Clinical trial NCT02173730: BIBR 953 ZW in Healthy Elderly Subjects
Official title: Pharmacokinetics of BIBR 953 ZW After 150 mg of BIBR 1048 (Oral Pro-drug of BIBR 953) Administered as Capsule Twice Daily Over Seven Days With or Without Pantoprazole Co-treatment to Healthy Male and Female Elderly Subjects
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Healthy
Lead sponsor: Boehringer Ingelheim
Sponsor class: INDUSTRY
First posted: 2014-06-25
Enrollment: 36
Sex: ALL
Minimum age (years): 65
Standard ages: OLDER_ADULT
Accepts healthy volunteers: yes
Allocation: RANDOMIZED
Intervention model: PARALLEL
Primary purpose: TREATMENT

Brief summary: To assess the steady state pharmacokinetic profile of BIBR 953 ZW after administration of BIBR 1048 to male and female elderly subjects, to assess pharmacokinetic gender differences. To assess the effect of coadministration of Pantoprazole on the bioavailability of BIBR 953 ZW.


Eligibility criteria: Inclusion Criteria:

* Healthy male and female elderly subjects as determined by results of screening
* Signed written informed consent in accordance with GCP and local legislation
* Age ≥ 65, no upper limit
* BMI ≥ 18.5 and ≤ 29.9 kg/m2

Exclusion Criteria:

* Any finding at the medical examination (including blood pressure, pulse rate and ECG) deviating from normal and of clinical relevance
* Clinically relevant gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunologic, hormonal disorders
* History of relevant 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
  * any bleeding disorder including prolonged or habitual bleeding
  * other hematologic disease
  * cerebral bleeding (e.g. after a car accident)
  * cranio-cerebral trauma
* Intake of drugs with a long half-life (\> 24 hours) within 1 month prior to administration
* Use of any drugs that 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 intake (\>30 - 40 g/day)
* Drug abuse
* Blood donation within 1 month prior to administration or during the trial
* Excessive physical activities within 5 days prior to administration or during the trial
* Any laboratory value outside the clinically accepted reference range
* History of any familial bleeding disorder
* Thrombocytes \< 140000/μl (male) or \< 156000/μl (female)

Primary outcomes:
measure: AUCτ,ss (area under the plasma concentration time curve during a dosing interval at steady state)
timeFrame: Day 4 and 7
measure: Cmax,ss (maximum measured concentration of the analyse in plasma at steady state over a uniform dosing interval τ)
timeFrame: Day 4 and 7
measure: Aeτ,ss (amount of dose excreted in urine over one dosing interval at steady state)
timeFrame: Day 4 and 7
measure: feτ,ss (percent of dose excreted in urine over one dosing interval at steady state)
timeFrame: Day 4 and 7
measure: AUC0-tz,ss (area under the plasma concentration time curve (AUC) from zero time (pre dose) to the time of the last quantifiable concentration (tz))
timeFrame: Day 4 and 7
measure: Cmin,ss (minimum measured concentration of the analyse in plasma at steady state over a uniform dosing interval τ)
timeFrame: Day 4 and 7
measure: tmax,ss (time from last dosing to the maximum concentration of the analyse in plasma at steady state over a uniform dosing interval τ)
timeFrame: Day 4 and 7
measure: t½,ss (terminal half-life, calculated from the terminal elimination rate constant)
timeFrame: Day 4 and 7
Secondary outcomes:
measure: CLR,ss (renal clearance at steady state following multiple dose administration)
timeFrame: Day 4 and 7
measure: MRTss (steady state mean residence time)
timeFrame: Day 4 and 7
measure: CL/F,ss (apparent clearance of the analyse in plasma at steady state after extravascular multiple dose administration)
timeFrame: Day 4 and 7
measure: Vz/F,ss (apparent volume of distribution during the terminal phase at steady state following extravascular administration)
timeFrame: Day 4 and 7
measure: Changes in activated partial thromboplastin time (aPTT)
timeFrame: Day 4 and 7
measure: Changes in ecarin clotting time (ECT)
timeFrame: Day 4 and 7
measure: Occurrence of Adverse Events
timeFrame: up to 10 days
Other outcomes:
Locations:
Study officials:
References: