HealthyPhase 1NCT02171442
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
A Phase 1 study testing BIBR 953 ZW Intravenously and BIBR 1048 Oral Solution in people with Healthy, run by Boehringer Ingelheim.
Trial summary
The aim of this study were to investigate the metabolism and pharmacokinetics of BIBR 1048 MS and BIBR 953 ZW in man. Read more about this study
- Who is it for?
- Ages 30 to 55 years, men onlyHealthy volunteers can take part
- Conditions the study is for
- Healthy
- What is being tested?
- BIBR 953 ZW Intravenously and BIBR 1048 Oral Solution
- Type of treatment
- Pill or oral medicine, Injection or infusion
- Could I receive a placebo?
- No, everyone receives an active treatment
- How many people
- 10 participants
- Where
- No sites listed yet
- Study dates
- Apr 2002to May 2002
- Phase
- Phase 1
- Are there results?
- None posted in the registry
Key requirements
Who can take part, as listed by the sponsor. Only the study team can confirm whether you are eligible, so take this list to your doctor.
- Ages 30 to 55 years
- Men only
- Healthy volunteers accepted
- Adult
Who may be able to join
- 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
Who cannot join
- 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
Show all 23Show fewer
- 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
- Alcohol abuse (> 60 g/day)
- Drug abuse
- Blood donation within 12 weeks prior to administration or during the trial
- Any excessive physical activities within 5 days prior to administration or during the trial
- Any laboratory value outside the clinically accepted reference range
- History of familial bleeding disorder
- Platelets > 150 x 10-9 /l
- Unable to defecate at least once a day every two days
About this study
Official title: Metabolism and Pharmacokinetics of [14C]-BIBR 953 ZW After Administration of Single Doses of 5 mg [14C]-BIBR 953 ZW Intravenously or 200 mg [14C]-BIBR 1048 Oral Solution in a Group Comparison Design in 12 Healthy Male Volunteers.
The aim of this study were to investigate the metabolism and pharmacokinetics of BIBR 1048 MS and BIBR 953 ZW in man.
- Conditions
- Healthy
- Being tested
- BIBR 953 ZW Intravenously, BIBR 1048 Oral Solution
What participants receive
What participants receive. In a randomised study each person is assigned to one group by chance.
BIBR 953 ZW IntravenouslyDrug
5 mg, 2.8 MBq (76 µCi)
BIBR 1048 Oral SolutionDrug
200 mg free base, 2.8 MBq (76 µCi)
| Study group | Role | What they receive |
|---|---|---|
| BIBR 953 ZW Intravenously | Experimental | Not described Receives: Drug: BIBR 953 ZW Intravenously |
| BIBR 1048 Oral Solution | Active comparator | Not described Receives: Drug: BIBR 1048 Oral Solution |
What is being measured
The primary outcome is the main question the study is designed to answer.
Total radioactivity in plasma and whole blood
Measured: 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
Measured: over 168 hours or 24 hour period
Concentrations of BIBR 953 ZW in plasma over 168 h, estimation of the extent of gastrointestinal absorption
Measured: 168 hours
Concentrations of BIBR 953 ZW in urine
Measured: 168 hours
[14C] metabolic pattern and identification of metabolites in urine and if feasible, in plasma and faeces in comparison with various animal species
Measured: -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)
Measured: 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
Measured: Screening, day-1, day 1-day 8
Cmax - Peak (maximum) plasma concentration of BIBR 953 ZW
Measured: Screening, day-1, day 1-day 8
tmax - time to reach the peak plasma concentration of BIBR 953 ZW
Measured: Screening, day-1, day 1-day 8
t1/2 - Terminal half-life derived from non-compartmental analysis of BIBR 953 ZW
Measured: Screening, day-1, day 1-day 8
AUC0-t - area under the plasma concentration vs. time curve from time zero to the time point for the last sample on the pharmacokinetic profile in which total radioactivity or active drug were reliably quantified) BIBR 953 ZW
Measured: Screening, day-1, day 1-day 8
AUC0-infinity - Area under the plasma concentration vs. time curve from time zero to infinity - BIBR 953 ZW
Measured: Screening, day-1, day 1-day 8
