Pharmacodynamics, Safety and Pharmacokinetics After Oral Administration of BIBR 1048 MS in Healthy Volunteers

NCT02170116 | Completed Phase 1

• 1 other identifier: 1160.1
• Study Type: interventional
• Target: 40
• Locations: 0 countries
• Sites: N/A

Brief Summary

The objective of this study was to assess safety, pharmacokinetics and the effect of BIBR 953 ZW on coagulation parameters of BIBR 953 ZW after oral single doses of the prodrug, BIBR 1048 MS, in healthy male subjects. This was the first administration of this substance to humans.

Conditions

Healthy

Outcome Measures

Primary Outcomes (2)

• Changes from baseline in prothrombin time (PT) (International Normalised Ratio (INR))

  - 0.5, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24 hours after administration

• Changes from baseline in activated partial thromboplastin time (aPTT)

  - 0.5, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24 hours after administration

Secondary Outcomes (15)

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

  - 0.5, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48 hours after administration

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

  - 0.5, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48 hours after administration

• AUC0-12 h - Area under the plasma concentration-time curve of BIBR 953 ZW from 0 to 12 h

  - 0.5, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48 hours after administration

• Area under the plasma concentration-time curve (AUC0-infinity) of BIBR 953 ZW from 0 to infinity

  - 0.5, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48 hours after administration

• Area under the plasma concentration-time curve of BIBR 953 ZW (AUCtf -infinity) from tf (last time point when measured plasma concentration) to infinity expressed as % of AUC0-infinity

  - 0.5, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48 hours after administration

Study Arms (6)

BIBR 1048 MS dose 1

EXPERIMENTAL

Drug: BIBR 1048 MS dose 1

BIBR 1048 MS dose 2

EXPERIMENTAL

Drug: BIBR 1048 MS dose 2

BIBR 1048 MS dose 3

EXPERIMENTAL

Drug: BIBR 1048 MS dose 3

BIBR 1048 MS dose 4

EXPERIMENTAL

Drug: BIBR 1048 MS dose 4

BIBR 1048 MS dose 5

EXPERIMENTAL

Drug: BIBR 1048 MS dose 5

Placebo

PLACEBO COMPARATOR

Drug: Placebo to BIBR 1048 MS

Interventions

BIBR 1048 MS dose 1 DRUG

BIBR 1048 MS dose 1

BIBR 1048 MS dose 2 DRUG

BIBR 1048 MS dose 2

BIBR 1048 MS dose 3 DRUG

BIBR 1048 MS dose 3

BIBR 1048 MS dose 4 DRUG

BIBR 1048 MS dose 4

BIBR 1048 MS dose 5 DRUG

BIBR 1048 MS dose 5

Placebo to BIBR 1048 MS DRUG

Placebo

Eligibility Criteria

• Age: 18 Years - 45 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 in accordance with Good Clinical Practice (GCP) and local legislation
• Age \>= 18 and \<= 45 years
• Broca \>= - 20 % and \<= + 20 %

You may not qualify if:

• 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, immunologic, 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)
• commotion 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

Sponsors & Collaborators

• Boehringer Ingelheim: lead

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: DOUBLE
• Purpose: TREATMENT
• Intervention Model: PARALLEL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: June 20, 2014
• First Posted: June 23, 2014
• Study Start: November 1, 1998
• Primary Completion: December 1, 1998
• Last Updated: June 23, 2014

Record last verified: 2014-06