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

An Open-label, Positron Emission Tomography (PET) Study to Evaluate Brain Receptor Occupancy, Safety, Tolerability, and Pharmacokinetics After Single Oral Doses of ITI-333 in Healthy Subjects

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT05470101

Enrollment

Registered

2022-07-22

Start date

2022-07-26

Completion date

2023-05-03

Last updated

2025-09-10

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Healthy Volunteers

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

Interventions

DRUGITI-333

ITI-333 oral solution

Study design

Allocation

RANDOMIZED

Intervention model

SEQUENTIAL

Primary purpose

BASIC_SCIENCE

Masking

NONE

Eligibility

Sex/Gender

ALL

Age

18 Years to 45 Years

Healthy volunteers

Yes

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).

Design outcomes

Primary

Measure	Time frame	Description
Pharmacodynamics: 5-HT2A receptor occupancy (RO) using [11C]-MDL100907	baseline 90-minute PET scan between Day -10 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
Pharmacokinetics: Cmax	predose and multiple timepoints up to 24 hours postdose	Maximum observed plasma concentration
Pharmacokinetics: Tmax	predose and multiple timepoints up to 24 hours postdose	Time to reach maximum observed plasma concentration

Secondary

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

Countries

United States

Outcome results

None listed

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026