Trial record 1 of 2 for:    HT-0712
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Study of the Inhibition of [11C]R-rolipram Binding to Brain Phosphodiesterase - 4 (PDE-4) by HT-0712

This study has been terminated.
(The experimental design was not sufficient to answer the proposed questions. A new study design is now being considered.)
Sponsor:
Information provided by:
Dart NeuroScience, LLC
ClinicalTrials.gov Identifier:
NCT01215552
First received: September 24, 2010
Last updated: May 27, 2011
Last verified: May 2011
  Purpose

This Positron Emission Tomography (PET) imaging study is designed to explore the relationship between HT-0712 dose level and inhibition of brain phosphodiesterase-4 activity, in order to optimize the dosage regimens utilized in subsequent trials.


Condition Intervention Phase
Healthy Elderly Volunteers
Drug: HT-0712
Phase 1

Study Type: Interventional
Study Design: Allocation: Non-Randomized
Endpoint Classification: Pharmacokinetics/Dynamics Study
Intervention Model: Single Group Assignment
Masking: Open Label
Primary Purpose: Basic Science
Official Title: A PET Study: Single-dose, Open-label Study of the Inhibition of [11C]R-rolipram Binding to Brain Phosphodiesterase - 4 (PDE-4) by HT-0712

Further study details as provided by Dart NeuroScience, LLC:

Primary Outcome Measures:
  • PET measurement of HT-0712 inhibition of [11C]R-rolipram binding [ Time Frame: 1 day ] [ Designated as safety issue: No ]
    To demonstrate Central Nervous System (CNS) exposure and dose-related inhibition of [11C]R-rolipram binding in brain regions of interest by HT-0712 when compared to baseline [11C]R-rolipram binding in the same individual.


Secondary Outcome Measures:
  • Brain uptake of [11C]R-rolipram, as determined by PET imaging, associated with both maximal plasma concentration of HT-0712 (Tmax) and overall plasma level exposure (AUC) following administration of different dose levels of HT-0712. [ Time Frame: 1 day ] [ Designated as safety issue: No ]
    Time-activity curves and plasma AUC will be assessed for [11C]R-rolipram at baseline and at 4-hours post oral administration of HT-0712.


Enrollment: 3
Study Start Date: September 2010
Study Completion Date: January 2011
Primary Completion Date: November 2010 (Final data collection date for primary outcome measure)
Arms Assigned Interventions
Experimental: HT-0712 Drug: HT-0712
A range of single oral dose levels will be explored, utilizing 5mg and 25mg strength capsules

Detailed Description:

The objective of this project is to demonstrate the inhibition of human brain PDE4 by HT-0712, by measuring the inhibition of [11C]R-rolipram binding, a radiotracer which also binds to and inhibits PDE4. Plasma samples will be drawn to determine if there is a relationship between plasma pharmacokinetics of HT-0712 and its pharmacodynamic effect, as determined through the inhibition of [11C]R-rolipram binding in the brain.

  Eligibility

Ages Eligible for Study:   55 Years to 80 Years
Genders Eligible for Study:   Both
Accepts Healthy Volunteers:   Yes
Criteria

Main Inclusion Criteria:

  • Healthy, elderly, non-smoking men and post-menopausal women
  • Ability to give informed consent

Main Exclusion Criteria:

  • Current or history of uncontrolled hypertension, major depression, Parkinson's disease, stroke and diabetes.
  • Physical or behavioral conditions that may alter brain function
  Contacts and Locations
Please refer to this study by its ClinicalTrials.gov identifier: NCT01215552

Locations
United States, New York
Brookhaven National Laboratory
Upton, New York, United States, 11973
Sponsors and Collaborators
Dart NeuroScience, LLC
Investigators
Study Director: Philip Perera, MD Dart NeuroScience, LLC
  More Information

No publications provided

Responsible Party: Dr. Philip Perera, MD, Helicon Therapeutics
ClinicalTrials.gov Identifier: NCT01215552     History of Changes
Other Study ID Numbers: HT-0712-006, BNL IRB #444
Study First Received: September 24, 2010
Last Updated: May 27, 2011
Health Authority: United States: Food and Drug Administration

Additional relevant MeSH terms:
Rolipram
Phosphodiesterase 4 Inhibitors
Phosphodiesterase Inhibitors
Enzyme Inhibitors
Molecular Mechanisms of Pharmacological Action
Pharmacologic Actions
Antidepressive Agents
Psychotropic Drugs
Central Nervous System Agents
Therapeutic Uses

ClinicalTrials.gov processed this record on April 20, 2014