Safety and Pharmacokinetics of Single Rising Oral Doses of BI 224436 ZW in Healthy Male Volunteers.

Phase 1

Completed

• Conditions: Healthy
• Interventions: Drug: BI 224436; Drug: Placebo to BI 224436

• Registration Number: NCT02183662
• Lead Sponsor: Boehringer Ingelheim

Brief Summary

To investigate safety and pharmacokinetics of BI 224436 ZW

Detailed Description

Not available

Study Timeline

• Study Start: 2009-11
• Primary Completion: 2010-03
• Status Verified: 2014-07
• Study First Submitted: 2014-07-07
• Study First Submitted QC: 2014-07-07
• Last Update Submitted: 2014-07-07
• Study First Posted: 2014-07-08
• Last Update Posted: 2014-07-08

Recruitment & Eligibility

• Status: COMPLETED
• Sex: Male
• Target Recruitment: 105

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)

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: CROSSOVER

Arm && Interventions

Group	Intervention	Description
BI 224436	BI 224436	-
Placebo	Placebo to BI 224436	-

Primary Outcome Measures

Name	Time	Method
maximum measured concentration of the analyte in plasma	up to 72 hours
area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to 24	up to 24 hours

Secondary Outcome Measures

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