Clinical trial NCT02268760: Safety, Tolerance, and Pharmacokinetics of BILN 2061 ZW in Healthy Male Subjects, Combined With Preliminary Evaluation of Food Effect
Official title: Safety, Tolerance, and Pharmacokinetics of Single Oral Doses of 5 mg, 20 mg, 60 mg, 100 mg, 200 mg, 400 mg, 600 mg, 800 mg, 1000 mg, 1200 mg, 1500 mg, 2000 mg and 2400 mg BILN 2061 ZW (PEG 400: Ethanol Solution) in Healthy Male Subjects, Combined With Preliminary Evaluation of Food Effect of the Dose of 200 mg (Two-Stage Trial Design With Randomised Double Blind Placebo Controlled Rising Dose Part and Subsequent Open Intraindividual Comparison Part)
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Healthy
Lead sponsor: Boehringer Ingelheim
Sponsor class: INDUSTRY
First posted: 2014-10-20
Enrollment: 103
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: To assess the safety, tolerance and pharmacokinetics of 5 mg to 2400 mg BILN 2061 ZW

1. In rising single doses
2. With and without a 64 g fat breakfast at one selected dose


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
* Broca ≥ - 20 % and ≤ + 20 %

Exclusion Criteria:

* Any finding of the medical examination (including blood pressure, pulse rate and ECG) deviating from normal and of clinical relevance
* History or current gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunologic, hormonal disorders, including a history of viral hepatitis, or serological evidence of active Hepatitis B or Hepatitis C infection
* History of orthostatic hypotension, fainting spells and blackouts
* Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or neurological 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) within 1 month prior to administration
* Use of any drugs which might influence the results of the trial within 10 days prior to administration or during the trial
* Participation in another trial with an investigational drug within 1 month prior to administration or during the trial
* Smoker (\> 10 cigarettes or 3 cigars or 3 pipes/day) or inability to refrain from smoking on trial days
* Alcohol abuse (\> 60 g/day)
* Drug abuse
* Blood donation within 1 month prior to administration or during the trial
* Excessive physical activities within 5 days prior to administration or during the trial
* Any laboratory value outside the clinically accepted reference range and of clinical relevance
* History of any familial bleeding disorder

Primary outcomes:
measure: Number of patients with clinically relevant changes in vital signs (systolic and diastolic blood pressure, pulse rate)
timeFrame: Pre-dose, up to 48 hours after drug administration
measure: Changes from baseline in laboratory tests
timeFrame: Pre-dose and 48 hours after drug administration
measure: Number of patients with clinically relevant changes in 12-lead ECG
timeFrame: Pre-dose, up to 48 hours after drug administration
measure: Changes from baseline in physical examination
timeFrame: Pre-dose and 48 hours after drug administration
measure: Number of patients with adverse events
timeFrame: Up to 48 hours after drug administration
measure: Global assessment of tolerability by the investigator on a 4-point scale
timeFrame: Up to 48 hours after drug administration
measure: Maximum concentration of the analyte in plasma after a single dose administration (Cmax)
timeFrame: up to 48 hours after drug administration
measure: Area under the concentration-time curve of the analyte in plasma from time 0 to infinity (AUC0-infinity)
timeFrame: up to 48 hours after drug administration
measure: Time to reach Cmax following a single dose administration (tmax)
timeFrame: up to 48 hours after drug administration
measure: Elimination half-life of the analyte in plasma (t1/2)
timeFrame: up to 48 hours after drug administration
measure: Total oral clearance of the analyte from plasma after oral administration, divided by F (bioavailability factor) (CL/F)
timeFrame: up to 48 hours after drug administration
measure: Total mean residence time of the analyte in plasma (MRT)
timeFrame: up to 48 hours after drug administration
measure: Apparent volume of distribution during the terminal elimination phase (Vz/F)
timeFrame: up to 48 hours after drug administration
measure: Amount of intact drug excreted in urine (Au)
timeFrame: up to 48 hours after drug administration
Secondary outcomes:
Other outcomes:
Locations:
Study officials:
References: