Metabolism and Pharmacokinetics of [14C]-BIBR 953 ZW After Administration of Single Doses of [14C]-BIBR 953 ZW Intravenously or [14C]-BIBR 1048 Oral Solution in Healthy Male Volunteers

NCT02171442 | Completed Phase 1

• 1 other identifier: 1160.6
• Study Type: interventional
• Target: 10
• Locations: 0 countries
• Sites: N/A

Brief Summary

The aim of this study were to investigate the metabolism and pharmacokinetics of BIBR 1048 MS and BIBR 953 ZW in man.

Conditions

Healthy

Outcome Measures

Primary Outcomes (5)

• Total radioactivity in plasma and whole blood

  168 hours

• Total radioactivity in urine and faeces (excretion balance) over 168 h or until < 1% excreted in urine/faeces samples in a 24 h period

  over 168 hours or 24 hour period

• Concentrations of BIBR 953 ZW in plasma over 168 h, estimation of the extent of gastrointestinal absorption

  168 hours

• Concentrations of BIBR 953 ZW in urine

  168 hours

• [14C] metabolic pattern and identification of metabolites in urine and if feasible, in plasma and faeces in comparison with various animal species

  -12, 0 hours, 0-24, 24-48, 48-72, 72-96, 96-120, 120-144, 144-168 post dose

Secondary Outcomes (25)

• Ratio of radioactivity in blood cells and plasma (CE/CP)

  0.5, 1, 2 ,4 ,8, 24 hours after oral study drug administration, 31min, 1, 2, 4, 8, 24h after start of infusion

• Measurement of in vitro plasma protein binding of [14C]-BIBR 953 ZW

  Screening, day-1, day 1-day 8

• Cmax - Peak (maximum) plasma concentration of BIBR 953 ZW

  Screening, day-1, day 1-day 8

• tmax - time to reach the peak plasma concentration of BIBR 953 ZW

  Screening, day-1, day 1-day 8

• t1/2 - Terminal half-life derived from non-compartmental analysis of BIBR 953 ZW

  Screening, day-1, day 1-day 8

Study Arms (2)

BIBR 953 ZW Intravenously

EXPERIMENTAL

Drug: BIBR 953 ZW Intravenously

BIBR 1048 Oral Solution

ACTIVE COMPARATOR

Drug: BIBR 1048 Oral Solution

Interventions

BIBR 953 ZW Intravenously DRUG

5 mg, 2.8 MBq (76 µCi)

BIBR 953 ZW Intravenously

BIBR 1048 Oral Solution DRUG

200 mg free base, 2.8 MBq (76 µCi)

BIBR 1048 Oral Solution

Eligibility Criteria

• Age: 30 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 from each subject in accordance with the regulatory and legal requirements of the UK
• Age between 30 and 55 years of age
• Body Mass Index (BMI) of between 18.5 and 29.9 kg/m²

You may not qualify if:

• Any of the findings from the medical examination (including BP, pulse rate and ECG) deviated from normal or were of clinical relevance
• History of current gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunologic, hormonal disorders
• History of relevant orthostatic hypotension, fainting spells and blackouts, or volunteers with diseases of the central nervous system (such as epilepsy) or psychiatric disorders
• 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 principal investigator
• History of any bleeding disorder including prolonged or habitual bleeding
• History of other hematologic disease
• History of cerebral bleeding (e.g. after a car accident)
• History of craniocerebral trauma
• Intake of drugs with a long half life (≥ 24h) within 1 month prior to administration
• Any drugs which may have had an influence on the results of the trial within 10 days prior to administration or during the trial
• Any volunteers who had participated in another trial with an investigational drug within 3 months ( 4 months if the drug was a new chemical entity) prior to administration or during the trial
• Exposition to radiation in the previous 12 months (i.e. serial x-rays, CT scan or barium meal)
• Smoker

Sponsors & Collaborators

• Boehringer Ingelheim: lead

MeSH Terms

Interventions

Dabigatran

Intervention Hierarchy (Ancestors)

Pyridines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds; Benzimidazoles; Heterocyclic Compounds, 2-Ring; Heterocyclic Compounds, Fused-Ring

Study Design

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

Study Record Dates

• First Submitted: June 20, 2014
• First Posted: June 24, 2014
• Study Start: April 1, 2002
• Primary Completion: May 1, 2002
• Last Updated: June 24, 2014

Record last verified: 2014-06