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.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
7
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
Subjects will be injected with approximately 250 MBq or 6.75 mCi of \[18F\]Fallypride \[5-6 mCi being the typical range of injected dose\].
Indiana Clinical Research Center, IU Health University Hospital
Indianapolis, Indiana, United States
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
Time frame: approximately 5 weeks
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.
Time frame: approximately 5 weeks
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