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

Healthy Elderly Volunteers Clinical Trial

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

Clinical Trial Details — Status: Terminated

Administrative data

• NCT number: NCT01215552
• Other study ID #: HT-0712-006
• Secondary ID: BNL IRB #444
• Status: Terminated
• Phase: Phase 1
• First received: September 24, 2010
• Last updated: May 27, 2011
• Start date: September 2010
• Est. completion date: January 2011

Study information

• Verified date: May 2011
• Source: Dart NeuroScience, LLC
• Contact: n/a
• Is FDA regulated: No
• Health authority: United States: Food and Drug Administration
• Study type: Interventional

Clinical Trial 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.

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.

Recruitment information / eligibility

• Status: Terminated
• Enrollment: 3
• Est. completion date: January 2011
• Est. primary completion date: November 2010
• Accepts healthy volunteers: Accepts Healthy Volunteers
• Gender: Both
• Age group: 55 Years to 80 Years

Eligibility

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

Study Design

Allocation: Non-Randomized, Endpoint Classification: Pharmacokinetics/Dynamics Study, Intervention Model: Single Group Assignment, Masking: Open Label, Primary Purpose: Basic Science

Related Conditions & MeSH terms

• Healthy Elderly Volunteers

Intervention

Drug:
• HT-0712
A range of single oral dose levels will be explored, utilizing 5mg and 25mg strength capsules

Locations

Country	Name	City	State
United States	Brookhaven National Laboratory	Upton	New York

Sponsors (1)

Lead Sponsor	Collaborator
Dart NeuroScience, LLC

Country where clinical trial is conducted

United States, 

Outcome

Type	Measure	Description	Time frame	Safety issue
Primary	PET measurement of HT-0712 inhibition of [11C]R-rolipram binding	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.	1 day	No
Secondary	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-activity curves and plasma AUC will be assessed for [11C]R-rolipram at baseline and at 4-hours post oral administration of HT-0712.	1 day	No