The main objective of this trial is to investigate the basic pharmacokinetics of BI 1358894 and its metabolites, total radioactivity, including mass balance, excretion pathways and metabolism following a single oral dose of \[14C\] BI 1358894 in Part 1 and to investigate the pharmacokinetics of BI 1358894 and its metabolite(s) following multiple-dose treatment over 21 days with non- radiolabelled compound of BI 1358894 in Part 2.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
15
Part 1
Part 2
ICON
Groningen, Netherlands
Part 1: Mass Balance and Recoveries of [14C] BI 1358894 Total Radioactivity in Urine and Faeces After Single Oral Dose (Fe0-tz)
Mass balance and recoveries of \[14C\] BI 1358894 total radioactivity in urine and faeces after single oral dose as percentage of the administered dose over the time interval from 0 to tz, where tz is the latest quantifiable data point across all participants. Urine collection intervals were within 2 hours (h) predose, 0-4, 4-8, 8-12, 12-24, 24-48, 48-72, 72-96, 96-120, 120-144, 144-168, 168-192, 192-216, 216-240, 240-264, 264-288, 288-312, 312-336 h after dosing on Day 1 and to be continued in 24 h intervals, on days 21-22, 28-29, 35-36, 42-43, and 49-50, if necessary. Faeces collection intervals were started from approximately -48 h before drug administration and 0-24, 24-48, 48-72, 72-96, 96-120, 120-144, 144-168, 168-192, 192-216, 216-240, 240-264, 264-288, 288-312, 312-336 h after dosing on Day 1 and to be continued in 24 h intervals, on days 21-22, 28-29, 35-36, 42-43, and 49-50, if necessary.
Time frame: From within 2 hours predose up to 50 days after dosing. For detailed time frames please refer to the intervals given under "measure description" above.
Part 1: Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz)
Area under the concentration-time curve of the analyte in plasma over the time interval from 0 to the last quantifiable data point (AUC0-tz) were determined for total \[14C\] BI 1358894 and non-radiolabeled BI 1358894 after single dose administration.
Time frame: At 2 hours (h) before first drug administration and at 20 minutes (min), 40min, 1h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h, 48h, 72h, 96h, 120h, 144h, 192h, 240h, 288h, 336h, 485h, 653h after first drug administration.
Part 1: Maximum Measured Concentration of the Analyte in Plasma (Cmax)
Maximum measured concentration of the analyte in plasma (Cmax) determined for total \[14C\] BI 1358894 and non-radiolabeled BI 1358894 after single dose administration.
Time frame: At 2 hours (h) before first drug administration and at 20 minutes (min), 40min, 1h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h, 48h, 72h, 96h, 120h, 144h, 192h, 240h, 288h, 336h, 485h, 653h after first drug administration.
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Part 2: Area Under the Concentration-time Curve of Non-radiolabeled BI 1358894 in Plasma Over the Time Interval From 0 to 24 (AUC0-24)
Area under the concentration-time curve of the analyte in plasma over the time interval from 0 to 24 hours(AUC0-24) was determined for non-radiolabeled BI 1358894.
Time frame: At 2 hours (h) before first drug administration and at 30 minutes (min), 1h, 2h, 4h, 5h, 6h, 7h, 8h, 10h, 12h, 14h and 24h after first drug administration.
Part 2: Maximum Measured Concentration of Non-radiolabeled BI 1358894 in Plasma (Cmax)
Maximum measured concentration of the analyte in plasma (Cmax) was determined for non-radiolabeled BI 1358894.
Time frame: At 2 hours (h) before first drug administration and at 30 minutes (min), 1h, 2h, 4h, 5h, 6h, 7h, 8h, 10h, 12h, 14h and 24h after first drug administration.
Part 2: Area Under the Concentration-time Curve of Non-radiolabeled BI 1358894 in Plasma at Steady State Over a Uniform Dosing Interval τ (AUCτ,ss)
Area under the concentration-time curve of the analyte in plasma at steady state over a uniform dosing interval τ (AUCτ,ss) was determined for non-radiolabeled BI 1358894. Tau = 24 hours.
Time frame: At 480h, 480.5h, 481h, 482h, 484h, 485h, 486h, 487h,488h, 490h, 492h, 494h and 504h after first drug administration.
Part 2: Maximum Measured Concentration of Non-radiolabeled BI 1358894 in Plasma at Steady State Over a Uniform Dosing Interval τ (Cmax,ss)
Maximum measured concentration of the analyte in plasma at steady state over a uniform dosing interval τ (Cmax,ss) was determined for non-radiolabeled BI 1358894. Tau = 24 hours.
Time frame: At 480h, 480.5h, 481h, 482h, 484h, 485h, 486h, 487h,488h, 490h, 492h, 494h and 504h after first drug administration.