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Metabolism and Pharmacokinetics of [14C]-BIBF 1120 in Healthy Male Volunteers

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ClinicalTrials.gov Identifier: NCT02182154
Recruitment Status : Completed
First Posted : July 8, 2014
Last Update Posted : July 18, 2014
Sponsor:
Information provided by (Responsible Party):
Boehringer Ingelheim

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
Healthy Drug: BIBF 1120 ES Phase 1

Study Type : Interventional  (Clinical Trial)
Actual Enrollment : 8 participants
Intervention Model: Single Group Assignment
Masking: None (Open Label)
Primary Purpose: Treatment
Official Title: Metabolism and Pharmacokinetics of [14C]-BIBF 1120 After Administration of Single Doses of 100 mg [14C]-BIBF 1120 Oral Solution in Healthy Male Volunteers
Study Start Date : October 2005
Actual Primary Completion Date : November 2005

Resource links provided by the National Library of Medicine


Arm Intervention/treatment
Experimental: BIBF 1120 ES Drug: BIBF 1120 ES



Primary Outcome Measures :
  1. [14C]-radioactivity in plasma and whole blood (C Blood cells/C plasma ratio of [14C]-radioactivity) [ Time Frame: Up to 96 h after drug administration ]
  2. [14C]-radioactivity in urine [ Time Frame: Up to 120 h after drug administration ]
  3. Measurement of the plasma protein binding of total [14C]-radioactivity in human plasma samples ex vivo [ Time Frame: Up to 96 h after drug administration ]
  4. Maximum observed concentration of the analyte in plasma (Cmax) [ Time Frame: Up to 96 h after drug administration ]
  5. Plasma concentration-time profiles of total radioactivity in whole blood and plasma [ Time Frame: Up to 96 h after drug administration ]
  6. [14C]-metabolic profile and identification of metabolites in urine, in comparison with various animal species [ Time Frame: Up to 120 h after drug aministration ]
  7. [14C]-radioactivity in faeces [ Time Frame: up to 120 h after administration ]
  8. [14C]-metabolic profile and identification of metabolites in faeces, in comparison with various animal species [ Time Frame: Up to 120 h after drug aministration ]
  9. [14C]-metabolic profile and identification of metabolites in plasma, in comparison with various animal species [ Time Frame: Up to 96 h after drug aministration ]
  10. Time from dosing to peak concentration (tmax) [ Time Frame: Up to 96 h after drug administration ]
  11. Terminal half-life of the analyte in plasma (t1/2) [ Time Frame: Up to 96 h after drug administration ]
  12. Terminal rate constant of the analyte in plasma (λz) [ Time Frame: Up to 96 h after drug administration ]
  13. Area under the concentration-time curve of the analyte in plasma from zero time to 24 hours (AUC0-24) [ Time Frame: Up to 24 h after drug administration ]
  14. 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) [ Time Frame: Up to 96 h after drug administration ]
  15. Area under the concentration-time curve of the analyte in plasma from zero time to infinity (AUC0-∞) [ Time Frame: Up to 96 h after drug administration ]
  16. Mean residence time of the analyte molecules in the body after oral administration (MRTpo) [ Time Frame: Up to 96 h after drug administration ]
  17. Total clearance of the analyte in plasma following extravascular administration (CL/F) [ Time Frame: Up to 96 h after drug administration ]
  18. Apparent volume of distribution during the terminal phase λz following extravascular administration (Vz/F) [ Time Frame: Up to 96 h after drug administration ]
  19. Fraction of analyte eliminated in urine from 0 to the limit of the last quantifiable data point (fe0-tz) [ Time Frame: Up to 96 h after drug administration ]
  20. Fraction of analyte eliminated in faeces from 0 to the limit of the last quantifiable data point (fe faeces,0-tz) [ Time Frame: Up to 96 h after drug administration ]
  21. Amount of analyte that was eliminated in faeces from 0 to the limit of the last quantifiable data point (Ae faeces,0-tz) [ Time Frame: Up to 96 h after drug administration ]
  22. Amount of analyte that was eliminated in urine from 0 to the limit of the last quantifiable data point (Ae0-tz) [ Time Frame: Up to 96 h after drug administration ]

Secondary Outcome Measures :
  1. Change from baseline in vital signs [ Time Frame: Baseline, day 14 after drug administration ]
  2. Change from baseline in routine laboratory [ Time Frame: Baseline, day 14 after drug aministration ]
  3. Number of participants with adverse events [ Time Frame: Up to day 14 after drug aministration ]
  4. Change from baseline in electrocardiogram [ Time Frame: Baseline, day 14 after drug aministration ]
  5. Assessment of tolerability by investigator according a 4 point scale [ Time Frame: Day 14 after drug administration ]


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Ages Eligible for Study:   21 Years to 55 Years   (Adult)
Sexes Eligible for Study:   Male
Accepts Healthy Volunteers:   Yes
Criteria

Inclusion Criteria:

  1. Healthy male subjects as determined by results of screening
  2. Signed written informed consent in accordance with GCP and local legislation
  3. Age ≥21 and ≤55 years
  4. Body Mass Index ≥18.5 kg/m2 and ≤29.9 kg/m2

Exclusion Criteria:

  1. Any finding of the medical examination (including blood pressure, pulse rate and ECG) deviating from normal and of clinical relevance
  2. History or current gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunologic, hormonal disorders
  3. History of any major surgery within the last four weeks before participation in this study or any bone fracture within the last two months
  4. History of orthostatic hypotension, fainting spells and blackouts
  5. Diseases of the central nervous system (such as epilepsy) or psychiatric disorders
  6. Chronic or relevant acute infections
  7. History of allergy/hypersensitivity (including drug allergy) which is deemed relevant to the trial as judged by the investigator
  8. 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
  9. Intake of drugs with a long half-life (> 24 hours) within 1 month prior to administration
  10. Planned use of any drugs which might influence the results of the trial within 10 days prior to administration or during the trial
  11. Participation in another trial with an investigational drug within 2 months prior to administration or during trial
  12. Smoker (> 10 cigarettes or 3 cigars or 3 pipes/day) or inability to refrain from smoking on study days
  13. Alcohol abuse (> 60 g/day)
  14. Drug abuse
  15. Blood donation within 1 month prior to administration or during the trial
  16. Excessive physical activities within 5 days prior to administration or during the trial
  17. Any laboratory value outside the reference range, unless considered to lack clinical reference
  18. Female gender
  19. 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

Additional Information:
Responsible Party: Boehringer Ingelheim
ClinicalTrials.gov Identifier: NCT02182154     History of Changes
Other Study ID Numbers: 1199.20
First Posted: July 8, 2014    Key Record Dates
Last Update Posted: July 18, 2014
Last Verified: July 2014

Additional relevant MeSH terms:
Nintedanib
Antineoplastic Agents
Enzyme Inhibitors
Molecular Mechanisms of Pharmacological Action