A Safety, Tolerability and Preliminary Pharmacokinetics of BILR 355 BS Single-rising Dose Study in Healthy Male Volunteers

Study Overview
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Brief Summary
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Assessment of safety, tolerability and preliminary pharmacokinetics in healthy male volunteers after oral administration of BILR 355 BS

Official Title
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A Double-blind (at Each Dose Level), Randomised, Placebo-controlled Single Increasing Dose Safety, Tolerability and Preliminary Pharmacokinetics Study in Healthy Male Volunteers After Oral Administration of BILR 355 BS Solved in PEG 400 (Dosage: 1 - 200 mg)

Conditions
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Healthy

Intervention / Treatment
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* Drug: BILR 355 BS
* Drug: PEG 400


Participation Criteria
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Eligibility Criteria
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Inclusion Criteria: All participants in the study should be healthy males, ranging from 21 to 50 years of age and their body mass index (BMI) be within 18.5 to 29.9 kg/m2 (BMI calculation: weight in kilograms divided by the square of height in meters). In accordance with Good clinical practice (GCP) and the local legislation all volunteers will have given their written informed consent prior to admission to the study Exclusion Criteria: Any finding 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 disorders Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or neurological disorders 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) within at least one month or less than ten half-lives of the respective drug before enrolment in the study or during the study Use of any drugs which might influence the results of the trial up to 7 days prior to enrolment in the study or during the study Participation in another trial with an investigational drug (≤ two months prior to administration or during the trial) Smoker (> 10 cigarettes or > 3 cigars of > 3 pipes/day) Inability to refrain from smoking on trial days Alcohol abuse (> 60 g/day) Drug abuse Blood donation (≥ 100 mL within four weeks prior to administration or during the trial) Any laboratory value outside the clinically accepted reference range Excessive physical activities within the last week before the trial or during the trial Following exclusion criteria are of special interest for this study: - Erythema, exanthema and comparable skin alterations

Ages Eligible for Study
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Minimum Age: 21 Years
Maximum Age: 50 Years

Sexes Eligible for Study
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Male

Accepts Healthy Volunteers
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Accepts Healthy Volunteers

Study Plan
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How is the study designed?
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Design Details

Primary Purpose: Treatment
Allocation: Randomized
Intervention Model: Parallel Assignment
Masking: Double


Arms and Interventions

| Participant Group/Arm | Intervention/Treatment |
| --- | --- |
| Experimental: BILR 355 BS<br>escalating doses | Drug: BILR 355 BS<br> <br> Drug: PEG 400<br> <br> |
| Placebo Comparator: Placebo<br> | Drug: PEG 400<br> <br> |

What is the study measuring?
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Primary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| Number of participants with clinically significant changes in vital functions |  | Up to 10 days after drug administration | 
| Number of participants with abnormal findings in ECG (electrocardiogram) |  | Up to 10 days after drug administration | 
| Number of participants with abnormal findings in skin inspections |  | Up to 10 days after drug administration | 
| Number of participants with abnormal neurological finding |  | Up to 10 days after drug administration | 
| Number of participants with abnormal changes in laboratory parameters |  | Up to 10 days after drug administration | 
| Number of participants with positive faecal occult blood testing |  | Up to 10 days after drug administration | 
| Number of participants with adverse events |  | Up to 10 days after drug administration | 

Secondary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| Maximum plasma concentration (Cmax) |  | Up to 144 hours after drug administration | 
| Time to attain maximum plasma concentration (tmax) |  | Up to 144 hours after drug administration | 
| Area under the concentration-time curve of the analyte in plasma from zero time to infinity (AUC0-∞) |  | Up to 144 hours after drug administration | 
| Terminal half life (t½) |  | Up to 144 hours after drug administration | 
| Apparent clearance of the analyte in plasma following extravascular administration (CL/F) |  | Up to 144 hours after drug administration | 
| Total mean residence time (MRTtot) |  | Up to 144 hours after drug administration | 
| Apparent volume of distribution during the terminal elimination phase (Vz/F) |  | Up to 144 hours after drug administration | 
| Renal clearance of the analyte (CLR) |  | Up to 72 hours after drug administration | 
| Amount of drug excreted in the urine (Ae) |  | Up to 72 hours after drug administration | 
| Area under the concentration-time curve of the analyte in plasma from zero time to the time of the last quantifiable drug concentration (AUC0-tz) |  | Up to 144 hours after drug administration |