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To evaluate the safety, tolerability and pharmacokinetics of single rising oral doses of BI 44370 TA in healthy male volunteers, to compare a drinking solution vs. a tablet formulation and to assess intra-individual pharmacokinetic (PK) variability by re-dosing two further doses.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| BI 44370 TA solution | Experimental |
| |
| BI 44370 TA tablet | Experimental |
| |
| Placebo solution | Placebo Comparator |
| |
| Placebo tablet | Placebo Comparator |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| BI 44370 TA solution | Drug |
| ||
| BI 44370 TA tablet |
| Measure | Description | Time Frame |
|---|---|---|
| Number of patients with adverse events | up to 10 days after last drug administration | |
| Number of patients with clinically significant findings in vital signs | up to 10 days after last drug administration | |
| Number of patients with clinically significant findings in laboratory tests | up to 10 days after last drug administration | |
| Number of patients with clinically significant findings in ECG | up to 10 days after last drug administration | |
| Assessment of tolerability by investigator on a 4-point scale | up to 10 days after last drug administration |
| Measure | Description | Time Frame |
|---|---|---|
| Cmax (maximum measured concentration of the analyte in plasma) | up to 72 hours after drug administration | |
| tmax (time from dosing to maximum measured concentration) | up to 72 hours after drug administration |
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Inclusion Criteria:
Healthy males according to the following criteria:
Based upon a complete medical history, including the physical examination, vital signs (BP, PR, RR and body temperature), 12-lead ECG, clinical laboratory tests
Age ≥21 and Age ≤50 years
Body Mass Index (BMI) ≥18.5 and BMI ≤29.9 kg/m2
Signed and dated written informed consent prior to admission to the study in accordance with Good clinical practice (GCP) and the local legislation
Exclusion Criteria:
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| Placebo solution | Drug |
|
| Placebo tablet | Drug |
|
| AUC0-∞ (area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity) | up to 72 hours after drug administration |
| %AUCtz-∞ (the percentage of the AUC0-∞ that is obtained by extrapolation) | up to 72 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 time of the last quantifiable data point) | up to 72 hours after drug administration |
| AUCt1-t2 (area under the concentration-time curve of the analyte in plasma over the time interval t1 to t2) | up to 72 hours after drug administration |
| tz (time of last measurable concentration of the analyte in plasma) | up to 72 hours after drug administration |
| t1/2 (terminal half-life of the analyte in plasma) | up to 72 hours after drug administration |
| MRTp.o. (mean residence time of the analyte in the body after oral administration) | up to 72 hours after drug administration |
| CL/F (total/apparent clearance of the analyte in plasma after extravascular administration) | up to 72 hours after drug administration |
| Vz/F (apparent volume of distribution during the terminal phase tz following an extravascular dose) | up to 72 hours after drug administration |
| λz (the terminal rate constant) | up to 72 hours after drug administration |
| Aet1/t2 (total quantity of analyte excreted in the urine in the time interval from t1 to t2) | up to 24 hours after drug administration |
| fet1/t2 (the fractional excretion of the analyte in the time interval from t1 to t2) | up to 24 hours after drug administration |
| CLR,t1/t2 (the renal clearance of the analyte in the time interval from t1 to t2) | up to 24 hours after drug administration |