Metabolism and Pharmacokinetics of [14C]-BIBF 1120 in Healthy Male Volunteers
Study Details
Study Description
Brief Summary
To assess the metabolic profile,
to obtain the mass balance after oral administration,
to determine the concentration of [14C]-radioactivity in blood cells, plasma, urine and faeces,
to determine BIBF 1120 and BIBF 1202 concentrations in plasma, urine, and faeces, if feasible,
to determine the protein binding of [14C]-radioactivity,
to determine the pharmacokinetics of BIBF 1120, BIBF 1202 and total radioactivity after a single oral administration of [14C]-BIBF 1120 in healthy volunteers
Condition or Disease | Intervention/Treatment | Phase |
---|---|---|
|
Phase 1 |
Study Design
Arms and Interventions
Arm | Intervention/Treatment |
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Experimental: BIBF 1120 ES
|
Drug: BIBF 1120 ES
|
Outcome Measures
Primary Outcome Measures
- [14C]-radioactivity in plasma and whole blood (C Blood cells/C plasma ratio of [14C]-radioactivity) [Up to 96 h after drug administration]
- [14C]-radioactivity in urine [Up to 120 h after drug administration]
- Measurement of the plasma protein binding of total [14C]-radioactivity in human plasma samples ex vivo [Up to 96 h after drug administration]
- Maximum observed concentration of the analyte in plasma (Cmax) [Up to 96 h after drug administration]
- Plasma concentration-time profiles of total radioactivity in whole blood and plasma [Up to 96 h after drug administration]
- [14C]-metabolic profile and identification of metabolites in urine, in comparison with various animal species [Up to 120 h after drug aministration]
- [14C]-radioactivity in faeces [up to 120 h after administration]
- [14C]-metabolic profile and identification of metabolites in faeces, in comparison with various animal species [Up to 120 h after drug aministration]
- [14C]-metabolic profile and identification of metabolites in plasma, in comparison with various animal species [Up to 96 h after drug aministration]
- Time from dosing to peak concentration (tmax) [Up to 96 h after drug administration]
- Terminal half-life of the analyte in plasma (t1/2) [Up to 96 h after drug administration]
- Terminal rate constant of the analyte in plasma (λz) [Up to 96 h after drug administration]
- Area under the concentration-time curve of the analyte in plasma from zero time to 24 hours (AUC0-24) [Up to 24 h after drug administration]
- Area under the concentration-time curve of the analyte in plasma from zero time to the time of the last quantifiable drug concentration (AUC0-tz) [Up to 96 h after drug administration]
- Area under the concentration-time curve of the analyte in plasma from zero time to infinity (AUC0-∞) [Up to 96 h after drug administration]
- Mean residence time of the analyte molecules in the body after oral administration (MRTpo) [Up to 96 h after drug administration]
- Total clearance of the analyte in plasma following extravascular administration (CL/F) [Up to 96 h after drug administration]
- Apparent volume of distribution during the terminal phase λz following extravascular administration (Vz/F) [Up to 96 h after drug administration]
- Fraction of analyte eliminated in urine from 0 to the limit of the last quantifiable data point (fe0-tz) [Up to 96 h after drug administration]
- Fraction of analyte eliminated in faeces from 0 to the limit of the last quantifiable data point (fe faeces,0-tz) [Up to 96 h after drug administration]
- Amount of analyte that was eliminated in faeces from 0 to the limit of the last quantifiable data point (Ae faeces,0-tz) [Up to 96 h after drug administration]
- Amount of analyte that was eliminated in urine from 0 to the limit of the last quantifiable data point (Ae0-tz) [Up to 96 h after drug administration]
Secondary Outcome Measures
- Change from baseline in vital signs [Baseline, day 14 after drug administration]
- Change from baseline in routine laboratory [Baseline, day 14 after drug aministration]
- Number of participants with adverse events [Up to day 14 after drug aministration]
- Change from baseline in electrocardiogram [Baseline, day 14 after drug aministration]
- Assessment of tolerability by investigator according a 4 point scale [Day 14 after drug administration]
Eligibility Criteria
Criteria
Inclusion Criteria:
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Healthy male subjects as determined by results of screening
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Signed written informed consent in accordance with GCP and local legislation
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Age ≥21 and ≤55 years
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Body Mass Index ≥18.5 kg/m2 and ≤29.9 kg/m2
Exclusion Criteria:
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Any finding of the medical examination (including blood pressure, pulse rate and ECG) deviating from normal and of clinical relevance
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History or current gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunologic, hormonal disorders
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History of any major surgery within the last four weeks before participation in this study or any bone fracture within the last two months
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History of orthostatic hypotension, fainting spells and blackouts
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Diseases of the central nervous system (such as epilepsy) or psychiatric disorders
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Chronic or relevant acute infections
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History of allergy/hypersensitivity (including drug allergy) which is deemed relevant to the trial as judged by the investigator
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History of any bleeding disorder including prolonged or habitual bleeding, other haematologic disease or cerebral bleeding (e.g. after a car accident) or commotio cerebri
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Intake of drugs with a long half-life (> 24 hours) within 1 month prior to administration
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Planned use of any drugs which might influence the results of the trial within 10 days prior to administration or during the trial
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Participation in another trial with an investigational drug within 2 months prior to administration or during trial
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Smoker (> 10 cigarettes or 3 cigars or 3 pipes/day) or inability to refrain from smoking on study days
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Alcohol abuse (> 60 g/day)
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Drug abuse
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Blood donation within 1 month prior to administration or during the trial
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Excessive physical activities within 5 days prior to administration or during the trial
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Any laboratory value outside the reference range, unless considered to lack clinical reference
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Female gender
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Male subjects must agree to minimize the risk of female partners becoming pregnant from the dosing day until 3 months after the completion of the study. Acceptable methods of contraception for male volunteers include a vasectomy no less than 3 months prior to dosing, barrier contraception or a medically accepted contraceptive method. For female partners of male volunteers, acceptable methods of contraception include intra-uterine device, tubal ligation, hormonal contraceptive since at least two months and diaphragm with spermicide
Contacts and Locations
Locations
No locations specified.Sponsors and Collaborators
- Boehringer Ingelheim
Investigators
None specified.Study Documents (Full-Text)
None provided.More Information
Additional Information:
Publications
None provided.- 1199.20