Clinical trial NCT02259894: Safety, Pharmacokinetics, and Pharmacodynamics of BIRT 2584 XX in Healthy Male Volunteers
Official title: 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.
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Healthy
Lead sponsor: Boehringer Ingelheim
Sponsor class: INDUSTRY
First posted: 2014-10-09
Enrollment: 55
Sex: MALE
Minimum age (years): 18
Maximum age (years): 50
Standard ages: ADULT
Accepts healthy volunteers: yes
Allocation: RANDOMIZED
Intervention model: PARALLEL
Primary purpose: TREATMENT

Brief summary: 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


Eligibility criteria: 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

Primary outcomes:
measure: Number of participants with adverse events
timeFrame: Up to 16 days after drug administration
measure: Number of participants with clinically significant changes in vital signs
timeFrame: Up to 16 days after drug administration
measure: Number of participants with abnormal changes in clinical laboratory parameters
timeFrame: Up to 16 days after drug administration
measure: Number of participants with abnormal findings in 12-lead ECG (electrocardiogram)
timeFrame: Up to 16 days after drug administration
measure: Number of participants with abnormal findings in physical examination
timeFrame: Screening and up to 16 days after drug administration
Secondary outcomes:
measure: Cmax (maximum concentration in plasma)
timeFrame: Up to 360 hours after drug administration
measure: tmax (time from dosing to maximum concentration)
timeFrame: Up to 360 hours after drug administration
measure: AUC0-∞ (area under the concentration-time curve of the analyte in plasma over the time) interval from 0 extrapolated to infinity)
timeFrame: Up to 360 hours after drug administration
measure: 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)
timeFrame: Up to 360 hours after drug administration
measure: λz (terminal rate constant in plasma)
timeFrame: Up to 360 hours after drug administration
measure: t1/2 (terminal half-life of the analyte in plasma)
timeFrame: Up to 360 hours after drug administration
measure: MRT(mean residence time of the analyte in the body)
timeFrame: Up to 360 hours after drug administration
measure: CL/F (apparent oral clearance in plasma after oral administration)
timeFrame: Up to 360 hours after drug administration
measure: Vz/F (apparent volume of distribution during the terminal phase λz) dose)
timeFrame: Up to 360 hours after drug administration
measure: Ae0-48 (amount of analyte that is eliminated in urine from 0-48 hours)
timeFrame: Up to 48 hours after drug administration
measure: fe0-48 (fraction of analyte eliminated in urine from 0-48 hours)
timeFrame: Up to 48 hours after drug administration
measure: CLR,0-48 (renal clearance of the analyte from 0-48 hours)
timeFrame: Up to 48 hours after drug administration
measure: Receptor occupancy as determined by binding of anti-LFA-1 antibody fragment (Fab)
timeFrame: Up to 360 hours after drug administration
measure: Inhibition of IL-2 production
timeFrame: Up to 360 hours after drug administration
Other outcomes:
Locations:
Study officials:
References: