PET Study to Evaluate Brain Receptor Occupancy, Safety and Pharmacokinetics of ITI-1284 in Healthy Subjects

An Open-label, Positron Emission Tomography Study to Evaluate Brain Receptor Occupancy, Safety, Tolerability, and Pharmacokinetics After a Single Sublingual Administration of ITI-1284 in Healthy Subjects

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.

Study Overview

• Status: Recruiting
• Conditions: Healthy Volunteers
• Intervention / Treatment: Drug: ITI-1284 10 mg; Drug: ITI-1284 20 mg

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.

• Study Type: Interventional
• Enrollment (Estimated): 42
• Phase: Phase 1

Contacts and Locations

• Study Contact: Name: ITI Clinical Trials; Phone Number: 646 440-9333; Email: ITCIClinicalTrials@itci-inc.com

Study Locations

• United States
  • Connecticut
    • New Haven, Connecticut, United States, 06520
      • Recruiting
      • Clinical Site 1

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: Adult
• Accepts Healthy Volunteers: Yes

Description

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 Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Non-Randomized
• Interventional Model: Parallel Assignment
• Masking: None (Open Label)

Number of Arms

6

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
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 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 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 C1: 20 mg ITI-1284; Radioligand: [11C]-raclopride or [11C]-MDL100907	Drug: ITI-1284 20 mg; ITI-1284 tablet

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
% Receptor occupancy	Percent change of binding potential from baseline	Day 1

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Percentage of subjects with treatment-emergent adverse events		Up to 30 days after the dose of study drug
Pharmacokinetics: AUC0-t	Area under the plasma drug concentration-time curve (AUC) from time zero to the last measurable concentration	Day 1
Pharmacokinetics: Cmax	Maximum plasma concentration	Day 1
Pharmacokinetics: Tmax	Time of maximum plasma concentration	Day 1
Change from baseline in ECG QT interval		Day 3
Change from baseline in aspartate aminotransferase		Day 3
Change from baseline in alanine aminotransferase		Day 3

Collaborators and Investigators

• Sponsor: Intra-Cellular Therapies, Inc.

Study record dates

Study Major Dates

• Study Start (Actual): April 11, 2024
• Primary Completion (Estimated): July 1, 2026
• Study Completion (Estimated): July 1, 2026

Study Registration Dates

• First Submitted: March 1, 2024
• First Submitted That Met QC Criteria: March 1, 2024
• First Posted (Actual): March 7, 2024

Study Record Updates

• Last Update Posted (Actual): May 26, 2026
• Last Update Submitted That Met QC Criteria: May 21, 2026
• Last Verified: May 1, 2026

More Information

Terms related to this study

• Other Study ID Numbers: ITI-1284-008

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: NO

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: Yes
• Studies a U.S. FDA-regulated device product: No