Excretion Balance of 14c-radiolabeled BIRB 796 BS in Normal Male Subjects

A Phase I Single Oral Dose (100 mg) Trial to Characterize the Excretion Balance of 14c-radiolabeled BIRB 796 BS and to Determine Its Metabolites in Normal Male Subjects

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

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: 14C-BIRB 796 BS

• Study Type: Interventional
• Enrollment (Actual): 6
• Phase: Phase 1

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 45 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: Male

Description

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

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: N/A
• Interventional Model: Single Group Assignment
• Masking: None (Open Label)

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
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
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
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
tmax 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
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

Secondary Outcome Measures

Outcome Measure	Time Frame
Excretion of 14C-radioactivity in saliva (percent of dose)	up to 24 hours after drug administration
Excretion of 14C-radioactivity in expired air (percent of dose)	up to 48 hours after drug administration

Collaborators and Investigators

• Sponsor: Boehringer Ingelheim

Publications and helpful links

Helpful Links

• Related Info

Study record dates

Study Major Dates

• Study Start: October 1, 2002
• Primary Completion (Actual): November 1, 2002

Study Registration Dates

• First Submitted: August 7, 2014
• First Submitted That Met QC Criteria: August 7, 2014
• First Posted (Estimate): August 8, 2014

Study Record Updates

• Last Update Posted (Estimate): August 8, 2014
• Last Update Submitted That Met QC Criteria: August 7, 2014
• Last Verified: August 1, 2014

More Information

Terms related to this study

• Other Study ID Numbers: 1175.6