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Single Rising Dose Study of BI 201335 ZW in Healthy Male Subjects

Phase 1
Terminated
Conditions
Healthy
Interventions
Drug: Placebo
Drug: BI 201335 ZW - single rising dose
Registration Number
NCT02182271
Lead Sponsor
Boehringer Ingelheim
Brief Summary

The objective of the current study is to investigate safety, tolerability, and pharmacokinetics of BI 201335 ZW following administration of single rising doses from 5 mg to 1500 mg. In addition Two stage intra-subject bioavailability comparison of 600 mg BI 201335 ZW as a liquid formulation given with and without food.

Detailed Description

Not available

Recruitment & Eligibility

Status
TERMINATED
Sex
Male
Target Recruitment
8
Inclusion Criteria
  • Healthy males according to the following criteria based upon a complete medical history, including the physical examination, vital signs ((blood pressure (BP), pulse rate (HR)), 12-lead electrocardiogram (ECG), clinical laboratory tests
  • Age ≥18 and Age ≤55 years
  • BMI ≥18.5 and BMI ≤29.9 kg/m2 (Body Mass Index)
  • Signed and dated written informed consent prior to admission to the study in accordance with Good Clinical Practice (GCP) and the local legislation
  • Willingness to abstain from alcohol from screening period until conclusion visit
Exclusion Criteria
  • Any finding of the medical examination (including blood pressure, pulse rate and ECG) deviating from normal and of clinical relevance
  • Any evidence of a clinically relevant concomitant disease
  • History or current gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunologic, hormonal disorders, including a clinical history of viral hepatitis, or serological evidence of active Hepatitis B or Hepatitis C infection
  • History of orthostatic hypotension, fainting spells and blackouts
  • Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or neurological 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
  • 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 the trial
  • Smoker (> 10 cigarettes or 3 cigars or 3 pipes/day) or inability to refrain from smoking on trial 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 and of clinical relevance
  • History of any familial bleeding disorder

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
PlaceboPlacebo-
BI 201335 ZW - single rising doseBI 201335 ZW - single rising dose-
Primary Outcome Measures
NameTimeMethod
Number of patients with abnormal findings in physical examinationBaseline, day 3 of each treatment period, within 8 days after last administration
Number of patients with clinically significant changes in 12-lead ECG (electrocardiogram)Baseline, day 1, 2 in treatment period, within 8 days after last administration
Number of patients with abnormal changes in laboratory parametersBaseline, day 1-3 of each treatment period, within 8 days after last administration
Number of patients with clinically significant changes in vital signsBaseline, day 1-3 of each treatment period, within 8 days after last administration
Number of patients with adverse eventsup to 13 days
Assessment of tolerability by investigator on a 4-point scaleon day 3 of each treatment period
Secondary Outcome Measures
NameTimeMethod
Cmax (maximum concentration of the analyte in plasma)pre-dose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 15, 24, 30, 36 and 48 hours post-dose
tmax (time from dosing to maximum concentration)pre-dose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 15, 24, 30, 36 and 48 hours post-dose
t1/2 (terminal half-life of the analyte in plasma)pre-dose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 15, 24, 30, 36 and 48 hours post-dose
AUC0-∞ (area under the concentration time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity)pre-dose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 15, 24, 30, 36 and 48 hours post-dose
AUC0-tz (area under the concentration-time curve of the analyte in plasma over the time interval from 0 to the last quantifiable data point)pre-dose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 15, 24, 30, 36 and 48 hours post-dose
λz (terminal elimination rate constant in plasma)pre-dose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 15, 24, 30, 36 and 48 hours post-dose
CL/F (apparent clearance of the analyte in the plasma after oral administration)pre-dose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 15, 24, 30, 36 and 48 hours post-dose
Vz/F (apparent volume of distribution during the terminal phase λz following an oral dose)pre-dose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 15, 24, 30, 36 and 48 hours post-dose
MRTpo (Mean residence time of the analyte in the body after oral administration)pre-dose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 15, 24, 30, 36 and 48 hours post-dose
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