MRT0-inf - the average amount of time a particle remains in a compartment or system, derived when the drug concentration profile is extrapolated to infinity) - BIBR 953 ZW
Measured: Screening, day-1, day 1-day 8
MRT0-t - the average amount of time a particle remains in a compartment or system - BIBR 953 ZW
Measured: Screening, day-1, day 1-day 8
CL renal - the apparent volume of the central compartment cleared of drug via renal excretion into the urine, per unit time - BIBR 953 ZW
Measured: Screening, day-1, day 1-day 8
CLtot - the apparent volume of the central compartment cleared of drug per unit tim after intravenous dosing - BIBR 953 ZW
Measured: Screening, day-1, day 1-day 8
CLtot/F - the apparent volume of the central compartment cleared of drug per unit time after extravascular dosing - BIBR 953 ZW
Measured: Screening, day-1, day 1-day 8
Vss - apparent volume of distribution at steady state following intravenous administration - BIBR 953 ZW
Measured: Screening, day-1, day 1-day 8
Vz/f - Volume of distribution during terminal phase after oral administration - BIBR 953 ZW
Measured: Screening, day-1, day 1-day 8
Cmax - Peak (maximum) plasma concentration for total radioactivity
Measured: up to day 8
tmax - time to reach the peak plasma concentration for total radioactivity
Measured: up to day 8
Occurence of Adverse events
Measured: Screening, upt to 10 days after study drug administration
Change from Baseline in physical examination
Measured: Screening, 8 to 10 days after study drug administration
Changes from Baseline in vital signs
Measured: Screening, 8 to 10 days after study drug administration
Change from Baseline in systolic and diastolic blood pressure
Measured: Screening, Day-1, day1, day2, day 8-10 after study drug administration
Change from Baseline in Pulse rate
Measured: Screening, Day-1, day1, day2, day 8-10 after study drug administration
Change from Baseline in 12-lead electrocardiogram (ECG)
Measured: Screening, Day-1, day1, day2, day 8-10 after study drug administration
Change from Baseline in clinical laboratory tests (hematology, clinical chemistry and urinanalysis)
Measured: Screening, day-1, day1, day2, day3, day 8-10 after study drug administration
Changes from baseline in activated partial thromboplastin time - aPTT
Measured: Screening, 1, 2, 24, 48 and 168 hours post dose administration
Changes from baseline in coagulation parameter INR - international normalized ratio prothrombin time
Measured: Screening, 1, 2, 24, 48 and 168 hours post dose administration
Timeline
From the start of the study to its completion; the mark is today. Estimated dates are the sponsor’s plan.
- First posted24 Jun 2014 (estimated)
- Study startApr 2002
- Primary completionMay 2002
Resources
- Official record on ClinicalTrials.govThe registry entry this page is built from, with its full change history.
- Other trials for HealthyStudies of the same condition, open and under way.
- More trials run by Boehringer IngelheimThe sponsor's other registered studies.
- What the trial phases meanHow a treatment moves from first tests in people to approval.
More details
For doctors and researchers: how the study is designed, who runs it, and its registry IDs.
Study design
- Study type
- Interventional
- Phase
- Phase 1
- Primary purpose
- Treatment
- Allocation
- Randomised
- Intervention model
- Parallel groups
- Masking
- None (open label)
- Enrolment
- 10 participants (actual)
Sponsor and investigators
- Lead sponsor
- Boehringer Ingelheim
- Sponsor type
- Industry (pharma, biotech, devices)
- Responsible party
- Sponsor
IDs, dates and publications
- ClinicalTrials.gov ID
- NCT02171442
- Sponsor's protocol ID
- 1160.6
- Status last verified
- Jun 2014
- First submitted
- 20 Jun 2014
- Last updated
- 24 Jun 2014
- Results posted
- No
Study at a glance
From the registry record, last updated by the sponsor on 24 Jun 2014. Recruitment status is as the sponsor reported it: confirm with the study team.
- Official title
- Metabolism and Pharmacokinetics of [14C]-BIBR 953 ZW After Administration of Single Doses of 5 mg [14C]-BIBR 953 ZW Intravenously or 200 mg [14C]-BIBR 1048 Oral Solution in a Group Comparison Design in 12 Healthy Male Volunteers.
