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Longitudinal PET Imaging of Antipsychotic Binding to the Dopamine-3 Receptor in Schizophrenia

2026年7月15日 更新者:Ragy Girgis、New York State Psychiatric Institute
This is a clinical trial in which 40 participants with schizophrenia will be randomized to 15 days of treatment with cariprazine (CAR) or brexpiprazole (BREX) in a single-blind manner. [11C]PHNO PET scans will be obtained before treatment and after 1 day and 15 days of treatment to examine the effects of antipsychotic medications on the dopamine-3 receptor (D3R). The overall objectives of the current study are to: 1) measure the acute binding of CAR/BREX to the D3R; 2) measure D3R availability for evidence of upregulation following subchronic administration of CAR/BREX in the same set of patients; 3) examine relationships between subchronic binding of CAR/BREX to, and upregulation of, the D3R vs. D2R and changes in positive symptoms, negative symptoms, and cognitive deficits. Relationships between subchronic binding of CAR/BREX and EPS will be explored.

研究概览

详细说明

There is a great need for the development of new treatments for schizophrenia (SCZ). Aside from the recently approved muscarinic agonist xanomeline, all current treatments have been assumed to function by blocking dopamine-2 receptors (D2Rs). Interest in the dopamine-3 receptor (D3R) was encouraged by preclinical findings that D3R antagonists reverse cognitive impairment and improve negative symptoms. In vivo imaging of the D3R became possible with the development of [11C]-(+)-PHNO, a D3R-preferring radioligand. However, while numerous preclinical studies have demonstrated that the D3R is relevant to both the neurobiology and treatment of SCZ, in vivo studies initially and surprisingly reported that, after several weeks of administration, antipsychotic medications may not bind to the D3R and may paradoxically increase levels of the D3R. These findings were discrepant with our own findings in non-human primates and individuals with SCZ demonstrating that acute doses of antipsychotic medications bind to the D3R and D2R in ratios predicted by their in vitro binding profiles. In a later study conducted by our group, 10 days of chronic dosing of the D2R-preferring antipsychotic medication brexpiprazole (BREX) also led to increased levels of the D3R at 1mg and negligible binding at 4mg. Finally, in our study of the D3R-preferring antipsychotic medication cariprazine (CAR), there was robust binding to the D3R and D2R after both acute and subchronic dosing. These seemingly discrepant findings may be related to methodological differences, differences in the binding profiles of D2R- vs. D3R-preferring antipsychotic medications, or to homeostatic responses to chronic antipsychotic treatment (i.e., upregulation). Upregulation is a potentially critical, though underexamined, effect common to all D2R/D3R-binding antipsychotic medications, including partial agonists. It has been hypothesized to be largely responsible for differences in occupancy estimates from single and repeat dose studies and contribute to waning effects of antipsychotic medications and tardive dyskinesia. The goals of this proposal are to elucidate the contribution of D3R, compared to D2R, binding to antipsychotic action, both acutely (SA1) and subchronically (SA2), in the same patients. The relationship between occupancy, upregulation, and clinical effects (SA3, EA) will be investigated.

研究类型

介入性

注册 (估计的)

100

阶段

  • 阶段1

联系人和位置

本节提供了进行研究的人员的详细联系信息,以及有关进行该研究的地点的信息。

学习联系方式

参与标准

研究人员寻找符合特定描述的人,称为资格标准。这些标准的一些例子是一个人的一般健康状况或先前的治疗。

资格标准

适合学习的年龄

  • 成人

接受健康志愿者

不

描述

Inclusion Criteria:

  1. Individuals, any gender or sex, aged 18 to 55, inclusive at screen
  2. Capable of understanding the study procedures and able to provide informed consent
  3. Diagnosed with schizophrenia, schizoaffective, or schizophreniform disorder
  4. Negative urine toxicology
  5. Antipsychotic free (by choice and for reasons unrelated to the study), and for at least 3 weeks (4 for aripiprazole or LAIs) at the time of the baseline PET scan, inclusive of any antipsychotic-free time prior to consent. [Any patient who requires inpatient hospitalization or acute medication treatment for clinical stabilization during the medication free period will not be included in this study; any participant who in the clinical judgment of the PIs or any involved clinician is not stable or appropriate for a medication free period will not be included.]
  6. PANSS total score > 80 and < 120 (inclusive)

Exclusion Criteria:

  1. Diagnosis of substance use disorder within the previous month
  2. A history of poor or inadequate response or hypersensitivity to CAR or BREX for any reason
  3. EKG abnormality that is clinically significant including a QTc interval > 450 msec for men and > 470 msec for women,
  4. Pregnant or breast-feeding women. Women of child-bearing potential must have a negative serum β-hCG pregnancy test at Visit 1, must have been using an acceptable method of contraception for 30 days before the study (i.e., before the first PET or MRI scan, whichever comes first), and must agree to do so for the whole study and 30 days after (unless post-menopausal or surgically sterile)
  5. Any clinically significant or unstable medical/neurological illness, condition, or disorder that is anticipated to potentially compromise participant safety on study medication
  6. Any material in the body that is a contraindication for MRI procedures or participated in prior nuclear medicine procedures in the past year that exceed FDA-defined limits when combined with radiation dosimetry from PET scanning in this protocol to avoid exceeding annual dosimetry limits (metal screener repeated before MRI scan). Individuals exposed to radiation in the workplace in the previous year will be excluded.
  7. Acute risk for suicide (i.e., score of 4-5 within the previous month or 6 within the previous 3 months on the CSSRS) or violence/homicide (e.g., homicidal ideation), or history of severe violent behavior or behavioral dyscontrol while antipsychotic-free
  8. A history of treatment resistance to antipsychotics or who have a duration of illness of greater than 20 years
  9. Claustrophobia
  10. Use of nicotine products within the previous month (prior to first PET scan)

学习计划

本节提供研究计划的详细信息,包括研究的设计方式和研究的衡量标准。

研究是如何设计的?

