([18F]-PBR-06) - 药物靶点：TSPO_在研适应症：阿尔茨海默症_专利_临床

概要

基本信息

药物类型

小分子化药、诊断用放射药物

别名

+ [1]

靶点

TSPO

作用机制

TSPO抑制剂(TSPO蛋白抑制剂)、PET imaging(正电子发射断层成像术增强剂)

治疗领域

神经系统疾病

在研适应症

阿尔茨海默症

非在研适应症

肌萎缩侧索硬化炎症多发性硬化症+ [1]

原研机构

The Brigham & Women's Hospital, Inc.

在研机构

National Institute of Mental Health

The Brigham & Women's Hospital, Inc.

非在研机构

Molecular NeuroImaging LLC

Institute for Neurodegenerative Disorders

Novartis AG

最高研发阶段临床2期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构

分子式C23H22FNO4

InChIKeyNSOMTOOLHNHIJA-MIGPCILRSA-N

CAS号1003581-94-9

关联

11

项与 [18F]-PBR-06 相关的临床试验

NCT05486806 / RecruitingN/AIIT

Longitudinal Tracking of Patients Diagnosed With Neurodegenerative Movement Disorders

The purpose of this protocol is to create an active natural history cohort of patients with degenerative movement disorders, tracked in a clinical setting with clinical rating scales and neuroimaging. The overarching rationale is that neurodegenerative diseases may be heterogeneous, complex disorders. A new way of performing clinical trials in these patients may be in order and this protocol aims to build a longitudinally tracked clinical trial-ready cohort of patients. The purpose of this protocol is to establish an active natural history cohort of patients with neurodegenerative movement disorders who are deeply phenotyped and "clinical trial ready" across Mass General Brigham.
After a thorough clinical diagnostic evaluation (this may include clinically indicated testing, for example MRI, FDG-PET, MIBG scan, polysomnography, genetic testing, autonomic function tests, inflammatory tests, skin biopsy) the investigators aim to achieve this through:
1. Longitudinal tracking of clinical progression through use of clinical scales including at the present time: UMSARS, BARS, MoCA and UPSIT, PROM, MDS-NMS, UPDRS, and SARA
2. Longitudinal tracking of disease progression through use of neuroimaging including at the present time: TSPO-PET and 3D MRI (see section 1.3)
This is a pilot study designed to track patients with neurodegenerative movement disorders across Mass General Brigham through MRI and PET imaging modalities and clinical measures. Figure 5 represents the study design in detail. In short, subjects will be asked to visit Mass General Brigham every 6-9 months over the course of 18 months for imaging and clinical evaluation.

开始日期2023-03-01

申办/合作机构

The Brigham & Women's Hospital, Inc.

NCT05269446 / RecruitingN/AIIT

Total-body 18F-PBR06 PET/CT to Evaluate Systemic Inflammation and Perfusion in STEMI and SA Patients Receiving PCI

The study will use 18F-PBR06/uExplorer to study the activation of macrophages and systemic perfusion in patients with ST-segment elevation myocardial infarction (STEMI) or stable angina (SA). Participants will receive the total-body PET/CT scan on the seventh day (Day 7, D7) and D180 of enrolment.

开始日期2022-07-08

申办/合作机构

上海仁玑医院管理有限公司

NCT04616456 / Completed早期临床1期IIT

Effect of Verdiperstat on Microglial Activation in Well-characterized MSA Patients

This study will comprise of two phases, an observational phase and a treatment phase.
In the observational phase the specific aims are: 1. To determine the presence and regional distribution of microglial activation, as assessed by 18F-PBR06 PET, in subjects with MSA as compared to healthy controls, at baseline and at 6-9 months' follow-up.
2. To assess the relationship between microglial activation and clinical progression at baseline and follow-up.
In the treatment phase the specific aims of the study are:
The specific aims of the study are:
To assess whether verdiperstat (BHV-3241) reduces 18F-PBR06 PET signal, and thus microglial activation and inflammation, in well-characterized MSA patients.
To assess the relationship between PET changes and clinical progression at baseline and follow-up in patients treated with verdiperstat.
To assess the relationship between PET changes and volumetric brain MRI at baseline and follow-up in patients treated with verdiperstat.
Currently there is no known disease modifying therapy for MSA. Recently, the drug verdiperstat (BHV-3241) has appeared in the investigational arena specifically for the indication of Multiple System Atrophy. Verdiperstat (BHV-3241) is currently being used in a phase 3 active drug trial at Massachusetts Hospital. Verdiperstat (BHV-3241) is known to target Myeloperoxidase, an enzyme implicated in neuroinflammation, a major driver in disease pathogenesis. Our previous study (IRB protocol #2016P002373) demonstrated that applying TSPO (translator protein) PET imaging enabled us to track changes in neuroinflammation and thus provide a viable biomarker for disease progression.
In this pilot study, the investigators aim to assess the effect of an investigational drug, verdiperstat (BHV-3241) on microglial activation in MSA patients using [F-18]PBR06 and to link it with clinical and morphometric MRI brain changes following treatment.

