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

ArmDescriptionAssigned Intervention
Experimental
Cohort A1: 10 mg ITI-1284 		Radioligand: [11C]-raclopride
  • Drug: ITI-1284 10 mg
    ITI-1284 tablet
Experimental
Cohort A2: 20 mg ITI-1284 		Radioligand: [11C]-raclopride
  • Drug: ITI-1284 20 mg
    ITI-1284 tablet
Experimental
Cohort A3: 30 mg ITI-1284 		Radioligand: [11C]-raclopride
  • Drug: ITI-1284 10 mg
    ITI-1284 tablet
  • Drug: ITI-1284 20 mg
    ITI-1284 tablet
Experimental
Cohort B1: 20 mg ITI-1284 		Radioligand: [11C]-MDL100907
  • Drug: ITI-1284 20 mg
    ITI-1284 tablet
Experimental
Cohort B2: 20 mg ITI-1284 		Radioligand: [11C]-DASB
  • Drug: ITI-1284 20 mg
    ITI-1284 tablet
Experimental
Cohort C1: 20 mg ITI-1284 		Radioligand: [11C]-raclopride or [11C]-MDL100907
  • Drug: ITI-1284 20 mg
    ITI-1284 tablet

Recruiting Locations

Yale University School Of Medicine
New Haven, Connecticut 06519

More Details

Status
Recruiting
Sponsor
Intra-Cellular Therapies, Inc.

Study Contact

ITI Clinical Trials
646 440-9333
ITCIClinicalTrials@itci-inc.com

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.