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
Choosing to participate in a study is an important personal decision. Talk with your doctor and family members or friends about deciding to join a study. To learn more about this study, you or your doctor may contact the study research staff using the Contacts provided below. For general information, see Learn About Clinical Studies.

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 July 26, 2014