<clinical_study>
  <!-- This xml conforms to an XML Schema at:
    https://clinicaltrials.gov/ct2/html/images/info/public.xsd -->
  <required_header>
    <download_date>ClinicalTrials.gov processed this data on September 20, 2023</download_date>
    <link_text>Link to the current ClinicalTrials.gov record.</link_text>
    <url>https://clinicaltrials.gov/ct2/show/NCT02256787</url>
  </required_header>
  <id_info>
    <org_study_id>1201.1</org_study_id>
    <nct_id>NCT02256787</nct_id>
  </id_info>
  <brief_title>Safety, Tolerance, and Pharmacokinetics of Single Rising Oral Doses of BILB 1941 ZW Solution in Healthy Male Subjects, Followed With Bioavailability Comparison of BILB 1941 ZW Tablet and Solution Formulation Administered With or Without Food</brief_title>
  <official_title>Safety, Tolerance, and Pharmacokinetics of Single Oral Doses of 5 mg, 20 mg, 60 mg, 120 mg, 200 mg, 300 mg, 600 mg, 1000 mg, 1500 mg, 2000 mg, 2400 mg, and 3000 mg BILB 1941 ZW (PEG 400/TRIS Solution) in Healthy Male Subjects, in a Randomised Double Blind, Placebo Controlled Rising Dose Study, Followed With an Open-label Intra-subject Three-Way Crossover Bioavailability Comparison of 600 mg BILB 1941 ZW in a PEG 400/TRIS Solution and 600 mg BILB 1941 ZW Tablet and 600 mg BILB 1941 ZW Tablet Administered With Food</official_title>
  <sponsors>
    <lead_sponsor>
      <agency>Boehringer Ingelheim</agency>
      <agency_class>Industry</agency_class>
    </lead_sponsor>
  </sponsors>
  <source>Boehringer Ingelheim</source>
  <brief_summary>
    <textblock>
      The objective of the current study was to investigate the safety, tolerability, and&#xD;
      pharmacokinetics of BILB 1941 ZW following the administration of single rising doses from 5&#xD;
      mg to 300 mg. In addition the bioavailability of the 60 mg dose given fasted and after a&#xD;
      high-fat breakfast was to be be investigated&#xD;
    </textblock>
  </brief_summary>
  <overall_status>Completed</overall_status>
  <start_date>January 2004</start_date>
  <primary_completion_date type="Actual">September 2004</primary_completion_date>
  <phase>Phase 1</phase>
  <study_type>Interventional</study_type>
  <has_expanded_access>No</has_expanded_access>
  <study_design_info>
    <allocation>Randomized</allocation>
    <intervention_model>Parallel Assignment</intervention_model>
    <primary_purpose>Treatment</primary_purpose>
    <masking>Double</masking>
  </study_design_info>
  <primary_outcome>
    <measure>Number of subjects with abnormal findings in physical examination</measure>
    <time_frame>up to 48 hours following drug administration</time_frame>
  </primary_outcome>
  <primary_outcome>
    <measure>Number of subjects with abnormal changes in laboratory parameters</measure>
    <time_frame>up to 48 hours following drug administration</time_frame>
  </primary_outcome>
  <primary_outcome>
    <measure>Number of subjects with clinically significant changes in vital signs</measure>
    <time_frame>up to 48 hours following drug administration</time_frame>
    <description>Blood pressure, Pulse Rate</description>
  </primary_outcome>
  <primary_outcome>
    <measure>Number of subjects with adverse events</measure>
    <time_frame>up to 48 hours following drug administration</time_frame>
  </primary_outcome>
  <primary_outcome>
    <measure>Number of subjects with clinically significant changes in 12-lead ECG (electrocardiogram)</measure>
    <time_frame>up to 48 hours following drug administration</time_frame>
  </primary_outcome>
  <primary_outcome>
    <measure>Assessment of tolerability by investigator on a 4-point scale</measure>
    <time_frame>after 48 hours following drug administration</time_frame>
  </primary_outcome>
  <secondary_outcome>
    <measure>Cmax (maximum concentration of the analyte in plasma)</measure>
    <time_frame>up to 48 hours following drug administration</time_frame>
  </secondary_outcome>
  <secondary_outcome>
    <measure>tmax (time from dosing to maximum concentration)</measure>
