BAY-85-8102(BAY-85-8102) - 药物靶点：TSPO_在研适应症：帕金森病，神经炎症，颈动脉狭窄_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

[18F]DPA-714

靶点

TSPO

作用方式

抑制剂、增强剂

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)、Translocator protein (TSPO; PBR) ligands

治疗领域

神经系统疾病内分泌与代谢疾病免疫系统疾病+ [5]

在研适应症

帕金森病神经炎症颈动脉狭窄+ [6]

非在研适应症

阿尔茨海默症肌萎缩侧索硬化特发性肺纤维化+ [1]

原研机构

Bayer AG

在研机构

The University of Alabama at Birmingham

Bayer AG

Atos SE

非在研机构-

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-

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结构/序列

分子式C22H27FN4O2

InChIKeyFLZZFWBNYJNHMY-VNRZBHCFSA-N

CAS号958233-09-5

关联

28

项与 BAY-85-8102 相关的临床试验

NCT05238961

/ Recruiting临床1期IIT

Neuroinflammation in Asymptomatic Carotid Artery Disease - Imaging Substudy

This clinical imaging substudy will use the small molecule translocator protein (TSPO) ligand, Fludeoxyglucose(18F)-labeled DPA-714, to compare neuroinflammation in individuals with high or low grade asymptomatic carotid artery stenosis (aCAD) who are participating in the separate Neuroinflammation in Asymptomatic Carotid Artery Disease study lead by Dr. Ron Lazar (IRB-300007806). The positron emission tomography (PET) tracer [18F]DPA-714 binds to the 18 kDa translocator protein (TSPO, also known as the peripheral benzodiazepine receptor) in the mitochondria of activated microglia/macrophages and provides a non-invasive measure of neuroinflammation.

开始日期2026-04-01

申办/合作机构

The University of Alabama at Birmingham

NCT04542603

/ Withdrawn临床1期IIT

Neuroinflammation and Age-associated Brain Pathology: Two Potential Mechanisms of Cognitive Impairment in Ovarian Cancer

This clinical study will use the small molecule translocator protein (TSPO) ligand, 18F-labeled DPA- 714, to visualize and quantify neuroinflammation in treatment naivete women with stage 1-4 newly diagnosed ovarian cancer (without brain metastases) prior to starting neoadjuvant chemotherapy treatment (baseline) and within a month of completing first 6 cycles of cytotoxic chemotherapy treatment (follow-up). In addition, we will use the well-characterized small molecule PET(Positron Emission Tomography) tracer, 11C-labeled Pittsburgh compound B (PiB) to visualize and quantify the regional brain distribution of pathological amyloid deposition at baseline only. The brain amyloid PET and MRI data acquired through this study will be correlated with cognitive test data, clinical data, genetic testing, and biospecimens collected in this study.

开始日期2025-06-01

申办/合作机构

The University of Alabama at Birmingham

NCT06453915

/ Not yet recruiting早期临床1期IIT

NeuroFLiPP - Parametric PET of Neuroinflammation in Fatty Liver Disease

Alzheimer's Disease and related dementias (ADRD) affect about 6 million people in the U.S. and are the fifth leading cause of death for adults over 65. Recent research is investigating how chronic liver diseases like Metabolic Dysfunction-Associated Steatotic Liver Disease (MASLD), which affects one-third of the U.S. population, might influence ADRD through the liver-brain axis. MASLD shares risk factors with Alzheimer's, such as diabetes and hypertension, and studies have linked MASLD to increased risks of cognitive decline and ADRD. Mouse-model studies suggest that chronic liver inflammation in MASLD can induce neuroinflammation and accelerate Alzheimer's pathology, highlighting the importance of studying the liver-brain connection to identify new therapeutic targets for ADRD.
The goal of this research is to develop a practical PET imaging method using 18F-FDG to simultaneously assess liver and brain inflammation in patients with MASLD-related ADRD. This approach leverages dynamic FDG-PET scanning and advanced tracer kinetic modeling to quantify glucose transport, overcoming limitations of traditional imaging methods that cannot noninvasively assess chronic liver inflammation. The new method aims to enable comprehensive imaging of liver-brain inflammation crosstalk, validated against the 18F-DPA-714 radiotracer. Success in this project could provide a valuable imaging tool for linking liver inflammation with neuroinflammation and cognitive decline, advancing clinical research and potentially uncovering new pathways for ADRD treatment

