Safety, Pharmacodynamics, and Pharmacokinetics of BIBT 1011 BS in Healthy Subjects

Safety, Pharmacodynamics, and Pharmacokinetics After Single Oral Administration of 1, 5, 10, 30, 100, 200 and 400 mg BIBT 1011 BS as Drinking Solution in Healthy Subjects. An Open, Placebo-controlled, Randomised Study, Double Blind at Each Dose Level

A study to assess safety, pharmacokinetics and the effect of BIBT 986 BS, given as BIBT 1011 BS, on coagulation parameters.

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: Single rising doses of BIBT 1011 BS; Drug: BIBT 1011 BS placebo

• Study Type: Interventional
• Enrollment (Actual): 56
• Phase: Phase 1

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 45 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: Male

Description

Inclusion Criteria:

• Healthy male subjects as determined by results of screening
• Signed written informed consent in accordance with good clinical practice (GCP) and local legislation
• Age ≥ 18 and ≤ 45 years
• Body Mass Index ≥ 18.5 and ≤ 29.9 kg/m2

Exclusion Criteria:

• 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, immunological, hormonal disorders
• History of orthostatic hypotension, fainting spells or 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)
  • commotio cerebri
• Intake of drugs with a long half-life (> 24 hours) within 1 month prior to administration
• 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
• 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 < 150000/µl

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Randomized
• Interventional Model: Parallel Assignment
• Masking: Double

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: BIBT 1011 BS	Drug: Single rising doses of BIBT 1011 BS
Placebo Comparator: BIBT 1011 BS placebo	Drug: BIBT 1011 BS placebo

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Determination of activated partial thromboplastin time (aPTT)	Pre-dose, up to 48 hours after start of treatment
Determination of international normalized ration (INR)	Pre-dose, up to 48 hours after start of treatment

Secondary Outcome Measures

Outcome Measure	Time Frame
Determination of thrombin time (TT)	Pre-dose, up to 48 hours after start of treatment
Determination of ecarin clotting time (ECT)	Pre-dose, up to 48 hours after start of treatment
Assessment of plasma concentration time profiles of BIBT 986 BS	Pre-dose, up to 48 hours after start of treatment
Maximum concentration of BIBT 986 BS in plasma (Cmax)	Pre-dose, up to 48 hours after start of treatment
Area under the concentration time curve for BIBT 986 BS (AUC)	Pre-dose, up to 48 hours after start of treatment
Time from dosing to when the plasma concentration reaches Cmax after a single extravascular dose (tmax)	Pre-dose, up to 48 hours after start of treatment
Total mean time of residence of BIBT 986 BS- molecules in the body (MRTtot)	Pre-dose, up to 48 hours after start of treatment
Apparent volume of distribution of the analytes during the terminal phase (Vz/f)	Pre-dose, up to 48 hours after start of treatment
Terminal elimination half life of BIBT 986 BS in plasma (t1/2)	Pre-dose, up to 48 hours after start of treatment
Amount excreted over the 24 hour sampling period (Ae0-24)	Pre-dose, up to 24 hours after start of treatment
Total clearance after oral administration (CLtot/F)	Pre-dose, up to 48 hours after start of treatment
Number of patients with adverse events	Up to 17 days
Assessment of BIBT 986 BS plasma concentration- aPTT relationship	Pre-dose, up to 48 hours after start of treatment

Collaborators and Investigators

• Sponsor: Boehringer Ingelheim

Publications and helpful links

Helpful Links

• Related Info

Study record dates

Study Major Dates

• Study Start: August 1, 2001
• Primary Completion (Actual): September 1, 2001

Study Registration Dates

• First Submitted: July 2, 2014
• First Submitted That Met QC Criteria: July 7, 2014
• First Posted (Estimate): July 8, 2014

Study Record Updates

• Last Update Posted (Estimate): July 14, 2014
• Last Update Submitted That Met QC Criteria: July 11, 2014
• Last Verified: July 1, 2014

More Information

Terms related to this study

• Other Study ID Numbers: 1193.1