    <time_frame>up to 48 hours following drug administration</time_frame>
  </secondary_outcome>
  <secondary_outcome>
    <measure>AUC0-∞ (area under the concentration time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity)</measure>
    <time_frame>up to 48 hours following drug administration</time_frame>
  </secondary_outcome>
  <secondary_outcome>
    <measure>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)</measure>
    <time_frame>up to 48 hours following drug administration</time_frame>
  </secondary_outcome>
  <secondary_outcome>
    <measure>λz (terminal rate constant in plasma)</measure>
    <time_frame>up to 48 hours following drug administration</time_frame>
  </secondary_outcome>
  <secondary_outcome>
    <measure>t1/2 (terminal half-life of the analyte in plasma)</measure>
    <time_frame>up to 48 hours following drug administration</time_frame>
  </secondary_outcome>
  <secondary_outcome>
    <measure>MRT (Mean time of residence of drug molecules in the body after intravascular administration)</measure>
    <time_frame>up to 48 hours following drug administration</time_frame>
  </secondary_outcome>
  <secondary_outcome>
    <measure>Vz/F (Apparent volume of distribution during the terminal phase after extravascular administration)</measure>
    <time_frame>up to 48 hours following drug administration</time_frame>
  </secondary_outcome>
  <number_of_arms>5</number_of_arms>
  <enrollment type="Actual">56</enrollment>
  <condition>Healthy</condition>
  <arm_group>
    <arm_group_label>BILB 1941 ZW - single rising dose</arm_group_label>
    <arm_group_type>Experimental</arm_group_type>
    <description>Single rising dose part</description>
  </arm_group>
  <arm_group>
    <arm_group_label>Placebo</arm_group_label>
    <arm_group_type>Placebo Comparator</arm_group_type>
    <description>Single rising dose part</description>
  </arm_group>
  <arm_group>
    <arm_group_label>BILB 1941 ZW - tablet - fasted</arm_group_label>
    <arm_group_type>Experimental</arm_group_type>
    <description>Relative bioavailability: The oral solution fasted should be compared with the solid form fasted and after a standardized breakfast</description>
  </arm_group>
  <arm_group>
    <arm_group_label>BILB 1941 ZW - solution</arm_group_label>
    <arm_group_type>Experimental</arm_group_type>
    <description>Relative bioavailability: The oral solution fasted should be compared with the solid form fasted and after a standardized breakfast</description>
  </arm_group>
  <arm_group>
    <arm_group_label>BILB 1941 ZW - tablet - fed</arm_group_label>
    <arm_group_type>Experimental</arm_group_type>
    <description>Relative bioavailability: The oral solution fasted should be compared with the solid form fasted and after a standardized breakfast</description>
  </arm_group>
  <intervention>
    <intervention_type>Drug</intervention_type>
    <intervention_name>BILB 1941 ZW - single rising dose part</intervention_name>
    <arm_group_label>BILB 1941 ZW - single rising dose</arm_group_label>
  </intervention>
  <intervention>
    <intervention_type>Drug</intervention_type>
    <intervention_name>Placebo</intervention_name>
    <arm_group_label>Placebo</arm_group_label>
  </intervention>
  <intervention>
    <intervention_type>Drug</intervention_type>
    <intervention_name>BILB 1941 ZW - solution</intervention_name>
    <arm_group_label>BILB 1941 ZW - solution</arm_group_label>
  </intervention>
  <intervention>
    <intervention_type>Drug</intervention_type>
    <intervention_name>BILB 1941 ZW - tablet</intervention_name>
    <arm_group_label>BILB 1941 ZW - tablet - fasted</arm_group_label>
    <arm_group_label>BILB 1941 ZW - tablet - fed</arm_group_label>
  </intervention>
  <intervention>
    <intervention_type>Other</intervention_type>
    <intervention_name>standardized breakfast</intervention_name>
    <arm_group_label>BILB 1941 ZW - tablet - fed</arm_group_label>
  </intervention>
  <eligibility>
    <criteria>
      <textblock>
        Inclusion Criteria:&#xD;
