients with clinically significant changes in vital signs (pulse rate, systolic and diastolic blood pressure)
timeFrame: up to day 10
measure: Number of patients with abnormal changes in clinical laboratory tests
timeFrame: up to day 10
measure: Number of patients with clinically relevant effect on electrocardiogram parameters
timeFrame: up to day 10
Secondary outcomes:
measure: Maximum concentration of BIRB 1017 BS in plasma (Cmax)
timeFrame: pre-dose and 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 12:00, 15:00, 24:00, 34:00, and 48:00 hours after administration of study drug
measure: Time from dosing to maximum concentration (tmax)
timeFrame: pre-dose and 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 12:00, 15:00, 24:00, 34:00, and 48:00 hours after administration of study drug
measure: Area under the concentration-time curve of the analyte in plasma ofer the time interval from 0 to the last quantifiable analyte plasma concentration (AUC0-infinity)
timeFrame: pre-dose and 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 12:00, 15:00, 24:00, 34:00, and 48:00 hours after administration of study drug
measure: Area under the concentration-time curve of the analyte in plasma over the time interval from 0 to the last quantifiable analyte plasma concentration (AUC0-tz)
timeFrame: pre-dose and 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 12:00, 15:00, 24:00, 34:00, and 48:00 hours after administration of study drug
measure: Terminal elimination rate constant in plasma (λz)
timeFrame: pre-dose and 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 12:00, 15:00, 24:00, 34:00, and 48:00 hours after administration of study drug
measure: Terminal half-life of the analyte in plasma (t1/2)
timeFrame: pre-dose and 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 12:00, 15:00, 24:00, 34:00, and 48:00 hours after administration of study drug
measure: Mean residence time of the analyte in the body (MRT)
timeFrame: pre-dose and 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 12:00, 15:00, 24:00, 34:00, and 48:00 hours after administration of study drug
measure: Apparent oral clearance of the analyte in the plasma after oral administration (CL/F)
timeFrame: pre-dose and 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 12:00, 15:00, 24:00, 34:00, and 48:00 hours after administration of study drug
measure: Apparent volume of distribution during the terminal phase λz following an oral dose (Vz/F)
timeFrame: pre-dose and 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 12:00, 15:00, 24:00, 34:00, and 48:00 hours after administration of study drug
Other outcomes:
Locations:
Study officials:
References: