The objective of the study was evaluate that there is no clinically relevant interaction between amitriptyline (or its metabolite nortriptyline) and BIRT 2584 XX (or its metabolite BI 610100) when BIRT 2584 XX is administered as a tablet formulation to near steady state in an estimated high therapeutic dose. Pharmacokinetics (PK) of amitriptyline and nortriptyline were measured before dosing of BIRT 2584 XX, after the first dose of BIRT 2584 XX, and after repeated doses of BIRT 2584 XX near steady state
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
24
AUC0-∞ of amitriptyline (area under the concentration-time curve of amitriptyline in plasma over the time interval from 0 extrapolated to infinity)
Time frame: up to 15 days
AUC0-∞ ratio of amitriptyline/nortriptyline
Time frame: up to 15 days
AUC0-∞ of amitriptyline (area under the concentration-time curve of amitriptyline in plasma over the time interval from 0 extrapolated to infinity)
1 hour after BIRT 2584 XX
Time frame: Day 1
Cmax of amitriptyline (maximum concentration of amitriptyline in plasma)
Time frame: up to 15 days
AUC0-∞ of nortriptyline (area under the concentration-time curve of nortriptyline in plasma over the time interval from 0 extrapolated to infinity)
Time frame: up to 15 days
Cmax of nortriptyline (maximum concentration of nortriptyline in plasma)
Time frame: up to 15 days
AUC0-∞ ratio of amitriptyline/nortriptyline
1 hour after BIRT 2584 XX
Time frame: Day 1
AUC0-tz (area under the concentration-time curve of the analytes in plasma over the time interval from 0 to the time of the last quantifiable data point)
Time frame: up to 15 days
tmax (time from dosing to the maximum concentration of the analytes in plasma)
Time frame: up to 15 days
λz (terminal rate constant of the analytes in plasma)
Time frame: up to 15 days
t1/2 (terminal half-life of the analytes in plasma)
Time frame: up to 15 days
MRTpo (mean residence time of the analytes in the body after po administration)
Time frame: up to 15 days
CL/F (apparent clearance of the analytes in the plasma after extravascular administration)
Time frame: up to 15 days
Vz/F (apparent volume of distribution during the terminal phase following an extravascular dose)
Time frame: up to 15 days
Pre-dose levels of BIRT 2584 XX and BI 610100
Time frame: up to 15 days
Number of subjects with adverse events
Time frame: up to 57 days
Number of subjects with abnormal changes in laboratory parameters
Time frame: up to 28 days
Assessment of tolerability by investigator on a 4-point scale
Time frame: Day 28
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