&#xD;
          1. Healthy males according to the following criteria based upon a complete medical&#xD;
             history, including the physical examination, vital signs (BP, PR), 12-lead ECG,&#xD;
             clinical laboratory tests:&#xD;
&#xD;
             1.1 No finding deviating from normal and of clinical relevance&#xD;
&#xD;
             1.2 No evidence of a clinically relevant concomitant disease&#xD;
&#xD;
          2. Age ≥18 and Age ≤50 years, BMI ≥18.5 and BMI ≤29.9 kg/m2 (Body Mass Index)&#xD;
&#xD;
          3. Signed and dated written informed consent prior to admission to the study in&#xD;
             accordance with Good Clinical Practice (GCP) and the local legislation&#xD;
&#xD;
        Exclusion Criteria:&#xD;
&#xD;
          -  Any finding of the medical examination (including blood pressure, pulse rate and ECG)&#xD;
             deviating from normal and of clinical relevance&#xD;
&#xD;
          -  History or current gastrointestinal, hepatic, renal, respiratory, cardiovascular,&#xD;
             metabolic, immunologic, hormonal disorders, including a clinical history of viral&#xD;
             hepatitis, or serological evidence of active Hepatitis B or Hepatitis C infection&#xD;
&#xD;
          -  History of orthostatic hypotension, fainting spells and blackouts&#xD;
&#xD;
          -  Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or&#xD;
             neurological disorders&#xD;
&#xD;
          -  Chronic or relevant acute infections&#xD;
&#xD;
          -  History of allergy/hypersensitivity (including drug allergy) which is deemed relevant&#xD;
             to the trial as judged by the investigator&#xD;
&#xD;
          -  Intake of drugs with a long half-life (&gt; 24 hours) within 1 month prior to&#xD;
             administration&#xD;
&#xD;
          -  Use of any drugs which might influence the results of the trial within 10 days prior&#xD;
             to administration or during the trial&#xD;
&#xD;
          -  Participation in another trial with an investigational drug within 1 month prior to&#xD;
             administration or during the trial&#xD;
&#xD;
          -  Smoker (&gt; 10 cigarettes or 3 cigars or 3 pipes/day) or inability to refrain from&#xD;
             smoking on trial days&#xD;
&#xD;
          -  Alcohol abuse (&gt; 60 g/day)&#xD;
&#xD;
          -  Drug abuse&#xD;
&#xD;
          -  Blood donation of more than 100 mL within 1 month prior to administration or during&#xD;
             the trial&#xD;
&#xD;
          -  Excessive physical activities within 5 days prior to administration or during the&#xD;
             trial&#xD;
&#xD;
          -  Any laboratory value outside the clinically accepted reference range and of clinical&#xD;
             relevance&#xD;
&#xD;
          -  History of any familial bleeding disorder&#xD;
      </textblock>
    </criteria>
    <gender>Male</gender>
    <minimum_age>18 Years</minimum_age>
    <maximum_age>50 Years</maximum_age>
    <healthy_volunteers>Accepts Healthy Volunteers</healthy_volunteers>
  </eligibility>
  <link>
    <url>http://trials.boehringer-ingelheim.com</url>
    <description>Related Info</description>
  </link>
  <verification_date>October 2014</verification_date>
  <study_first_submitted>October 2, 2014</study_first_submitted>
  <study_first_submitted_qc>October 2, 2014</study_first_submitted_qc>
  <study_first_posted type="Estimate">October 6, 2014</study_first_posted>
  <last_update_submitted>October 2, 2014</last_update_submitted>
  <last_update_submitted_qc>October 2, 2014</last_update_submitted_qc>
  <last_update_posted type="Estimate">October 6, 2014</last_update_posted>
  <responsible_party>
    <responsible_party_type>Sponsor</responsible_party_type>
  </responsible_party>
  <!-- Results have not yet been posted for this study                                          -->
</clinical_study>


download date: ClinicalTrials.gov processed this data on September 20, 2023
link text: Link to the current ClinicalTrials.gov record.