开始日期2025-04-30

申办/合作机构

University of California, Davis

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100 项与 BAY-85-8102 相关的转化医学

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100 项与 BAY-85-8102 相关的专利（医药）

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161

项与 BAY-85-8102 相关的文献（医药）

2025-02-01·EPILEPSIA

TSPO‐PET in pre‐surgical evaluations: Correlation of neuroinflammation and SEEG epileptogenicity mapping in drug‐resistant focal epilepsy

Article

作者: Aghakhani, Nozar ; Rodrigo, Sebatian ; Herbrecht, Anne ; Bouilleret, Viviane ; Bottlaender, Michel ; Petrescu, Ana‐maria ; Kilmer, Jennifer ; Tournier, Nicolas ; Taussig, Delphine ; Leroy, Claire

Abstract:

Objectives:

Resective surgery in drug‐resistant focal epilepsy (DRFE) requires extensive evaluation to localize the epileptogenic zone (EZ). When non‐invasive phase 1 assessments (electroencephalography, EEG; magnetic resonance imaging, MRI; and 18F‐Fluorodeoxyglucose–positron emission tomography, [18F]FDG‐PET) are inconclusive for EZ localization, invasive investigations such as stereo‐EEG (SEEG) are necessary. Epileptogenicity maps (Ems) visualize the EZ using SEEG‐identified ictal high‐frequency oscillations (iHFOs). PET imaging with radioligands targeting the18‐kDa translocator protein (TSPO), a marker of glial activation, may aid EZ localization. This study investigates the correlation between TSPO‐PET imaging and SEEG iHFOs in DRFE to determine the utility of TSPO‐PET in pre‐surgical assessments, especially in complex or non‐lesional cases.

Methods:

Patients with DRFE and inconclusive phase 1 assessments were recruited from Bicêtre Hospital (AP‐HP) for a prospective study (Eudract 2017–003381‐27). They underwent SEEG and [18F]DPA‐714 (N,N‐diethyl‐2‐(2‐(4‐(2‐(fluoro‐18F)ethoxy)phenyl)‐5,7‐dimethylpyrazolo[1,5‐a]pyrimidin‐3‐yl)acetamide) (TSPO radioligand) PET imaging. Statistical parametric mapping (SPM) techniques analyzed significant [18F]DPA‐714‐PET uptake (TSPO‐map) and generated epileptogenicity maps (EM‐map). Correlation analyses at regional and voxel‐of‐interest (VOI) levels assessed the relationship between TSPO‐map and EM‐map.

Results:

We were able to obtain and analyze both maps in 12 of 17 patients recruited. A significant positive correlation between EM‐map and TSPO‐map in focal epilepsies was found regionally (r = .81, p < .00004) and at the VOI level (r = .79, p < .00003). Temporal, insular, parietal, and occipital regions showed particularly strong correspondence. In frontal epilepsies, TSPO‐map was more focal than EM‐map, suggesting increased specificity for SEEG planning. This study also demonstrated the benefit of the TSPO‐map in identifying multiple foci in multifocal epilepsies, with or without lesions.

Significance:

These findings suggest that neuroinflammation may be a molecular substrate of the EZ in non‐lesional focal epilepsy. Identifying the EZ inpatients with complex DRFE and inconclusive MRI/[18F]FDG‐PET imaging is essential to improve resective surgery outcomes. Combining TSPO‐PET imaging with SEEG recordings may help bridge this gap.

2025-02-01·CNS Neuroscience & Therapeutics

Hybrid PET/MRI Imaging of 18F‐Fluorodeoxyglucose and 18‐kDa Translocator Protein for Presurgical Localization in Refractory Epilepsy

Article

作者: Wang, Jingjuan ; Lu, Jie ; Yao, Chenyang ; Zhang, Siqi ; Cui, Bixiao ; Hu, Jie ; Wang, Zhenming ; Qi, Zhigang

ABSTRACT:

Purpose:

Surgery remains the only curative option for a third of refractory epilepsy patients, though success depends on precise localization of the epileptogenic zone (EZ). This study aims to assess the clinical value of hybrid 18F‐FDG and 18F‐DPA‐714 PET/MRI for accurate localization and precise boundary delineation.