- ClinicalTrials.gov ID
- NCT02171442
- Acronym / sponsor ID
- 1160.6
- Conditions
- Healthy
- Phase
- Phase 1
- Study type
- Interventional
- Recruitment status
- Completed
- Enrolment
- 10 participants (actual)
- Lead sponsor
- Boehringer IngelheimIndustry (pharma, biotech, devices)
- Study start
- Apr 2002
- Primary completion
- May 2002 (actual)
- First posted
- 24 Jun 2014 (estimated)
- Results
- Not posted in the source record
Clinical summary
The research question as the sponsor registered it. This describes what the study plans to test, not what it found.
The aim of this study were to investigate the metabolism and pharmacokinetics of BIBR 1048 MS and BIBR 953 ZW in man.
Study design
- Primary purpose
- Treatment
- Allocation
- Randomised
- Intervention model
- Parallel groups
- Masking
- None (open label)
- Number of arms
- 2
| Arm | Type | Receives |
|---|---|---|
| BIBR 953 ZW Intravenously | Experimental | Drug: BIBR 953 ZW Intravenously |
| BIBR 1048 Oral Solution | Active comparator | Drug: BIBR 1048 Oral Solution |
Who may qualify
- Ages
- 30 to 55 years
- Sex
- Male only
- Healthy volunteers
- Accepted
- Age groups
- Adult
Key inclusion criteria (4 listed)
- 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
Key exclusion criteria (23 listed)
- 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
Eligibility is decided by the study team after screening; this overview does not establish that a patient qualifies. Full inclusion and exclusion criteria.
Interventions
| Intervention | Type | Arms |
|---|---|---|
| BIBR 953 ZW Intravenously5 mg, 2.8 MBq (76 µCi) | Drug | BIBR 953 ZW Intravenously |
| BIBR 1048 Oral Solution200 mg free base, 2.8 MBq (76 µCi) | Drug | BIBR 1048 Oral Solution |
Primary outcome
Total radioactivity in plasma and whole blood
Time frame: 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
Time frame: over 168 hours or 24 hour period
Concentrations of BIBR 953 ZW in plasma over 168 h, estimation of the extent of gastrointestinal absorption
Time frame: 168 hours
Concentrations of BIBR 953 ZW in urine
Time frame: 168 hours
[14C] metabolic pattern and identification of metabolites in urine and if feasible, in plasma and faeces in comparison with various animal species
Time frame: -12, 0 hours, 0-24, 24-48, 48-72, 72-96, 96-120, 120-144, 144-168 post dose
25 secondary outcomes
Ratio of radioactivity in blood cells and plasma (CE/CP)
Time frame: 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
Time frame: Screening, day-1, day 1-day 8
Cmax - Peak (maximum) plasma concentration of BIBR 953 ZW
Time frame: Screening, day-1, day 1-day 8
tmax - time to reach the peak plasma concentration of BIBR 953 ZW
Time frame: Screening, day-1, day 1-day 8
t1/2 - Terminal half-life derived from non-compartmental analysis of BIBR 953 ZW
Time frame: Screening, day-1, day 1-day 8
AUC0-t - area under the plasma concentration vs. time curve from time zero to the time point for the last sample on the pharmacokinetic profile in which total radioactivity or active drug were reliably quantified) BIBR 953 ZW
Time frame: Screening, day-1, day 1-day 8
AUC0-infinity - Area under the plasma concentration vs. time curve from time zero to infinity - BIBR 953 ZW
Time frame: Screening, day-1, day 1-day 8
MRT0-inf - the average amount of time a particle remains in a compartment or system, derived when the drug concentration profile is extrapolated to infinity) - BIBR 953 ZW
Time frame: Screening, day-1, day 1-day 8
MRT0-t - the average amount of time a particle remains in a compartment or system - BIBR 953 ZW
Time frame: Screening, day-1, day 1-day 8
CL renal - the apparent volume of the central compartment cleared of drug via renal excretion into the urine, per unit time - BIBR 953 ZW
Time frame: Screening, day-1, day 1-day 8
CLtot - the apparent volume of the central compartment cleared of drug per unit tim after intravenous dosing - BIBR 953 ZW
Time frame: Screening, day-1, day 1-day 8
CLtot/F - the apparent volume of the central compartment cleared of drug per unit time after extravascular dosing - BIBR 953 ZW
Time frame: Screening, day-1, day 1-day 8
Vss - apparent volume of distribution at steady state following intravenous administration - BIBR 953 ZW
Time frame: Screening, day-1, day 1-day 8
Vz/f - Volume of distribution during terminal phase after oral administration - BIBR 953 ZW
