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.
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 Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
BASIC_SCIENCE
Masking
NONE
Enrollment
3
A range of single oral dose levels will be explored, utilizing 5mg and 25mg strength capsules
Brookhaven National Laboratory
Upton, New York, United States
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.
Time frame: 1 day
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.
Time frame: 1 day
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