<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/NCT02209688</url>
  </required_header>
  <id_info>
    <org_study_id>1172.2</org_study_id>
    <nct_id>NCT02209688</nct_id>
  </id_info>
  <brief_title>Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of ESR 1150 CL in Healthy Subjects</brief_title>
  <official_title>Administration of ESR 1150 CL in Ascending Doses of 0.5, 1, 2, 4 and 8 mg in an Open, Group Comparison and Placebo-controlled Design (Placebo Randomised Double Blind in the Dose Groups) for the Assessment of Safety, Tolerability (Maximum Tolerated Dose, MTD), Pharmacokinetics and Pharmacodynamics in 5 Groups of 8 Female and 5 Male Healthy Subjects, and 4 mg Additionally in Fed State, in a Cross Over Design. Safety, Tolerability and Pharmacokinetics of MTD/4, MTD/2 and MTD in 6 Healthy Male Subjects, Identified as CYP2D6 and/or &quot;Spartein&quot; Poor Metabolizers, in a 3-fold Cross Over, Open Study.</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 this study was to obtain safety and tolerability data and first&#xD;
      pharmacokinetic and pharmacodynamic data of escalating doses of ESR 1150 CL.&#xD;
    </textblock>
  </brief_summary>
  <overall_status>Terminated</overall_status>
  <start_date>February 2000</start_date>
  <primary_completion_date type="Actual">March 2000</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>Crossover Assignment</intervention_model>
    <primary_purpose>Treatment</primary_purpose>
    <masking>None (Open Label)</masking>
  </study_design_info>
  <primary_outcome>
    <measure>Number of patients with adverse events</measure>
    <time_frame>up to 30 days</time_frame>
  </primary_outcome>
  <primary_outcome>
    <measure>Area under the curve (AUC)</measure>
    <time_frame>up to 24 hours after administration</time_frame>
  </primary_outcome>
  <primary_outcome>
    <measure>Maximum concentration (Cmax)</measure>
    <time_frame>up to 24 hours after administration</time_frame>
  </primary_outcome>
  <primary_outcome>
    <measure>Time to maximum concentration (tmax)</measure>
    <time_frame>up to 24 hours after administration</time_frame>
  </primary_outcome>
  <primary_outcome>
    <measure>Apparent total plasma clearance (CLtot/f)</measure>
    <time_frame>up to 24 hours after administration</time_frame>
  </primary_outcome>
  <primary_outcome>
    <measure>Apparent volume of distribution (Vz/f)</measure>
    <time_frame>up to 24 hours after administration</time_frame>
  </primary_outcome>
  <primary_outcome>
    <measure>Elimination half-life (t1/2)</measure>
    <time_frame>up to 24 hours after administration</time_frame>
  </primary_outcome>
  <primary_outcome>
    <measure>Amount excreted in urine (Ae)</measure>
    <time_frame>up to 24 hours after administration</time_frame>
  </primary_outcome>
  <primary_outcome>
    <measure>Maximum flow rate (Qmax)</measure>
    <time_frame>up to 8 hours after administration</time_frame>
    <description>assessed by free uroflowmetry</description>
  </primary_outcome>
  <primary_outcome>
    <measure>Average flow rate (Qave)</measure>
    <time_frame>up to 8 hours after administration</time_frame>
    <description>assessed by free uroflowmetry</description>
  </primary_outcome>
  <primary_outcome>
    <measure>Voided volume (Vcomp)</measure>
    <time_frame>up to 8 hours after administration</time_frame>
    <description>assessed by free uroflowmetry</description>
  </primary_outcome>
  <primary_outcome>
    <measure>Voiding time (T100)</measure>
    <time_frame>up to 8 hours after administration</time_frame>
    <description>assessed by free uroflowmetry</description>
  </primary_outcome>
  <primary_outcome>
    <measure>Time to maximum flow (TQmax)</measure>
    <time_frame>up to 8 hours after administration</time_frame>
    <description>assessed by free uroflowmetry</description>
