Study of the Inhibition of [11C]R-rolipram Binding to Brain Phosphodiesterase - 4 (PDE-4) by HT-0712

Sponsor

Dart NeuroScience, LLC (Industry)

Overall Status

Terminated

CT.gov ID

NCT01215552

Collaborator

(none)

Enrollment

Location

Arm

Duration (Months)

0.7

Patients Per Site Per Month

Study Details

Study Description

Brief Summary

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 or Disease	Intervention/Treatment	Phase
Healthy Elderly Volunteers	Drug: HT-0712	Phase 1

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.

Study Design

Study Type:

Interventional

Actual Enrollment :

3 participants

Allocation:

Non-Randomized

Intervention Model:

Single Group Assignment

Masking:

None (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

Study Start Date :

Sep 1, 2010

Actual Primary Completion Date :

Nov 1, 2010

Actual Study Completion Date :

Jan 1, 2011

Arms and Interventions

Arm	Intervention/Treatment
Experimental: HT-0712	Drug: HT-0712 A range of single oral dose levels will be explored, utilizing 5mg and 25mg strength capsules

Arm

Intervention/Treatment

Experimental: HT-0712

Drug: HT-0712

A range of single oral dose levels will be explored, utilizing 5mg and 25mg strength capsules

Outcome Measures

Primary Outcome Measures

PET measurement of HT-0712 inhibition of [11C]R-rolipram binding [1 day]
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. [1 day]
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.

Eligibility Criteria

Criteria

Ages Eligible for Study:

55 Years to 80 Years

Sexes Eligible for Study:

All

Accepts Healthy Volunteers:

Yes

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

Locations

	Site	City	State	Country	Postal Code
1	Brookhaven National Laboratory	Upton	New York	United States	11973

Sponsors and Collaborators

Dart NeuroScience, LLC

Investigators

Study Director: Philip Perera, MD, Dart NeuroScience, LLC

Study Documents (Full-Text)

None provided.

More Information

Publications

None provided.

Responsible Party:

, ,

ClinicalTrials.gov Identifier:

NCT01215552

Other Study ID Numbers:

HT-0712-006
BNL IRB #444

First Posted:

Oct 6, 2010

Last Update Posted:

Jun 1, 2011

Last Verified:

May 1, 2011

Study Results

No Results Posted as of Jun 1, 2011