Safety, Pharmacokinetics and Pharmacodynamics of BIBR 1048 MS Capsule in Healthy Male Subjects of Japanese and Caucasian Origin

Boehringer Ingelheim

Status and phase: Completed; Phase 1

Conditions: Healthy

Treatments: Drug: BIBR 1048 MS low dose; Drug: BIBR 1048 MS medium dose; Drug: BIBR 1048 MS high dose

Study type: Interventional

Funder types: Industry

Identifiers

NCT02170909

1160.29

Details and patient eligibility

About

Study to investigate and compare safety, pharmacokinetics and pharmacodynamics of BIBR 1048 MS following oral administration of single (150 mg, 220 mg and 300 mg) and multiple (150 mg and 220 mg q.d. and 150 mg b.i.d.) rising doses in healthy male subjects of Japanese and Caucasian origin.

Enrollment: 42 patients

Sex: Male

Ages: 20 to 45 years old

Volunteers: Accepts Healthy Volunteers

Inclusion criteria

1. Healthy male subjects of Japanese or Caucasian origin according to the following criteria: Based upon a complete medical history, including the physical examination, vital signs (blood pressure, pulse rate, respiratory rate and tympanic body temperature), 12- lead ECG (electrocardiogram), clinical laboratory tests

   • 1.1 No finding deviating from normal and of clinical relevance
   • 1.2 No evidence of a clinically relevant concomitant disease

2. Age ≥ 20 and Age ≤ 45 years

3. Body mass index (BMI) ≥ 18 and ≤ 25 kg/m2

4. Japanese subjects were from a well-defined Japanese population, both parents of Japanese origin and the subjects have Japanese passport and had lived ≤ 8 years outside Japan.

5. Signed and dated written informed consent prior to admission to the study in accordance with GCP (Good Clinical Practice) and the local legislation.

Exclusion criteria

1. Current gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders

2. An unwillingness of male subjects to abstain from sexual intercourse with pregnant or lactating women, or an unwillingness of male subjects to use an adequate form of contraception as well as having their female partner(s) use another form of contraception (if the woman possibly become pregnant) from the time of the single dose on Day 1 until Day 22-26 (end-of study examination)

3. Current diseases of the central nervous system (such as epilepsy), or psychiatric disorders or neurological disorders

4. History of clinically significant orthostatic hypotension, clinically significant current or past fainting spells or blackouts

5. Chronic or relevant acute infections

6. 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)
   • concussions (head trauma resulting in injuring to brain) with or without loss of consciousness

7. Intake of drugs with a long half-life (> 24 hours) within at least one month or less than 10 half-lives, whichever is shorter, of the respective drug prior to administration or during the trial

8. Use of acetylsalicylic acid (ASA)-containing over-the-counter medications, clopidogrel or ticlopidine or dipyridamole, chronic administration of non-steroidal anti-inflammatory drugs (NSAIDs) (cyclooxygenase-2 (COX-2) inhibitors excluded), coumadin like anticoagulants, chronic use of corticosteroids, heparin and fibrinolytic agents within 14 days prior to administration or during the trial.

9. Participation in another trial with an investigational drug within three months prior to administration or during the trial

10. Smoker (> 10 cigarettes/day or > 3 cigars/day or > 3 pipes/day)

11. Inability to refrain from smoking on trial days

12. Alcohol abuse (more than 21unit/week; one unit was approximately half a pint of beer, a small glass of wine or one measure of spirits)

13. History of drug abuse

14. Blood donation (more than 100 mL within three months prior to screening administration and any blood donation from screening to end-of-study examination)

15. Excessive physical activities (within one week prior to administration or during the trial and until end-of-study examination)

16. Any laboratory value outside the reference range that was of clinical relevance

17. Inability to comply with dietary regimen of study centre

18. Known hypersensitivity to the drug or its excipients

19. History of any familial bleeding disorder

20. Thrombocytes < 150000/μL

Trial design

Primary purpose: Treatment

Allocation: Non-Randomized

Interventional model: Parallel Assignment

Masking: None (Open label)

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42 participants in 3 patient groups

BIBR 1048 MS low dose

Experimental group

Treatment:

Drug: BIBR 1048 MS low dose

BIBR 1048 MS medium dose

Experimental group

Treatment:

Drug: BIBR 1048 MS medium dose

BIBR 1048 MS high dose

Experimental group

Treatment:

Drug: BIBR 1048 MS high dose