url: https://clinicaltrials.gov/ct2/show/NCT02256787
org study id: 1201.1
nct id: NCT02256787
lead sponsor: 
The objective of the current study was to investigate the safety, tolerability, and
      pharmacokinetics of BILB 1941 ZW following the administration of single rising doses from 5
      mg to 300 mg. In addition the bioavailability of the 60 mg dose given fasted and after a
      high-fat breakfast was to be be investigated
allocation: Randomized
intervention model: Parallel Assignment
primary purpose: Treatment
masking: Double
measure: Number of subjects with abnormal findings in physical examination
time frame: up to 48 hours following drug administration
measure: Number of subjects with abnormal changes in laboratory parameters
time frame: up to 48 hours following drug administration
measure: Number of subjects with clinically significant changes in vital signs
time frame: up to 48 hours following drug administration
description: Blood pressure, Pulse Rate
measure: Number of subjects with adverse events
time frame: up to 48 hours following drug administration
measure: Number of subjects with clinically significant changes in 12-lead ECG (electrocardiogram)
time frame: up to 48 hours following drug administration
measure: Assessment of tolerability by investigator on a 4-point scale
time frame: after 48 hours following drug administration
measure: Cmax (maximum concentration of the analyte in plasma)
time frame: up to 48 hours following drug administration
measure: tmax (time from dosing to maximum concentration)
time frame: up to 48 hours following drug administration
measure: AUC0-∞ (area under the concentration time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity)
time frame: up to 48 hours following drug administration
measure: 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)
time frame: up to 48 hours following drug administration
measure: λz (terminal rate constant in plasma)
time frame: up to 48 hours following drug administration
measure: t1/2 (terminal half-life of the analyte in plasma)
time frame: up to 48 hours following drug administration
measure: MRT (Mean time of residence of drug molecules in the body after intravascular administration)
time frame: up to 48 hours following drug administration
measure: Vz/F (Apparent volume of distribution during the terminal phase after extravascular administration)
time frame: up to 48 hours following drug administration
arm group label: BILB 1941 ZW - single rising dose
arm group type: Experimental
description: Single rising dose part
arm group label: Placebo
arm group type: Placebo Comparator
description: Single rising dose part
arm group label: BILB 1941 ZW - tablet - fasted
arm group type: Experimental
description: Relative bioavailability: The oral solution fasted should be compared with the solid form fasted and after a standardized breakfast
arm group label: BILB 1941 ZW - solution
arm group type: Experimental
description: Relative bioavailability: The oral solution fasted should be compared with the solid form fasted and after a standardized breakfast
arm group label: BILB 1941 ZW - tablet - fed
arm group type: Experimental
description: Relative bioavailability: The oral solution fasted should be compared with the solid form fasted and after a standardized breakfast
intervention type: Drug
intervention name: BILB 1941 ZW - single rising dose part
arm group label: BILB 1941 ZW - single rising dose
intervention type: Drug
intervention name: Placebo
arm group label: Placebo
intervention type: Drug
intervention name: BILB 1941 ZW - solution
arm group label: BILB 1941 ZW - solution
intervention type: Drug
intervention name: BILB 1941 ZW - tablet
arm group label: BILB 1941 ZW - tablet - fasted
arm group label: BILB 1941 ZW - tablet - fed
intervention type: Other
intervention name: standardized breakfast
arm group label: BILB 1941 ZW - tablet - fed
criteria: 
gender: Male
minimum age: 18 Years
maximum age: 50 Years
healthy volunteers: Accepts Healthy Volunteers
url: http://trials.boehringer-ingelheim.com
description: Related Info
responsible party type: Sponsor