Safety and Pharmacokinetics of BIRB 796 BS Tablets Administered to Healthy Human Subjects

Study Overview
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Brief Summary
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Study to assess the safety and pharmacokinetics of BIRB 796 BS tablets administered as multiple daily doses at various dose levels.

Official Title
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Safety and Pharmacokinetics of BIRB 796 BS Tablets Administered Twice Daily Orally (Total Daily Dose 30, 60, and 120 mg) to Healthy Human Subjects for 14 Days. A Double-blind, Placebo-controlled, Parallel Group Study.

Conditions
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Healthy

Intervention / Treatment
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* Drug: BIRB 796 BS, low dose
* Drug: BIRB 796 BS, high dose
* Drug: Placebo


Participation Criteria
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Eligibility Criteria
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Inclusion Criteria: Healthy male subjects as determined by results of screening Signed written informed consent in accordance with Good Clinical Practice and local legislation Age >= 18 and <= 45 years Broca >= - 20 % and <= + 20% Able to communicate well with the investigator and to comply with study requirements > 10 elimination half lives present since last use of any investigational drug for that investigational drug Laboratory values within a clinically relevant reference range Exclusion Criteria: Any finding of the medical examination (including blood pressure, pulse rate, temperature, and EKG) deviating from normal and of clinical relevance Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders Surgery of gastrointestinal tract (except appendectomy) 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 History of vasculitis (past history of fever, malaise, myalgias, rash, etc.) 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 administration or during the trial) Participation in another trial with an investigational drug (< 1 months prior to administration or during trial) Smoker Inability to refrain from smoking on trial days Alcohol abuse (> 60 g/day) Drug abuse Use of methylxanthine-containing drinks or foods (coffee, tea, cola, energy drinks, chocolate, etc.) < one week prior to administration of study drug Blood donation or loss > 400 mL (< 1 month prior to administration or during the trial) Excessive physical activities (< 5 days prior to administration or during the trial) Following specific laboratory findings: total white blood cell >= 10 x 109/L, C-Reactive Protein >= 4.5 mg/L, gamma-glutamyl-transferase >= 25 U/L, aspartate transaminase >= 16 U/L, alanine transaminase >= 20 U/L any erythrocytes or > 15 mg/dl protein on urine dipstick Any EKG value outside of the reference range of clinical relevance including, but not limited to QTcB > 480 ms, PR interval > 240 ms, QRS interval > 110 ms History of any familial bleeding disorder Inability to comply with dietary regimen of study centre Inability to comply with investigator's instructions

Ages Eligible for Study
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Minimum Age: 18 Years
Maximum Age: 45 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: BIRB 796 BS, low dose<br> | Drug: BIRB 796 BS, low dose<br> <br> |
| Experimental: BIRB 796 BS, high dose<br> | Drug: BIRB 796 BS, high dose<br> <br> |
| Placebo Comparator: Placebo<br> | Drug: Placebo<br> <br> |
| Experimental: BIRB 796 BS, medium dose<br> | Drug: BIRB 796 BS, low dose<br> <br> Drug: BIRB 796 BS, high dose<br> <br> |

What is the study measuring?
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Primary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| Number of patients with clinically significant changes in vital signs |  | up to 21 days | 
| Number of patients with clinically significant changes in laboratory parameters |  | up to 21 days | 
| Number of patients with abnormal findings in electrocardiogram |  | up to 21 days | 
| Number of patients with adverse events |  | up to 24 days | 

Secondary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| Maximum concentration of the analyte in plasma (Cmax) for several time points |  | up to 36 hours after dosing | 
| Area under the plasma concentration versus time curve (AUC) for several time points |  | up to 36 hours after dosing | 
| Time at which maximum plasma concentration occurred over a dosing interval (tmax) |  | up to 36 hours after dosing | 
| Terminal elimination rate constant (λZ) |  | up to 36 hours after dosing | 
| Elimination half-life (t1/2) |  | up to 36 hours after dosing | 
| Mean residence time (MRT) |  | up to 36 hours after dosing | 
| Apparent oral clearance (CL/F) |  | up to 36 hours after dosing | 
| Apparent volume of distribution during the terminal elimination phase, divided by F (bioavailability factor) (Vz/F) |  | up to 36 hours after dosing |