Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of ESR 1150 CL in Healthy Subjects

NCT02209688 | Terminated Phase 1

• 1 other identifier: 1172.2
• Study Type: interventional
• Target: 39
• Locations: 0 countries
• Sites: N/A

Brief Summary

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.

Conditions

Healthy

Outcome Measures

Primary Outcomes (16)

• Number of patients with adverse events

  up to 30 days

• Area under the curve (AUC)

  up to 24 hours after administration

• Maximum concentration (Cmax)

  up to 24 hours after administration

• Time to maximum concentration (tmax)

  up to 24 hours after administration

• Apparent total plasma clearance (CLtot/f)

  up to 24 hours after administration

• Apparent volume of distribution (Vz/f)

  up to 24 hours after administration

• Elimination half-life (t1/2)

  up to 24 hours after administration

• Amount excreted in urine (Ae)

  up to 24 hours after administration

• Maximum flow rate (Qmax)

  assessed by free uroflowmetry

  up to 8 hours after administration

• Average flow rate (Qave)

  assessed by free uroflowmetry

  up to 8 hours after administration

• Voided volume (Vcomp)

  assessed by free uroflowmetry

  up to 8 hours after administration

• Voiding time (T100)

  assessed by free uroflowmetry

  up to 8 hours after administration

• Time to maximum flow (TQmax)

  assessed by free uroflowmetry

  up to 8 hours after administration

• Residual urinary volume

  assessed by means of transabdominal ultrasound evaluation

  up to 8 hours after administration

• Assessment of micturition pattern

  evaluated by Independent reviewer

  up to 8 hours after administration

• Amount of inhibition constants (Ki) at α1A, adrenoreceptor subtype level

  assessed by ex vivo radioreceptor assay

  up to 8 hours after administration

Study Arms (3)

ESR 1150 CL dose escalation fasted

EXPERIMENTAL

Drug: ESR 1150 CL

ESR 1150 CL fed

EXPERIMENTAL

Drug: ESR 1150 CL

Placebo

PLACEBO COMPARATOR

Drug: Placebo

Interventions

ESR 1150 CL DRUG

ESR 1150 CL dose escalation fasted; ESR 1150 CL fed

Placebo DRUG

Placebo

Eligibility Criteria

• Age: 18 Years - 50 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Healthy male and female Caucasian subjects as determined by results of screening
• Written informed consent in accordance with Good Clinical Practice and local legislation given
• Age ≥ 18 and ≤ 50 years
• Broca ≥ - 20 % and ≤ + 20 %
• for first part of study: extensive metabolizers of CYP2D6 and/or "spartein" type; for second part of study: poor metabolizers of CYP2D6 and/or "spartein"

You may not qualify if:

• Any finding of the medical examination (including blood pressure, pulse rate and electrocardiogram) deviating from normal and of clinical relevance
• Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders
• Surgery of gastrointestinal tract (except appendectomy)
• Diseases of the central nervous system (such as epilepsy) or psychiatric disorders of neurological disorders
• History of orthostatic hypotension, fainting spells or blackouts
• 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) (≤ 1 month prior to administration or during the trial, except for oral contraceptives)
• Use of any drugs which might influence the results of the trial (≤ 10 days prior to administration or during the trial except for oral contraceptives)
• Participation in another trial with an investigational drug (≤ 2 months prior to administration or during the trial)
• Smoker (\> 10 cigarettes or \> 3 cigars or \> 3 pipes/day)
• Inability to refrain from smoking on trial days
• Alcohol abuse (\> 60 g/days)
• Drug abuse
• Blood donation \> 100 ml (≤ 4 weeks prior to administration or during the trial)

Sponsors & Collaborators

• Boehringer Ingelheim: lead

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: August 5, 2014
• First Posted: August 6, 2014
• Study Start: February 1, 2000
• Primary Completion: March 1, 2000
• Last Updated: August 6, 2014

Record last verified: 2014-08