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

Phase 1

Recruiting

• Conditions: Healthy Volunteers
• Interventions: Drug: ITI-1284 10 mg; Drug: ITI-1284 20 mg

• Registration Number: NCT06299410
• Lead Sponsor: Intra-Cellular Therapies, Inc.

Brief Summary

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.

Detailed Description

This study consists of up to 3 sequential parts. Part A will evaluate the D2 receptor occupancy for ITI-1284 at two dose levels. Part B will evaluate the 5HT-2A receptor and SERT occupancy for ITI-1284 at one dose level. Part C (optional) will evaluate the time course of receptor occupancy of ITI-1284 on the D2 or 5-HT2A receptor at one dose level.

Study Timeline

• Study First Submitted: 2024-03-01
• Study First Submitted QC: 2024-03-01
• Study First Posted: 2024-03-07
• Study Start: 2024-04-11
• Status Verified: 2025-01
• Last Update Submitted: 2025-01-24
• Last Update Posted: 2025-01-28
• Primary Completion: 2025-09
• Study Completion: 2025-09

Recruitment & Eligibility

• Status: RECRUITING
• Sex: All
• Target Recruitment: 30

Inclusion Criteria

• Healthy male and female subjects between 18 and 50 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 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

• Study Type: INTERVENTIONAL
• Study Design: SEQUENTIAL

Arm && Interventions

Group	Intervention	Description
Cohort A1: 10 mg ITI-1284	ITI-1284 10 mg	Radioligand: \[11C\]-raclopride
Cohort A2: 20 mg ITI-1284	ITI-1284 20 mg	Radioligand: \[11C\]-raclopride
Cohort B1: 20 mg ITI-1284	ITI-1284 20 mg	Radioligand: \[11C\]-MDL100907
Cohort B2: 20 mg ITI-1284	ITI-1284 20 mg	Radioligand: \[11C\]-DASB
Cohort C: 20 mg ITI-1284	ITI-1284 20 mg	Radioligand: \[11C\]-MDL100907 or \[11C\]-raclopride

Primary Outcome Measures

Name	Time	Method
% Receptor occupancy	Day 1	Percent change of binding potential from baseline

Secondary Outcome Measures

Name	Time	Method
Pharmacokinetics: AUC0-t	Day 1	Area under the plasma drug concentration-time curve (AUC) from time zero to the last measurable concentration
Pharmacokinetics: Cmax	Day 1	Maximum plasma concentration
Pharmacokinetics: Tmax	Day 1	Time of maximum plasma concentration
Percentage of subjects with treatment-emergent adverse events	Up to 30 days after the dose of study drug
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

Trial Locations

Locations (1)

Clinical Site 1; 🇺🇸 New Haven, Connecticut, United States