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

Phase 1

Terminated

• Conditions: Healthy Elderly Volunteers
• Interventions: Drug: HT-0712

• Registration Number: NCT01215552
• Lead Sponsor: Dart NeuroScience, LLC

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.

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 Timeline

• Study Start: 2010-09
• Study First Submitted: 2010-09-24
• Study First Submitted QC: 2010-10-05
• Study First Posted: 2010-10-06
• Primary Completion: 2010-11
• Study Completion: 2011-01
• Status Verified: 2011-05
• Last Update Submitted: 2011-05-27
• Last Update Posted: 2011-06-01

Recruitment & Eligibility

• Status: TERMINATED
• Sex: All
• Target Recruitment: 3

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

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: SINGLE_GROUP

Arm && Interventions

Group	Intervention	Description
HT-0712	HT-0712	-

Primary Outcome Measures

Name	Time	Method
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

Name	Time	Method
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.

Trial Locations

Locations (1)

Brookhaven National Laboratory; 🇺🇸 Upton, New York, United States