  </primary_outcome>
  <primary_outcome>
    <measure>Residual urinary volume</measure>
    <time_frame>up to 8 hours after administration</time_frame>
    <description>assessed by means of transabdominal ultrasound evaluation</description>
  </primary_outcome>
  <primary_outcome>
    <measure>Assessment of micturition pattern</measure>
    <time_frame>up to 8 hours after administration</time_frame>
    <description>evaluated by Independent reviewer</description>
  </primary_outcome>
  <primary_outcome>
    <measure>Amount of inhibition constants (Ki) at α1A, adrenoreceptor subtype level</measure>
    <time_frame>up to 8 hours after administration</time_frame>
    <description>assessed by ex vivo radioreceptor assay</description>
  </primary_outcome>
  <number_of_arms>3</number_of_arms>
  <enrollment type="Actual">39</enrollment>
  <condition>Healthy</condition>
  <arm_group>
    <arm_group_label>ESR 1150 CL dose escalation fasted</arm_group_label>
    <arm_group_type>Experimental</arm_group_type>
  </arm_group>
  <arm_group>
    <arm_group_label>ESR 1150 CL fed</arm_group_label>
    <arm_group_type>Experimental</arm_group_type>
  </arm_group>
  <arm_group>
    <arm_group_label>Placebo</arm_group_label>
    <arm_group_type>Placebo Comparator</arm_group_type>
  </arm_group>
  <intervention>
    <intervention_type>Drug</intervention_type>
    <intervention_name>ESR 1150 CL</intervention_name>
    <arm_group_label>ESR 1150 CL dose escalation fasted</arm_group_label>
    <arm_group_label>ESR 1150 CL fed</arm_group_label>
  </intervention>
  <intervention>
    <intervention_type>Drug</intervention_type>
    <intervention_name>Placebo</intervention_name>
    <arm_group_label>Placebo</arm_group_label>
  </intervention>
  <eligibility>
    <criteria>
      <textblock>
        Inclusion Criteria:&#xD;
&#xD;
          -  Healthy male and female Caucasian subjects as determined by results of screening&#xD;
&#xD;
          -  Written informed consent in accordance with Good Clinical Practice and local&#xD;
             legislation given&#xD;
&#xD;
          -  Age ≥ 18 and ≤ 50 years&#xD;
&#xD;
          -  Broca ≥ - 20 % and ≤ + 20 %&#xD;
&#xD;
          -  for first part of study: extensive metabolizers of CYP2D6 and/or &quot;spartein&quot; type; for&#xD;
             second part of study: poor metabolizers of CYP2D6 and/or &quot;spartein&quot;&#xD;
&#xD;
        Exclusion Criteria:&#xD;
&#xD;
          -  Any finding of the medical examination (including blood pressure, pulse rate and&#xD;
             electrocardiogram) deviating from normal and of clinical relevance&#xD;
&#xD;
          -  Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic,&#xD;
             immunological or hormonal disorders&#xD;
&#xD;
          -  Surgery of gastrointestinal tract (except appendectomy)&#xD;
&#xD;
          -  Diseases of the central nervous system (such as epilepsy) or psychiatric disorders of&#xD;
             neurological disorders&#xD;
&#xD;
          -  History of orthostatic hypotension, fainting spells or blackouts&#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) (≤ 1 month prior to administration&#xD;
             or during the trial, except for oral contraceptives)&#xD;
&#xD;
          -  Use of any drugs which might influence the results of the trial (≤ 10 days prior to&#xD;
             administration or during the trial except for oral contraceptives)&#xD;
&#xD;
          -  Participation in another trial with an investigational drug (≤ 2 months prior to&#xD;
             administration or during the trial)&#xD;
&#xD;
          -  Smoker (&gt; 10 cigarettes or &gt; 3 cigars or &gt; 3 pipes/day)&#xD;
&#xD;
          -  Inability to refrain from smoking on trial days&#xD;
&#xD;
          -  Alcohol abuse (&gt; 60 g/days)&#xD;
&#xD;
          -  Drug abuse&#xD;
&#xD;
