A PET Study Following a Single Oral Dose of ITI-333 in Healthy Subjects

Phase 1

Completed

• Conditions: Healthy Volunteers
• Interventions: Drug: ITI-333

• Registration Number: NCT05470101
• Lead Sponsor: Intra-Cellular Therapies, Inc.

Brief Summary

This is an open-label, single-dose study of up to 4 dose levels of ITI-333 in healthy male and female subjects. Each cohort will enroll 6 subjects. Subjects will have a baseline PET/CT scan and a postdose PET/CT scan using \[14C\]-MDL100907 to characterize 5-HT2A receptor occupancy

Detailed Description

Not available

Study Timeline

• Study First Submitted: 2022-07-20
• Study First Submitted QC: 2022-07-20
• Study First Posted: 2022-07-22
• Study Start: 2022-07-26
• Primary Completion: 2023-05-03
• Study Completion: 2023-05-03
• Status Verified: 2025-02
• Last Update Submitted: 2025-02-18
• Last Update Posted: 2025-02-19

Recruitment & Eligibility

• Status: COMPLETED
• Sex: All
• Target Recruitment: 12

Inclusion Criteria

• Healthy male and female subjects between 18 and 45 years old (inclusive);
• BMI inclusive of 18.0-32.0 kg/m2 at screening and a minimum weight of 50 kg;
• Willing to be confined to the clinical research unit for the duration of the inpatient period of the study;

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 (including history of gastric bypass), pulmonary, endocrinologic, hematologic, or immunologic disease or history of malignancy;
• Clinically significant abnormal findings in vital sign assessments, including blood oxygen saturation (SpO2) < 96% and respiratory rate < 12 breaths per min;
• 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).

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: SEQUENTIAL

Arm && Interventions

Group	Intervention	Description
Cohort A1: ITI-333 2.25 mg	ITI-333	-
Cohort A2: ITI-333 dose to be determined based on Cohort A1	ITI-333	-
Cohort A3: ITI-333 dose to be determined based on Cohort A1 and A2	ITI-333	-
Cohort A4: ITI-333 dose to be determined based on Cohort A1, A2 and A3	ITI-333	-

Primary Outcome Measures

Name	Time	Method
Pharmacodynamics: Receptor occupancy (RO)	baseline 90-minute PET scan between Day -5 and Day -1, and a 90-minute PET scan starting at approximately 1 hour postdose
Pharmacokinetics: AUC0-t	predose and multiple timepoints up to 24 hours postdose	Area under the plasma concentration time curve from time zero to the last measurable of concentration of ITI-333 and its metabolites

Secondary Outcome Measures

Name	Time	Method
Change from baseline in systolic and diastolic blood pressure	Up to Day 7
Change from baseline in ECG QT interval	Up to Day 7
Percentage of subjects with treatment-emergent adverse events	up to 30 days after last dose
Change from baseline in aspartate aminotransferase	Up to Day 7
Change from baseline in alanine aminotransferase	Up to Day 7

Trial Locations

Locations (2)

Clinical Site 2; 🇺🇸 Creve Coeur, Missouri, United States

Clinical Site 1; 🇺🇸 Saint Louis, Missouri, United States