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

NCT02182154 | Completed Phase 1

• 1 other identifier: 1199.20
• Study Type: interventional
• Target: 8
• Locations: 0 countries
• Sites: N/A

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

Conditions

Healthy

Outcome Measures

Primary Outcomes (22)

• [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 Outcomes (5)

• 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

Study Arms (1)

BIBF 1120 ES

EXPERIMENTAL

Drug: BIBF 1120 ES

Interventions

BIBF 1120 ES DRUG

BIBF 1120 ES

Eligibility Criteria

• Age: 21 Years - 55 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

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

You may not qualify if:

• Any finding of the medical examination (including blood pressure, pulse rate and ECG) deviating from normal and of clinical relevance
• History or current gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunologic, hormonal disorders
• History of any major surgery within the last four weeks before participation in this study or any bone fracture within the last two months
• History of orthostatic hypotension, fainting spells and blackouts
• Diseases of the central nervous system (such as epilepsy) or psychiatric disorders
• Chronic or relevant acute infections
• History of allergy/hypersensitivity (including drug allergy) which is deemed relevant to the trial as judged by the investigator
• 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
• Intake of drugs with a long half-life (\> 24 hours) within 1 month prior to administration
• Planned use of any drugs which might influence the results of the trial within 10 days prior to administration or during the trial
• Participation in another trial with an investigational drug within 2 months prior to administration or during trial
• Smoker (\> 10 cigarettes or 3 cigars or 3 pipes/day) or inability to refrain from smoking on study days
• Alcohol abuse (\> 60 g/day)
• Drug abuse
• Blood donation within 1 month prior to administration or during the trial

Sponsors & Collaborators

• Boehringer Ingelheim: lead

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NA
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: July 2, 2014
• First Posted: July 8, 2014
• Study Start: October 1, 2005
• Primary Completion: November 1, 2005
• Last Updated: July 18, 2014

Record last verified: 2014-07