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

Phase 1

Completed

• Conditions: Healthy
• Interventions: Drug: BIBT 1011 BS placebo; Drug: Single rising doses of BIBT 1011 BS

• Registration Number: NCT02182037
• Lead Sponsor: Boehringer Ingelheim

Brief Summary

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

Detailed Description

Not available

Study Timeline

• Study Start: 2001-08
• Primary Completion: 2001-09
• Status Verified: 2014-07
• Study First Submitted: 2014-07-02
• Study First Submitted QC: 2014-07-07
• Study First Posted: 2014-07-08
• Last Update Submitted: 2014-07-11
• Last Update Posted: 2014-07-14

Recruitment & Eligibility

• Status: COMPLETED
• Sex: Male
• Target Recruitment: 56

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 & Design

• Study Type: INTERVENTIONAL
• Study Design: PARALLEL

Arm && Interventions

Group	Intervention	Description
BIBT 1011 BS placebo	BIBT 1011 BS placebo	-
BIBT 1011 BS	Single rising doses of BIBT 1011 BS	-

Primary Outcome Measures

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

Secondary Outcome Measures

Name	Time	Method
Assessment of plasma concentration time profiles of BIBT 986 BS	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
Determination of thrombin time (TT)	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
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
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
Determination of ecarin clotting time (ECT)	Pre-dose, up to 48 hours after start of treatment