Healthy
Conditions
Brief summary
Study to characterize the pharmacokinetics of 14C-radiolabeled BIRB 796 BS and its metabolites including excretion and mass balance of parent compound and radioactivity; to isolate, identify and quantify major radiolabeled metabolites of BIRB 796 in plasma, urine and feces
Interventions
DRUG14C-BIRB 796 BS
14C-radiolabeled BIRB 796 BS
Sponsors
Boehringer Ingelheim
Study design
Allocation
NA
Intervention model
SINGLE_GROUP
Primary purpose
TREATMENT
Masking
NONE
Eligibility
Sex/Gender
MALE
Age
18 Years to 45 Years
Healthy volunteers
Yes
Inclusion criteria
* Healthy male subjects as determined by results of screening. Health is confirmed by medical history, physical examination, laboratory testing and 12-lead electrocardiogram (ECG) * Signed written informed consent in accordance with Good Clinical Practice * Age ≥ 18 and ≤ 45 years * Subjects within 10% of the normal height: weight range defined by the Metropolitan Life Insurance Company Tables
Exclusion criteria
* Any finding of the medical examination (including blood pressure, pulse rate, and ECG) deviating from normal and of clinical relevance * History of clinically significant disease including metabolic, endocrinologic, immunological, hepatic, renal, gastrointestinal, respiratory, cardiovascular, psychiatric or neurological * History of allergy/hypersensitivity (including drug allergy) which is deemed relevant to the trial as judged by the investigator * Subjects with a history of drug abuse or alcoholism * Chronic or relevant acute (within 1 month of screening) infections * Subjects who have taken prescription within one month or over-the-counter drugs within two weeks of the start of the trial * Participation in another trial with an investigational drug (≤ 2 months prior to administration or during trial) * Inability to refrain from smoking on trial days * Blood donation \> 400 mL (within 1 month prior to administration or during the trial) * Any laboratory value outside 10% of the reference range of clinical relevance (but not exclusive to) total white cell count ≥ 10 x 10\*\*9/L, any hemoglobin \< 12 mg/dl or \>15 mg/dl. Protein on urine dipstick * Positive urine drug screen, positive HIV or Hepatitis C antibodies * History of any familial bleeding disorder
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| tmax of BIRB 796BS in plasma | up to 96 hours after drug administration |
| Cmax of BIRB 796BS in plasma | up to 96 hours after drug administration |
| AUC0-∞ of BIRB 796BS in plasma | up to 96 hours after drug administration |
| t1/2 of BIRB 796BS in plasma | up to 96 hours after drug administration |
| Quantification of radiolabeled metabolites in urine (percent of dose) | up to 5 days |
| Cumulative amount of 14C-BIRB 796 BS radioactivity excreted in feces (percent of dose) | up to 5 days |
| Cumulative amount of 14C-BIRB 796 BS radioactivity excreted in urine (percent of dose) | up to 5 days |
| Maximum observed Concentration (Cmax) of 14C-BIRB 796BS in plasma | up to 96 hours after drug administration |
| Quantification of radiolabeled metabolites in feces (percent of dose) | up to 5 days |
| Quantification of radiolabeled metabolites in plasma (percent of dose) | up to 96 hours after drug administration |
| Area under the Concentration versus time curve from time 0 to infinity (AUC0-∞) of 14C-BIRB 796BS in plasma | up to 96 hours after drug administration |
| Time To The Maximum Concentration (tmax) of 14C-BIRB 796BS in plasma | up to 96 hours after drug administration |
| Elimination Half-Life (t1/2) of 14C-BIRB 796BS in plasma | up to 96 hours after drug administration |
| Erythrocyte-plasma partition ratio of 14C-radioactivity | up to 5 days |
| Cmax of 14C-BIRB 796BS in blood | up to 96 hours after drug administration |
| AUC0-∞ of 14C-BIRB 796BS in blood | up to 96 hours after drug administration |
| tmax of 14C-BIRB 796BS in blood | up to 96 hours after drug administration |
| t1/2 of 14C-BIRB 796BS in blood | up to 96 hours after drug administration |
Secondary
| Measure | Time frame |
|---|---|
| Excretion of 14C-radioactivity in expired air (percent of dose) | up to 48 hours after drug administration |
| Excretion of 14C-radioactivity in saliva (percent of dose) | up to 24 hours after drug administration |
Outcome results
None listed