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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.
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.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Cohort A1: 10 mg ITI-1284 | Experimental | Radioligand: [11C]-raclopride |
|
| Cohort A2: 20 mg ITI-1284 | Experimental | Radioligand: [11C]-raclopride |
|
| Cohort A3: 30 mg ITI-1284 | Experimental | Radioligand: [11C]-raclopride |
|
| Cohort B1: 20 mg ITI-1284 | Experimental | Radioligand: [11C]-MDL100907 |
|
| Cohort B2: 20 mg ITI-1284 | Experimental | Radioligand: [11C]-DASB |
|
| Cohort C1: 20 mg ITI-1284 | Experimental | Radioligand: [11C]-raclopride or [11C]-MDL100907 |
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| ITI-1284 10 mg | Drug | ITI-1284 tablet |
| |
| Measure | Description | Time Frame |
|---|---|---|
| % Receptor occupancy | Percent change of binding potential from baseline | Day 1 |
| Measure | Description | Time Frame |
|---|---|---|
| Pharmacokinetics: AUC0-t | Area under the plasma drug concentration-time curve (AUC) from time zero to the last measurable concentration | Day 1 |
| Pharmacokinetics: Cmax | Maximum plasma concentration |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Role | Phone | Extension | |
|---|---|---|---|---|
| ITI Clinical Trials | Contact | 646 440-9333 | ITCIClinicalTrials@itci-inc.com |
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| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Yale University School Of Medicine | Recruiting | New Haven | Connecticut | 06519 | United States |
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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.
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| ITI-1284 20 mg |
| Drug |
ITI-1284 tablet |
|
| Day 1 |
| Pharmacokinetics: Tmax | Time of maximum plasma concentration | Day 1 |
| 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 |