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To assess safety, tolerability, pharmacokinetics, and pharmacodynamics of BIRT 2584 XX in single rising oral doses of 5 mg to 700 mg in a polyethylene glycol 400 (PEG 400) solution in healthy subjects
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| BIRT 2584 | Experimental | single rising doses |
|
| Placebo | Placebo Comparator |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| BIRT 2584 XX | Drug |
| ||
| Placebo |
| Measure | Description | Time Frame |
|---|---|---|
| Number of participants with adverse events | Up to 16 days after drug administration | |
| Number of participants with clinically significant changes in vital signs | Up to 16 days after drug administration | |
| Number of participants with abnormal changes in clinical laboratory parameters | Up to 16 days after drug administration | |
| Number of participants with abnormal findings in 12-lead ECG (electrocardiogram) | Up to 16 days after drug administration | |
| Number of participants with abnormal findings in physical examination | Screening and up to 16 days after drug administration |
| Measure | Description | Time Frame |
|---|---|---|
| Cmax (maximum concentration in plasma) | Up to 360 hours after drug administration | |
| tmax (time from dosing to maximum concentration) | Up to 360 hours after drug administration | |
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Inclusion Criteria:
Exclusion Criteria:
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|
| AUC0-∞ (area under the concentration-time curve of the analyte in plasma over the time) interval from 0 extrapolated to infinity) |
| Up to 360 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 last quantifiable analyte plasma concentration) | Up to 360 hours after drug administration |
| λz (terminal rate constant in plasma) | Up to 360 hours after drug administration |
| t1/2 (terminal half-life of the analyte in plasma) | Up to 360 hours after drug administration |
| MRT(mean residence time of the analyte in the body) | Up to 360 hours after drug administration |
| CL/F (apparent oral clearance in plasma after oral administration) | Up to 360 hours after drug administration |
| Vz/F (apparent volume of distribution during the terminal phase λz) dose) | Up to 360 hours after drug administration |
| Ae0-48 (amount of analyte that is eliminated in urine from 0-48 hours) | Up to 48 hours after drug administration |
| fe0-48 (fraction of analyte eliminated in urine from 0-48 hours) | Up to 48 hours after drug administration |
| CLR,0-48 (renal clearance of the analyte from 0-48 hours) | Up to 48 hours after drug administration |
| Receptor occupancy as determined by binding of anti-LFA-1 antibody fragment (Fab) | Up to 360 hours after drug administration |
| Inhibition of IL-2 production | in response to superantigen challenge ex vivo | Up to 360 hours after drug administration |