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This study involves evaluating the occupancy of ATI-9242 at steady state at three different dose levels on D2 receptors in the brain using [18F] Fallypride PET in up to three cohorts of subjects.
This study involves evaluating the occupancy of ATI-9242 at steady state at three different dose levels on D2 receptors in the brain using [18F]Fallypride PET in up to three cohorts of subjects. The first dose evaluated will be 0.5 mg/kg administered as an IV bolus injection. The second dose that will be evaluated will be 1.0 mg/kg as an IV bolus injection. The safety and occupancy after each dose level will be evaluated prior to moving to the next dose. On two separate days, subjects will undergo [18F]Fallypride PET imaging sessions. The plasma concentration of ATI-9242 will be obtained prior to and during the course of the imaging session to allow determination of the relationship between plasma concentration of ATI-9242 with in vivo D2 occupancy.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| 0.5 mg/kg | Experimental | • Cohort 1: ATI-9242 - Single IV bolus dose of 0.5 mg/kg |
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| ATI-9242 1.0 mg/kg | Experimental | • Cohort 2: ATI-9242 - Single IV bolus dose of 1.0 mg/kg |
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| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| ATI-9242 | Drug | Formulated ATI-9242 will be administered as an IV bolus injection (2mg/mL of ATI-9242 in 40% solution of propylene glycol). Two doses will be tested: single IV bolus injection of 0.5mg/kg and single IV bolus injection 1.0 mg/kg. In the event that a third cohort is needed the IV bolus injection would be 2.0 mg/kg |
| Measure | Description | Time Frame |
|---|---|---|
| Target receptor occupancy after single intravenous(IV) of ATI-9242 in 6 healthy adults using the D2 receptor ligand [18F]Fallypride and PET imaging. | Change from baseline in PET imaging at baseline of ATI-9242 and post-dose | approximately 5 weeks |
| Measure | Description | Time Frame |
|---|---|---|
| Explore the relationship between ATI-9242 dose, plasma concentrations of ATI-9242 and target receptor occupancy in 6 subjects. | The relationship between plasma drug concentration/PK parameters of ATI-9242 and D2 occupancy will be explored. | approximately 5 weeks |
| Measure | Description | Time Frame |
|---|---|---|
| Safety and tolerability of ATI-9242 following single IV dose in 6 healthy subjects via safety assessments . | incidence of adverse events (AEs), vital signs (blood pressure, pulse and oral temperature), physical examinations 12-lead ECG, CSSRS and clinical laboratory tests (hematology, clinical chemistry and urinalysis). | approximately 5 weeks |
Inclusion Criteria:
Exclusion Criteria:
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| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Indiana Clinical Research Center, IU Health University Hospital | Indianapolis | Indiana | 46202 | United States |
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| ID | Term |
|---|---|
| D012559 | Schizophrenia |
| ID | Term |
|---|---|
| D019967 | Schizophrenia Spectrum and Other Psychotic Disorders |
| D001523 | Mental Disorders |
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| [18F]Fallypride Imaging | Radiation | Subjects will be injected with approximately 250 MBq or 6.75 mCi of [18F]Fallypride [5-6 mCi being the typical range of injected dose]. |
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