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

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

Status

Terminated

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT01215552

Enrollment

Registered

2010-10-06

Start date

2010-09-30

Completion date

2011-01-31

Last updated

2011-06-01

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Healthy Elderly Volunteers

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.

Interventions

DRUGHT-0712

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

Study design

Allocation

NON_RANDOMIZED

Intervention model

SINGLE_GROUP

Primary purpose

BASIC_SCIENCE

Masking

NONE

Eligibility

Sex/Gender

ALL

Age

55 Years to 80 Years

Healthy volunteers

Yes

Inclusion 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

Design outcomes

Primary

Measure	Time frame	Description
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

Measure	Time frame	Description
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.

Countries

United States

Outcome results

None listed

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026