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

Intra-Cellular Therapies

Status and phase: Enrolling; Phase 1

Conditions: Healthy Volunteers

Treatments: Drug: ITI-1284 10 mg; Drug: ITI-1284 20 mg

Study type: Interventional

Funder types: Industry

Identifiers

NCT06299410

ITI-1284-008

Details and patient eligibility

About

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.

Full 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.

Enrollment: 42 estimated patients

Sex: All

Ages: 18 to 55 years old

Volunteers: Accepts Healthy Volunteers

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.

Trial design

Primary purpose: Treatment

Allocation: Non-Randomized

Interventional model: Parallel Assignment

Masking: None (Open label)

---

42 participants in 6 patient groups

Cohort A1: 10 mg ITI-1284

Experimental group

Description:

Radioligand: \[11C\]-raclopride

Treatment:

Drug: ITI-1284 10 mg

Cohort A2: 20 mg ITI-1284

Experimental group

Description:

Radioligand: \[11C\]-raclopride

Treatment:

Drug: ITI-1284 20 mg

Cohort A3: 30 mg ITI-1284

Experimental group

Description:

Radioligand: \[11C\]-raclopride

Treatment:

Drug: ITI-1284 20 mg

Drug: ITI-1284 10 mg

Cohort B1: 20 mg ITI-1284

Experimental group

Description:

Radioligand: \[11C\]-MDL100907

Treatment:

Drug: ITI-1284 20 mg

Cohort B2: 20 mg ITI-1284

Experimental group

Description:

Radioligand: \[11C\]-DASB

Treatment:

Drug: ITI-1284 20 mg

Cohort C1: 20 mg ITI-1284

Experimental group

Description:

Radioligand: \[11C\]-raclopride or \[11C\]-MDL100907

Treatment:

Drug: ITI-1284 20 mg