          -  Blood donation &gt; 100 ml (≤ 4 weeks prior to administration or during the trial)&#xD;
&#xD;
          -  Excessive physical activities (≤ 10 days prior to administration or during the trial)&#xD;
&#xD;
          -  Any laboratory value outside the reference range of clinical relevance&#xD;
&#xD;
          -  Females only:&#xD;
&#xD;
               -  No reliable contraception (examples of reliable contraception: oral&#xD;
                  contraceptives, 3-month injection, intrauterine device, sterilisation, condoms +&#xD;
                  spermicide)&#xD;
&#xD;
               -  pregnancy or breast feeding period&#xD;
      </textblock>
    </criteria>
    <gender>All</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>August 2014</verification_date>
  <study_first_submitted>August 5, 2014</study_first_submitted>
  <study_first_submitted_qc>August 5, 2014</study_first_submitted_qc>
  <study_first_posted type="Estimate">August 6, 2014</study_first_posted>
  <last_update_submitted>August 5, 2014</last_update_submitted>
  <last_update_submitted_qc>August 5, 2014</last_update_submitted_qc>
  <last_update_posted type="Estimate">August 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/NCT02209688
org study id: 1172.2
nct id: NCT02209688
lead sponsor: 
The objective of this study was to obtain safety and tolerability data and first
      pharmacokinetic and pharmacodynamic data of escalating doses of ESR 1150 CL.
allocation: Randomized
intervention model: Crossover Assignment
primary purpose: Treatment
masking: None (Open Label)
measure: Number of patients with adverse events
time frame: up to 30 days
measure: Area under the curve (AUC)
time frame: up to 24 hours after administration
measure: Maximum concentration (Cmax)
time frame: up to 24 hours after administration
measure: Time to maximum concentration (tmax)
time frame: up to 24 hours after administration
measure: Apparent total plasma clearance (CLtot/f)
time frame: up to 24 hours after administration
measure: Apparent volume of distribution (Vz/f)
time frame: up to 24 hours after administration
measure: Elimination half-life (t1/2)
time frame: up to 24 hours after administration
measure: Amount excreted in urine (Ae)
time frame: up to 24 hours after administration
measure: Maximum flow rate (Qmax)
time frame: up to 8 hours after administration
description: assessed by free uroflowmetry
measure: Average flow rate (Qave)
time frame: up to 8 hours after administration
description: assessed by free uroflowmetry
measure: Voided volume (Vcomp)
time frame: up to 8 hours after administration
description: assessed by free uroflowmetry
measure: Voiding time (T100)
time frame: up to 8 hours after administration
description: assessed by free uroflowmetry
measure: Time to maximum flow (TQmax)
time frame: up to 8 hours after administration
description: assessed by free uroflowmetry
measure: Residual urinary volume
time frame: up to 8 hours after administration
description: assessed by means of transabdominal ultrasound evaluation
measure: Assessment of micturition pattern
time frame: up to 8 hours after administration
description: evaluated by Independent reviewer
measure: Amount of inhibition constants (Ki) at α1A, adrenoreceptor subtype level
time frame: up to 8 hours after administration
description: assessed by ex vivo radioreceptor assay
arm group label: ESR 1150 CL dose escalation fasted
arm group type: Experimental
arm group label: ESR 1150 CL fed
arm group type: Experimental
arm group label: Placebo
arm group type: Placebo Comparator
intervention type: Drug
intervention name: ESR 1150 CL
arm group label: ESR 1150 CL dose escalation fasted
arm group label: ESR 1150 CL fed
intervention type: Drug
intervention name: Placebo
arm group label: Placebo
criteria: 
gender: All
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