Clinical trial NCT02183662: Safety and Pharmacokinetics of Single Rising Oral Doses of BI 224436 ZW in Healthy Male Volunteers.
Official title: Safety and Pharmacokinetics of Single Rising Oral Doses of BI 224436 ZW at 6.2 mg, 12.5 mg, 25 mg, 50 mg, 100 mg, 200 mg, 400 mg, 600 mg, 900 mg and 1200 mg Dose Levels in Healthy Male Volunteers (Randomized, Double-blind, Placebo-controlled Within Dose Groups)
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Healthy
Lead sponsor: Boehringer Ingelheim
Sponsor class: INDUSTRY
First posted: 2014-07-08
Enrollment: 105
Sex: MALE
Minimum age (years): 21
Maximum age (years): 50
Standard ages: ADULT
Accepts healthy volunteers: yes
Allocation: RANDOMIZED
Intervention model: CROSSOVER
Primary purpose: TREATMENT

Brief summary: To investigate safety and pharmacokinetics of BI 224436 ZW


Eligibility criteria: Inclusion Criteria:

1. Healthy males
2. Age ≥21 and Age ≤50 years
3. Body Mass Index (BMI) ≥18.5 and BMI ≤29.9 kg/m2
4. 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:

1. Any finding of the medical examination (including blood pressure (BP), pulse rate (PR) and electrocardiogram (ECG)) deviating from normal and of clinical relevance
2. Any evidence of a clinically relevant concomitant disease
3. Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders
4. Surgery of the gastrointestinal tract (except appendectomy)
5. Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or neurological disorders
6. History of relevant orthostatic hypotension, fainting spells or blackouts
7. HIV infection and other chronic or relevant acute infections
8. History of relevant allergy/hypersensitivity (including allergy to drug or its excipients)
9. Intake of drugs with a long half-life (\>24 hours) within at least one month or less than 10 half-lives of the respective drug prior to administration or during the trial
10. Use of drugs which might reasonably influence the results of the trial within 10 days prior to administration or during the trial
11. Participation in another trial with an investigational drug within one month prior to administration or during the trial
12. Smoker (\>10 cigarettes or \>3 cigars or \>3 pipes/day)
13. Inability to refrain from smoking on trial days
14. Alcohol abuse (more than 60 g/day)
15. Drug abuse
16. Blood donation (more than 100 mL within four weeks prior to administration or during the trial)
17. Excessive physical activities (within one week prior to administration or during the treatment period)
18. Any laboratory value outside the reference range that is of clinical relevance
19. A baseline prolongation of QT/QTc interval (e.g., a QTc interval ≥450 ms)
20. A history of additional risk factors for Torsades de points (TdP) (e.g., heart failure, hypokalemia, family history of Long QT Syndrome)
21. Bradycardia (PR \<60 beats/min)

Primary outcomes:
measure: maximum measured concentration of the analyte in plasma
timeFrame: up to 72 hours
measure: area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to 24
timeFrame: up to 24 hours
Secondary outcomes:
measure: area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity
timeFrame: up to 72 hours
measure: minimum observed concentration at 24 hours
timeFrame: up to 24 hours
measure: terminal half-life of the analyte in plasma
timeFrame: up to 72 hours
measure: time from dosing to maximum measured concentration of the analyte in plasma
timeFrame: up to 72 hours
measure: apparent clearance of the analyte in plasma
timeFrame: up to 72 hours
measure: apparent volume of distribution during the terminal phase λz
timeFrame: up to 72 hours
measure: apparent volume of distribution
timeFrame: up to 72 hours
measure: mean residence time of the analyte in the body after single oral administration
timeFrame: up to 72 hours
measure: terminal rate constant in plasma
timeFrame: up to 72 hours
measure: the last measurable concentration in the concentration-time profile
timeFrame: up to 72 hours
measure: the extrapolated Area under the curve from the time of the last measurable concentration in the concentration-time profile to infinity
timeFrame: up to 72 hours
measure: the percentage of the Area under the concentration-time curve until infinity, that is determined by extrapolation
timeFrame: up to 72 hours
measure: amount of analyte that is eliminated in urine from the time point t0 to time point t4
timeFrame: up to 4 hours
measure: amount of analyte that is eliminated in urine from the time point t4 to time point t8
timeFrame: from 4 to 8 hours
measure: amount of analyte that is eliminated in urine from the time point t8 to time point t12
timeFrame: from 8 to 12 hours
measure: amount of analyte that is eliminated in urine from the time point t12 to time point t24
timeFrame: from 12 to 24 hours
measure: fraction of analyte eliminated in urine from time point t0 to time point t24
timeFrame: up to 24 hours
measure: renal clearance of the analyte from the time point t0 until the time point t24
timeFrame: up to 24 hours
Other outcomes:
Locations:
Study officials:
References: