PET Study to Evaluate Brain Receptor Occupancy, Safety and Pharmacokinetics of ITI-1284 in Healthy Subjects
Purpose
The study will be conducted as an open-label and single-center study to evaluate the occupancy of ITI-1284 to the dopamine D2 receptor, serotonin 2A (5-HT2A) receptor, and serotonin transporter (SERT) in healthy subjects.
Condition
- Healthy Volunteers
Eligibility
- Eligible Ages
- Between 18 Years and 55 Years
- Eligible Sex
- All
- Accepts Healthy Volunteers
- Yes
Inclusion Criteria
- Healthy male and female subjects between 18 and 55 years old (inclusive); - BMI inclusive of 18-32 kg/m2 at screening and a minimum weight of 50 kg; - Willingness to remain in the hospital research unit for the duration of the inpatient period.
Exclusion Criteria
- Clinically significant abnormality within 2 years of Screening that in the Investigator's opinion may place the subject at risk or interfere with study outcome variables; this includes, but is not limited to, history of or current cardiac, hepatic, renal, neurologic, gastrointestinal, pulmonary, endocrinologic, hematologic, or immunologic disease or history of malignancy; - Clinically significant abnormal findings in vital sign assessments, supine SBP > 140 mmHg or < 90 mmHg, or supine DBP >90 mmHg or < 50 mmHg or supine pulse rate > 100 bpm or < 45 bpm at Screening; - History of psychiatric condition that in the Investigator's opinion may be detrimental to participation in the study; - Any condition which would preclude MRI or PET/CT examination (eg, implanted metal, claustrophobia, unable to fit in PET/CT or MRI scanners); - Contraindications based on any previous MRI or the study MRI performed prior to the baseline PET/CT scan.
Study Design
- Phase
- Phase 1
- Study Type
- Interventional
- Allocation
- Non-Randomized
- Intervention Model
- Parallel Assignment
- Intervention Model Description
- This study includes up to 3 sequential parts (Parts A, B and C). In Part A, subjects will be assigned to 1 of 3 cohorts, will receive a single dose of ITI-1284, and undergo one postdose PET/CT scan starting at 1 hour postdose. In Part B, subjects will be assigned to 1 of 2 cohorts, will receive a single dose of ITI-1284, and undergo one postdose PET/CT scan starting at 1 hour postdose. In Part C, subjects will receive a single dose of ITI-1284 and undergo one postdose PET/CT scans starting at approximately 24 hours postdose.
- Primary Purpose
- Treatment
- Masking
- None (Open Label)
Arm Groups
| Arm | Description | Assigned Intervention |
|---|---|---|
|
Experimental Cohort A1: 10 mg ITI-1284 |
Radioligand: [11C]-raclopride |
|
|
Experimental Cohort A2: 20 mg ITI-1284 |
Radioligand: [11C]-raclopride |
|
|
Experimental Cohort A3: 30 mg ITI-1284 |
Radioligand: [11C]-raclopride |
|
|
Experimental Cohort B1: 20 mg ITI-1284 |
Radioligand: [11C]-MDL100907 |
|
|
Experimental Cohort B2: 20 mg ITI-1284 |
Radioligand: [11C]-DASB |
|
|
Experimental Cohort C1: 20 mg ITI-1284 |
Radioligand: [11C]-raclopride or [11C]-MDL100907 |
|
Recruiting Locations
Yale University School Of Medicine
New Haven, Connecticut 06519
New Haven, Connecticut 06519
More Details
- Status
- Recruiting
- Sponsor
- Intra-Cellular Therapies, Inc.
Detailed Description
This study consists of up to 3 sequential parts. Part A will evaluate the D2 receptor occupancy for ITI-1284 at three dose levels. Part B will evaluate the 5HT-2A receptor and SERT occupancy for ITI-1284 at one dose level. Part C will evaluate the late postdose receptor occupancy of ITI-1284 on the D2 or 5-HT2A receptor at one dose level.