开始日期2020-12-30

申办/合作机构

The Brigham & Women's Hospital, Inc.

[+1]

100 项与 [18F]-PBR-06 相关的临床结果

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100 项与 [18F]-PBR-06 相关的转化医学

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100 项与 [18F]-PBR-06 相关的专利（医药）

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2

项与 [18F]-PBR-06 相关的文献（医药）

PLOS ONE3区 · 综合性期刊

Preclinical TSPO Ligand PET to Visualize Human Glioma Xenotransplants: A Preliminary Study

3区 · 综合性期刊

ArticleOA

作者: Cooper, Michael K ; Manning, H Charles ; Chambless, Lola ; Watchmaker, Jennifer M ; Fu, Allie ; Harty, James P ; McKinley, Eliot T ; Abel, Ty W ; Buck, Jason R ; Thompson, Reid C

Current positron emission tomography (PET) imaging biomarkers for detection of infiltrating gliomas are limited. Translocator protein (TSPO) is a novel and promising biomarker for glioma PET imaging. To validate TSPO as a potential target for molecular imaging of glioma, TSPO expression was assayed in a tumor microarray containing 37 high-grade (III, IV) gliomas. TSPO staining was detected in all tumor specimens. Subsequently, PET imaging was performed with an aryloxyanilide-based TSPO ligand, [18F]PBR06, in primary orthotopic xenograft models of WHO grade III and IV gliomas. Selective uptake of [18F]PBR06 in engrafted tumor was measured. Furthermore, PET imaging with [18F]PBR06 demonstrated infiltrative glioma growth that was undetectable by traditional magnetic resonance imaging (MRI). Preliminary PET with [18F]PBR06 demonstrated a preferential tumor-to-normal background ratio in comparison to 2-deoxy-2-[18F]fluoro-D-glucose ([18F]FDG). These results suggest that TSPO PET imaging with such high-affinity radiotracers may represent a novel strategy to characterize distinct molecular features of glioma growth, as well as better define the extent of glioma infiltration for therapeutic purposes.

Molecules

Rapid Purification and Formulation of Radiopharmaceuticals via Thin-Layer Chromatography

Article

作者: Carlucci, Giuseppe ; Laferriere-Holloway, Travis S ; van Dam, R Michael ; Rios, Alejandra

Before formulating radiopharmaceuticals for injection, it is necessary to remove various impurities via purification. Conventional synthesis methods involve relatively large quantities of reagents, requiring high-resolution and high-capacity chromatographic methods (e.g., semi-preparative radio-HPLC) to ensure adequate purity of the radiopharmaceutical. Due to the use of organic solvents during purification, additional processing is needed to reformulate the radiopharmaceutical into an injectable buffer. Recent developments in microscale radiosynthesis have made it possible to synthesize radiopharmaceuticals with vastly reduced reagent masses, minimizing impurities. This enables purification with lower-capacity methods, such as analytical HPLC, with a reduction of purification time and volume (that shortens downstream re-formulation). Still, the need for a bulky and expensive HPLC system undermines many of the advantages of microfluidics. This study demonstrates the feasibility of using radio-TLC for the purification of radiopharmaceuticals. This technique combines high-performance (high-resolution, high-speed separation) with the advantages of a compact and low-cost setup. A further advantage is that no downstream re-formulation step is needed. Production and purification of clinical scale batches of [18F]PBR-06 and [18F]Fallypride are demonstrated with high yield, purity, and specific activity. Automating this radio-TLC method could provide an attractive solution for the purification step in microscale radiochemistry systems.

100 项与 [18F]-PBR-06 相关的药物交易

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研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
多发性硬化症	临床2期	美国	Novartis AG	2020-09-21
肌萎缩侧索硬化	临床2期	美国	Molecular NeuroImaging LLC	2016-06-28
阿尔茨海默症	临床2期	-	National Institute of Mental Health	-
阿尔茨海默症	临床2期	-	The Brigham & Women's Hospital, Inc.	-
多发性硬化症	临床1期	美国	Novartis AG	2020-09-21
炎症	临床1期	美国	Institute for Neurodegenerative Disorders	2009-11-01
帕金森病	临床1期	美国	Institute for Neurodegenerative Disorders	2009-11-01

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


ECTRIMS2020	N/A	多发性硬化症 [F-18]PBR06-Positron Emission Tomography (PET)	22	[f-18]pbr06	廠願鬱齋鹹構積襯顧鑰(鹹鬱網壓鬱艱窪範範醖) = 齋窪餘範獵願鏇繭簾繭壓膚膚願憲糧鹹願齋觸 (鹽願鬱鹹襯構鹽鹹襯衊 ) 更多	积极	2020-12-07
				[f-18]pbr06	廠願鬱齋鹹構積襯顧鑰(鹹鬱網壓鬱艱窪範範醖) = 窪鹹鹹繭憲襯獵餘構衊壓膚膚願憲糧鹹願齋觸 (鹽願鬱鹹襯構鹽鹹襯衊 ) 更多