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
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
DOUBLE
Enrollment
55
Number of participants with adverse events
Time frame: Up to 16 days after drug administration
Number of participants with clinically significant changes in vital signs
Time frame: Up to 16 days after drug administration
Number of participants with abnormal changes in clinical laboratory parameters
Time frame: Up to 16 days after drug administration
Number of participants with abnormal findings in 12-lead ECG (electrocardiogram)
Time frame: Up to 16 days after drug administration
Number of participants with abnormal findings in physical examination
Time frame: Screening and up to 16 days after drug administration
Cmax (maximum concentration in plasma)
Time frame: Up to 360 hours after drug administration
tmax (time from dosing to maximum concentration)
Time frame: 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)
Time frame: 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)
Time frame: Up to 360 hours after drug administration
λz (terminal rate constant in plasma)
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Time frame: Up to 360 hours after drug administration
t1/2 (terminal half-life of the analyte in plasma)
Time frame: Up to 360 hours after drug administration
MRT(mean residence time of the analyte in the body)
Time frame: Up to 360 hours after drug administration
CL/F (apparent oral clearance in plasma after oral administration)
Time frame: Up to 360 hours after drug administration
Vz/F (apparent volume of distribution during the terminal phase λz) dose)
Time frame: Up to 360 hours after drug administration
Ae0-48 (amount of analyte that is eliminated in urine from 0-48 hours)
Time frame: Up to 48 hours after drug administration
fe0-48 (fraction of analyte eliminated in urine from 0-48 hours)
Time frame: Up to 48 hours after drug administration
CLR,0-48 (renal clearance of the analyte from 0-48 hours)
Time frame: Up to 48 hours after drug administration
Receptor occupancy as determined by binding of anti-LFA-1 antibody fragment (Fab)
Time frame: Up to 360 hours after drug administration
Inhibition of IL-2 production
in response to superantigen challenge ex vivo
Time frame: Up to 360 hours after drug administration