Study to assess safety, tolerability and pharmacokinetics of BIRB 1017 BS in single rising oral doses of 5 to 800 mg in a polyethylene glycol 400 (PEG 400) / 26% ethanol solution in healthy male subjects
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
DOUBLE
Enrollment
48
PEG 400
Assessment of safety and tolerability by the investigator on a 4-point scale
Time frame: at day 5-10
Number of patients with adverse events
Time frame: up to 25 days
Number of patients with clinically significant changes in vital signs (pulse rate, systolic and diastolic blood pressure)
Time frame: up to day 10
Number of patients with abnormal changes in clinical laboratory tests
Time frame: up to day 10
Number of patients with clinically relevant effect on electrocardiogram parameters
Time frame: up to day 10
Maximum concentration of BIRB 1017 BS in plasma (Cmax)
Time frame: pre-dose and 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 12:00, 15:00, 24:00, 34:00, and 48:00 hours after administration of study drug
Time from dosing to maximum concentration (tmax)
Time frame: pre-dose and 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 12:00, 15:00, 24:00, 34:00, and 48:00 hours after administration of study drug
Area under the concentration-time curve of the analyte in plasma ofer the time interval from 0 to the last quantifiable analyte plasma concentration (AUC0-infinity)
Time frame: pre-dose and 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 12:00, 15:00, 24:00, 34:00, and 48:00 hours after administration of study drug
Area under the concentration-time curve of the analyte in plasma over the time interval from 0 to the last quantifiable analyte plasma concentration (AUC0-tz)
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Time frame: pre-dose and 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 12:00, 15:00, 24:00, 34:00, and 48:00 hours after administration of study drug
Terminal elimination rate constant in plasma (λz)
Time frame: pre-dose and 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 12:00, 15:00, 24:00, 34:00, and 48:00 hours after administration of study drug
Terminal half-life of the analyte in plasma (t1/2)
Time frame: pre-dose and 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 12:00, 15:00, 24:00, 34:00, and 48:00 hours after administration of study drug
Mean residence time of the analyte in the body (MRT)
Time frame: pre-dose and 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 12:00, 15:00, 24:00, 34:00, and 48:00 hours after administration of study drug
Apparent oral clearance of the analyte in the plasma after oral administration (CL/F)
Time frame: pre-dose and 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 12:00, 15:00, 24:00, 34:00, and 48:00 hours after administration of study drug
Apparent volume of distribution during the terminal phase λz following an oral dose (Vz/F)
Time frame: pre-dose and 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 12:00, 15:00, 24:00, 34:00, and 48:00 hours after administration of study drug