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Study to investigate the basic pharmacokinetics of BI 44370 BS, its metabolite CD 10419 BS, and 14C-radioactivity including mass balance, excretion pathways, and metabolism following a single oral administration of 200 mg [14C]BI 44370 BS to healthy male volunteers and to evaluate safety and tolerability following a single oral administration of 200 mg [14C]BI 44370 BS to healthy male volunteers
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| BI 44370 BS | Experimental | 200 mg containing 2.43 megabecquerel (MBq) 14C-radioactivity |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| BI 44370 BS | Drug |
|
| Measure | Description | Time Frame |
|---|---|---|
| Individual time course profiles of [14C]-radioactivity in whole blood, plasma, urine | in nmoleq/L | up to day 15 |
| Individual time course profiles of [14C]-radioactivity in faeces | in nmoleq/kg | up to day 15 |
| Individual time course profiles of BI 44370 BS (and its glucuronide CD 10419 BS) in plasma and urine | up to 15 days | |
| Rate and extent of excretion mass balance based on the total radioactivity in urine and faeces | up to 15 days | |
| Cblood cells/Cplasma ratio of [14C]-radioactivity | up to 12 hours after drug administration | |
| Cblood /Cplasma ratio of [14C]-radioactivity | up to 144 hours after drug administration | |
| Identification of major metabolites in plasma, urine, and faeces | up to day 15 | |
| Cmax (maximum concentration of the analyte(s) in plasma) | up to 144 hours after drug administration | |
| tmax (time from dosing to the maximum concentration of the analyte(s) in plasma) | up to 144 hours after drug administration | |
| AUC0-tz (area under the concentration-time curve of the analyte(s) in plasma over the time interval from 0 to the time of the last quantifiable data point) |
| Measure | Description | Time Frame |
|---|---|---|
| Number of patients with clinically relevant findings in vital signs | up to 23 days | |
| Number of patients with clinically relevant findings in 12-lead electrocardiogram (ECG) | up to 23 days | |
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Inclusion Criteria:
Exclusion Criteria:
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| up to 144 hours after drug administration |
| AUC0-inf. (area under the concentration-time curve of the analyte(s) in plasma over the time interval from 0 to infinity) | up to 144 hours after drug administration |
| λz (terminal rate constant in plasma) | up to 144 hours after drug administration |
| t1/2 (terminal half-life of the analyte(s) in plasma) | up to 144 hours after drug administration |
| MRTpo (mean residence time of the analyte(s) in the body after oral administration) | up to 144 hours after drug administration |
| CL/F (total clearance of the analyte in plasma after oral administration) | up to 144 hours after drug administration |
| Vz/F (apparent volume of distribution during the terminal phase λz following an oral dose) | up to 144 hours after drug administration |
| Ae0-tz (amount of analyte that is eliminated in urine within the time interval zero to tz, additionally excretion within each sampling interval will be calculated) | up to 15 days |
| fe0-tz (fraction of analyte excreted in urine within the time interval zero to tz in % of dose, additionally excretion within each sampling interval will be calculated) | up to 15 days |
| Aefaeces,0-tz (amount of analyte excreted in faeces within the time interval zero to tz, additionally excretion within each sampling interval will be calculated) | up to 15 days |
| fefaeces,0-tz (fraction of analyte excreted in faeces within the time interval zero to tz in % of dose, additionally excretion within each sampling interval will be calculated) | up to 15 days |
| CLR,t1-t2 (renal clearance of analyte from the within the time interval t1 to t2) | up to 15 days |
| Number of patients with clinically relevant laboratory findings |
| up to 23 days |
| Number of patients with adverse events | up to up to 44 days |
| Assessment of global tolerability on a 4-point scale | day 15 |