Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Study to determine the pharmacokinetics (PK) of BI 201335 and total radioactivity including excretion mass balance, excretion pathways and metabolism following the oral administration of [14C]-BI 201335 at steady state.
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
| Label | Type | Description | Intervention Names |
|---|---|---|---|
| BI 201335 NA | Experimental | multiple doses of BI 201335 NA soft gelatin capsule on days 1-8 and 11-15 and one single dose of [14C]-BI 201335 NA radiolabelled drug on day 9 |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| BI 201335 NA soft gelatin capsule | Drug |
| ||
| [14C]-BI 201335 NA radiolabelled drug |
| Measure | Description | Time Frame |
|---|---|---|
| Individual concentration-time profiles of [14C]-radioactivity in whole blood, plasma, saliva, urine, and faeces | up to 28 days | |
| Individual concentration-time profiles of BI 201335 ZW in plasma and urine | up to 28 days | |
| Rate and extent of excretion mass balance based on the total radioactivity in urine and faeces | up to 28 days | |
| Elucidation of metabolite structures and identification of major metabolites in urine, faeces, and plasma in comparison with various animal species | up to 28 days | |
| Cblood cell/Cplasma ratio of [14C]-radioactivity | up to 28 days | |
| Measurement of the plasma protein binding of total [14C]-radioactivity in human plasma samples ex vivo | up to day 28 | |
| Cmax,ss (maximum measured concentration of the analyte in plasma at steady state over a uniform dosing interval τ) | up to day 28 | |
| tmax,ss (time from last dosing to maximum concentration of the analyte in plasma at steady state) | up to day 28 | |
| Cmin,ss (minimum concentration of the analyte in plasma at steady state over a uniform dosing interval τ) | up to day 28 | |
| AUCτ,ss (area under the concentration-time curve of the analyte in plasma at steady state over a uniform dosing interval τ) |
| Measure | Description | Time Frame |
|---|---|---|
| Number of patients with abnormal findings in physical examination | Baseline and day 28 | |
| Number of patients with clinically significant changes in vital signs (blood pressure, pulse rate) | Baseline, day 1, 10, 16 and 28 |
Not provided
Inclusion Criteria:
Exclusion Criteria:
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
| Drug |
|
| up to day 28 |
| λz,ss (terminal rate constant of the analyte in plasma at steady state) | up to day 28 |
| t1/2,ss (terminal half-life of the analyte in plasma at steady state) | up to day 28 |
| MRTpo,ss (mean residence time of the analyte in the body at steady state after oral administration) | up to day 28 |
| CL/F,ss (apparent clearance of the analyte in the plasma at steady state following multiple oral dose administration) | up to day 28 |
| Vz/F,ss (apparent volume of distribution of the analyte during the terminal phase λz at steady state following oral administration) | up to day 28 |
| Ae,urine,0-tz,ss (amount of analyte that is eliminated in urine at steady state from the time point 0 to time point tz) | up to day 28 |
| fe,urine,t1-t2,ss (fraction of the analyte in % of dose that is eliminated in urine at steady state from the time point 0 to time point tz) | up to day 28 |
| Ae,feces,t1-t2,ss (fraction of the analyte that is eliminated in faeces at steady state from time point 0 to time point tz) | up to day 28 |
| fe,feces,0-tz,ss (fraction of the analyte eliminated in faeces at steady state from time point 0 to time point tz) | up to day 28 |
| CLR,t1-t2,ss (renal clearance of the analyte at steady state from the time point 0 to time point tz) | up to day 28 |
| Number of patients with clinically significant changes in 12-lead electrocardiogram (ECG) | Baseline, day 1, 10, 16 and 28 |
| Number of patients with clinically significant changes in clinical laboratory tests (haematology, clinical chemistry, urinalysis) | Baseline, day 10 and 28 |
| Number of patients with adverse events | up to 28 days |
| Assessment of tolerability on a 4-point scale by the investigator | Day 28 |