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| ID | Type | Description | Link |
|---|---|---|---|
| BNL IRB #444 | Other Identifier | Brookhaven National Laboratory |
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The experimental design was not sufficient to answer the proposed questions. A new study design is now being considered.
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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.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| HT-0712 | Experimental |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| HT-0712 | Drug | A range of single oral dose levels will be explored, utilizing 5mg and 25mg strength capsules |
|
| Measure | Description | Time Frame |
|---|---|---|
| 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 |
| Measure | Description | Time Frame |
|---|---|---|
| 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 |
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Main Inclusion Criteria:
Main Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Philip Perera, MD | Dart NeuroScience, LLC | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Brookhaven National Laboratory | Upton | New York | 11973 | United States |
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| ID | Term |
|---|---|
| C000599150 | HT-0712 |
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