Safety, Pharmacokinetics, and Pharmacodynamics of BIRT 2584 XX in Healthy Male Volunteers

Study Overview
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Brief Summary
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To assess safety, tolerability, pharmacokinetics, and pharmacodynamics of BIRT 2584 XX in single rising oral doses of 5 mg to 700 mg in a polyethylene glycol 400 (PEG 400) solution in healthy subjects

Official Title
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Safety, Pharmacokinetics, and Pharmacodynamics of Single Rising Oral Doses of BIRT 2584 XX (5, 30, 100, 200, 350, 500, and 700 mg) as a Solution in PEG 400 Administered to Healthy Male Volunteers. Placebo Controlled and Blinded at Each Dose Level.

Conditions
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Healthy

Intervention / Treatment
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* Drug: BIRT 2584 XX
* 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 (GCP) and local legislation Age >=18 and <=50 years BMI >=18.5 and <=29.9 kg/m2 Exclusion Criteria: Any finding of the medical examination (including blood pressure, pulse rate, and electrocardiogram) deviating from normal and of clinical relevance Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunologic, haematological, oncological or hormonal disorders Surgery of gastrointestinal tract (except appendectomy) Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or neurological disorders Relevant 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) (< 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 study drug administration or expected during the trial) Participation in another trial with an investigational drug (< 2 months prior to administration or expected during trial) Smoker (> 10 cigarettes or >3 cigars or >3 pipes/day) Alcohol abuse (> 60 g/day) Drug abuse Blood donation or loss > 400 mL, < 1 month prior to administration or expected during the trial Clinically relevant laboratory abnormalities Any ECG value outside of the reference range and of clinical relevance including, but not limited to QRS interval > 110 ms or QT interval, Bazett correction (QTcB) > 450 ms or QT interval >500 ms 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: 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: BIRT 2584<br>single rising doses | Drug: BIRT 2584 XX<br> <br> |
| Placebo Comparator: Placebo<br> | Drug: Placebo<br> <br> |

What is the study measuring?
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Primary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| Number of participants with adverse events |  | Up to 16 days after drug administration | 
| Number of participants with clinically significant changes in vital signs |  | Up to 16 days after drug administration | 
| Number of participants with abnormal changes in clinical laboratory parameters |  | Up to 16 days after drug administration | 
| Number of participants with abnormal findings in 12-lead ECG (electrocardiogram) |  | Up to 16 days after drug administration | 
| Number of participants with abnormal findings in physical examination |  | Screening and up to 16 days after drug administration | 

Secondary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| Cmax (maximum concentration in plasma) |  | Up to 360 hours after drug administration | 
| tmax (time from dosing to maximum concentration) |  | Up to 360 hours after drug administration | 
| AUC0-∞ (area under the concentration-time curve of the analyte in plasma over the time) interval from 0 extrapolated to infinity) |  | Up to 360 hours after drug administration | 
| AUC0-tz (area under the concentration-time curve of the analyte in plasma over the time) interval from 0 to the last quantifiable analyte plasma concentration) |  | Up to 360 hours after drug administration | 
| λz (terminal rate constant in plasma) |  | Up to 360 hours after drug administration | 
| t1/2 (terminal half-life of the analyte in plasma) |  | Up to 360 hours after drug administration | 
| MRT(mean residence time of the analyte in the body) |  | Up to 360 hours after drug administration | 
| CL/F (apparent oral clearance in plasma after oral administration) |  | Up to 360 hours after drug administration | 
| Vz/F (apparent volume of distribution during the terminal phase λz) dose) |  | Up to 360 hours after drug administration | 
| Ae0-48 (amount of analyte that is eliminated in urine from 0-48 hours) |  | Up to 48 hours after drug administration | 
| fe0-48 (fraction of analyte eliminated in urine from 0-48 hours) |  | Up to 48 hours after drug administration | 
| CLR,0-48 (renal clearance of the analyte from 0-48 hours) |  | Up to 48 hours after drug administration | 
| Receptor occupancy as determined by binding of anti-LFA-1 antibody fragment (Fab) |  | Up to 360 hours after drug administration | 
| Inhibition of IL-2 production | in response to superantigen challenge ex vivo | Up to 360 hours after drug administration |