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
Overview
- Phase
- Phase 1
- Intervention
- HT-0712
- Conditions
- Healthy Elderly Volunteers
- Sponsor
- Dart NeuroScience, LLC
- Enrollment
- 3
- Locations
- 1
- Primary Endpoint
- PET measurement of HT-0712 inhibition of [11C]R-rolipram binding
- Status
- Terminated
- Last Updated
- 14 years ago
Overview
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.
Investigators
Eligibility Criteria
Inclusion Criteria
- •Healthy, elderly, non-smoking men and post-menopausal women
- •Ability to give informed consent
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
Arms & Interventions
HT-0712
Intervention: HT-0712
Outcomes
Primary Outcomes
PET measurement of HT-0712 inhibition of [11C]R-rolipram binding
Time Frame: 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 Outcomes
- 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)