设计细节

  • 主要用途:其他
  • 分配:随机化
  • 介入模型:并行分配
  • 屏蔽:单身的

武器和干预

参与者组/臂
干预/治疗
实验性的:Cariprazine 1mg
Cariprazine 1mg daily for 15 days
Cariprazine is an antipsychotic medication
This is the radiotracer that will be used to examine antipsychotic binding to D2 and D3 receptors in this study. It is experimental and used for imaging purposes.
实验性的:Cariprazine 2mg
Cariprazine 2mg daily for 15 days
Cariprazine is an antipsychotic medication
This is the radiotracer that will be used to examine antipsychotic binding to D2 and D3 receptors in this study. It is experimental and used for imaging purposes.
实验性的:Cariprazine 3mg
Cariprazine 3mg daily for 15 days
Cariprazine is an antipsychotic medication
This is the radiotracer that will be used to examine antipsychotic binding to D2 and D3 receptors in this study. It is experimental and used for imaging purposes.
实验性的:Cariprazine 4mg
Cariprazine 4mg daily for 15 days
Cariprazine is an antipsychotic medication
This is the radiotracer that will be used to examine antipsychotic binding to D2 and D3 receptors in this study. It is experimental and used for imaging purposes.
实验性的:Brexpiprazole 1mg
Brexpiprazole 1mg daily for 15 days
This is the radiotracer that will be used to examine antipsychotic binding to D2 and D3 receptors in this study. It is experimental and used for imaging purposes.
Brexpiprazole is an antipsychotic medication
实验性的:Brexpiprazole 2mg
Brexpiprazole 2mg daily for 15 days
This is the radiotracer that will be used to examine antipsychotic binding to D2 and D3 receptors in this study. It is experimental and used for imaging purposes.
Brexpiprazole is an antipsychotic medication
实验性的:Brexpiprazole 3mg
Brexpiprazole 3mg daily for 15 days
This is the radiotracer that will be used to examine antipsychotic binding to D2 and D3 receptors in this study. It is experimental and used for imaging purposes.
Brexpiprazole is an antipsychotic medication
实验性的:Brexpiprazole 4mg
Brexpiprazole 4mg daily for 15 days
This is the radiotracer that will be used to examine antipsychotic binding to D2 and D3 receptors in this study. It is experimental and used for imaging purposes.
Brexpiprazole is an antipsychotic medication

研究衡量的是什么?

主要结果指标

结果测量
措施说明
大体时间
Acute D2 and D3 Receptor Occupancy
大体时间:Day 1
Delta BPND in poscommissural putamen and midbrain
Day 1
Upregulation of D3 receptor following subchronic administration of antipsychotics
大体时间:Day 15
The availability of D3Rs following two weeks of antipsychotic treatment will be measured.
Day 15

次要结果测量

结果测量
措施说明
大体时间
Positive and Negative Syndrome Scale (PANSS) Total Positive Symptoms
大体时间:15 days
Correlations between changes in PANSS total positive symptoms and receptor binding will be examined.
15 days
Positive and Negative Syndrome Scale (PANSS) Total Negative Symptoms
大体时间:15 days
Correlations between changes in PANSS total negative symptom scores and receptor binding will be examined.
15 days
MATRICS Cognitive Deficits (Composite Score)
大体时间:15 days
Correlations between changes in cognitive deficits (MATRICS composite score) and receptor binding will be examined.
15 days

其他结果措施

结果测量
措施说明
大体时间
Abnormal Involuntary Movement Scale (AIMS) Score
大体时间:15 days
Correlations between changes in extrapyramidal side effect scores (AIMS) and receptor binding will be examined.
15 days
Simpson-Angus Scale (SAS) Score
大体时间:15 days
Correlations between changes in extrapyramidal side effect scores (SAS) and receptor binding will be examined.
15 days
Barnes Akathisia Rating Scale (BARS) Score
大体时间:15 days
Correlations between changes in extrapyramidal side effect scores (BARS) and receptor binding will be examined.
15 days

合作者和调查者

在这里您可以找到参与这项研究的人员和组织。

研究记录日期

这些日期跟踪向 ClinicalTrials.gov 提交研究记录和摘要结果的进度。研究记录和报告的结果由国家医学图书馆 (NLM) 审查,以确保它们在发布到公共网站之前符合特定的质量控制标准。

研究主要日期

学习开始 (估计的)

2026年12月1日

初级完成 (估计的)

2030年8月30日

研究完成 (估计的)

2030年11月30日

研究注册日期

首次提交

2026年7月11日

首先提交符合 QC 标准的

2026年7月15日

首次发布 (实际的)

2026年7月20日

研究记录更新

最后更新发布 (实际的)

2026年7月20日

上次提交的符合 QC 标准的更新

2026年7月15日

最后验证

2026年7月1日

更多信息

与本研究相关的术语

关键字

其他研究编号

  • NYSPI2026-31
  • 1R01MH139651-01A1 (美国 NIH 拨款/合同)

计划个人参与者数据 (IPD)

计划共享个人参与者数据 (IPD)?

是的

IPD 计划说明

Data will be shared via the NIH data archive.

IPD 共享时间框架

Data will be shared after the study has been completed, as per NIH guidelines.

药物和器械信息、研究文件

研究美国 FDA 监管的药品

是的

研究美国 FDA 监管的设备产品

不

此信息直接从 clinicaltrials.gov 网站检索,没有任何更改。如果您有任何更改、删除或更新研究详细信息的请求,请联系 register@clinicaltrials.gov. clinicaltrials.gov 上实施更改,我们的网站上也会自动更新.

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