Healthy Volunteers
Conditions
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 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.
Interventions
DRUGITI-1284 10 mg
ITI-1284 tablet
DRUGITI-1284 20 mg
ITI-1284 tablet
Sponsors
Intra-Cellular Therapies, Inc.
Study design
Allocation
NON_RANDOMIZED
Intervention model
PARALLEL
Primary purpose
TREATMENT
Masking
NONE
Intervention model description
This study includes up to 3 sequential parts (Parts A, B and C). In Part A, subjects will be assigned to 1 of 3 cohorts, will receive a single dose of ITI-1284, and undergo one postdose PET/CT scan starting at 1 hour postdose. In Part B, subjects will be assigned to 1 of 2 cohorts, will receive a single dose of ITI-1284, and undergo one postdose PET/CT scan starting at 1 hour postdose. In Part C, subjects will receive a single dose of ITI-1284 and undergo one postdose PET/CT scans starting at approximately 24 hours postdose.
Eligibility
Sex/Gender
ALL
Age
18 Years to 55 Years
Healthy volunteers
Yes
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.
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| % Receptor occupancy | Day 1 | Percent change of binding potential from baseline |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| 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 | — |
Countries
United States
Contacts
STUDY_DIRECTORIntra-Cellular Therapies, Inc. Clinical Trial
Intra-Cellular Therapies, Inc.
Outcome results
None listed