Time frame: Screening, day-1, day 1-day 8
Cmax - Peak (maximum) plasma concentration for total radioactivity
Time frame: up to day 8
tmax - time to reach the peak plasma concentration for total radioactivity
Time frame: up to day 8
Occurence of Adverse events
Time frame: Screening, upt to 10 days after study drug administration
Change from Baseline in physical examination
Time frame: Screening, 8 to 10 days after study drug administration
Changes from Baseline in vital signs
Time frame: Screening, 8 to 10 days after study drug administration
Change from Baseline in systolic and diastolic blood pressure
Time frame: Screening, Day-1, day1, day2, day 8-10 after study drug administration
Change from Baseline in Pulse rate
Time frame: Screening, Day-1, day1, day2, day 8-10 after study drug administration
Change from Baseline in 12-lead electrocardiogram (ECG)
Time frame: Screening, Day-1, day1, day2, day 8-10 after study drug administration
Change from Baseline in clinical laboratory tests (hematology, clinical chemistry and urinanalysis)
Time frame: Screening, day-1, day1, day2, day3, day 8-10 after study drug administration
Changes from baseline in activated partial thromboplastin time - aPTT
Time frame: Screening, 1, 2, 24, 48 and 168 hours post dose administration
Changes from baseline in coagulation parameter INR - international normalized ratio prothrombin time
Time frame: Screening, 1, 2, 24, 48 and 168 hours post dose administration
Results and safety
The study is completed, but results are not available in the source record. That does not mean the treatment did or did not work.
Research links
- Official record on ClinicalTrials.govLast updated by the sponsor 24 Jun 2014.
- Related InfoLink provided by the sponsor.
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Referral and contact
AzTrials does not enrol participants or take referrals. Contact the study team or a site listed below; they decide who can take part. This study is not recruiting at the moment.
The record lists no contact. Use the official record to reach the sponsor.
Questions about this trial
What is this clinical trial studying?
A Phase 1 study testing BIBR 953 ZW Intravenously and BIBR 1048 Oral Solution in people with Healthy, run by Boehringer Ingelheim.
The full registered description is in the About this study section and the official record.
Who may be eligible to take part?
The sponsor lists 4 inclusion and 23 exclusion criteria. Eligibility is decided by the study team after screening, so read the full criteria and contact a listed site.
Is this clinical trial currently recruiting?
The record says: finished, as of the sponsor's last update on 24 Jun 2014. Status can change between updates, so confirm with the study contact before making plans.
What are the possible benefits and risks?
They depend on the study and the treatment, and no study can promise a benefit. The study team explains the known risks during informed consent, before anyone joins; the record itself does not list them.
What does this phase mean?
Phase 1 studies test a treatment in a small group of people for the first time or in a new way, mainly to check safety and find the right dose.
Not every study follows the same path, and some studies (observational studies, device studies) have no phase.
Are results available for this study?
The study is completed, but results are not available in the source record. That does not mean the treatment did or did not work.
How can a doctor refer a patient or contact the research team?
The record lists no contact. The official record names the sponsor, who can be asked directly. AzTrials does not enrol participants or take referrals.
What does the primary outcome measure?
Total radioactivity in plasma and whole blood (time frame: 168 hours). The study lists 5 primary outcomes in all. It is what the study was designed to measure, not a finding.
Where can I read the original study information?
Does a listing mean the treatment is approved or proven to work?
No. A listing means the study is registered. It does not show that the treatment is safe, works, or is approved by a regulator.
How often is this information updated?
AzTrials copies changed records from ClinicalTrials.gov every night and reloads the whole registry every week. The sponsor last updated this record on 24 Jun 2014.