Methods:

The refractory epilepsy patients who underwent surgery at Xuanwu Hospital from November 2022 to November 2023 were retrospectively recruited. Preoperative simultaneous 18F‐FDG and 18F‐DPA‐714 PET/MRI imaging were analyzed using the asymmetry index (AI) and a 4‐point visual score, with the surgical site and pathological findings serving as the gold standard.

Results:

A total of 43 patients (mean age: 26.30 ± 8.37 years, male: 28) were included in this study. Lesion localization accuracy within the EZ was 76.7% for 18F‐FDG PET/MRI, 69.8% for 18F‐DPA‐714 PET/MRI, and 60.5% for conventional MRI (p = 0.26). In 26 MRI‐positive cases, conventional MRI accurately localized all lesions within the EZ, with three cases showing negative findings on 18F‐FDG images and six on 18F‐DPA‐714. Among 17 MRI‐negative patients, thirteen demonstrated positive results on hybrid PET/MRI. Additionally, 18F‐DPA‐714 PET/MRI proved more effective in delineating lesion boundaries. Compared to 18F‐FDG, the AI score was significantly lower (0.25 ± 0.18 vs. 0.46 ± 0.19, p < 0.001), while the visual score was higher (4.00 ± 2.00 vs. 3.00 ± 0.00, p = 0.01).

Conclusion:

18F‐DPA‐714 PET/MRI can effectively complement conventional MRI in the preoperative assessment of refractory epilepsy, with localization accuracy on par with 18F‐FDG and enhanced capability in delineating lesion boundaries.

2024-12-01·JOURNAL OF NEUROLOGY

18F-DPA714 PET/MRI as a potential imaging tool for detecting possible antibody-negative autoimmune encephalitis: a prospective study

Article

作者: Chen, Sheng ; Zhou, Qinming ; Zhang, Yu ; Hai, Wangxi ; Zhang, Min ; Chunyu, Hangxing ; Meng, Huanyu ; Qu, Qian ; He, Lu ; Li, Biao ; Wang, Jin

BACKGROUND AND OBJECTIVES:

Conventional magnetic resonance imaging (MRI) used for detecting possible antibody-negative autoimmune encephalitis (AIE) often fails to meet the diagnostic requirements of this disease. Positron emission tomography (PET) with a translocator protein radioligand can help visualize microglia distribution density in inflammation-related diseases, thereby offering potentially incremental value to conventional MRI for the in vivo assessment of possible antibody-negative AIE.

METHODS:

In this prospective study, 15 participants diagnosed with possible antibody-negative AIE and 10 healthy controls were enrolled (ClinicalTrials.gov: NCT05293405, dated March 15, 2022). All participants underwent hybrid ¹⁸F-DPA714 PET/MRI and evaluation for modified Rankin scale (mRS) score, clinical assessment scale for AIE (CASE), and appropriate antibodies. A positive finding was defined as the intensity of ¹⁸F-DPA714 uptake that was above a threshold of mean standardized uptake value ratio (SUVR) + two standard deviations of SUVR within the corresponding brain regions of healthy controls.

RESULTS:

The positive detection rate of ¹⁸F-DPA714 PET for possible antibody-negative AIE was significantly higher than that of brain MRI (10/15 [67%] vs. 3/15 [20%]; P = 0.039). In addition, both the intensity and extent of ¹⁸F-DPA714 uptake were significantly associated with the CASE score (P = 0.002 and 0.001). Meanwhile, SUVR levels in the cerebellar region were significantly higher in patients with ataxia than in those without ataxia (P = 0.006). Furthermore, ¹⁸F-DPA714 uptake decreased in 5/10 [50%] patients who underwent follow-up PET/MRI, which mirrored their symptom relief.

CONCLUSION:

¹⁸F-DPA714 PET demonstrated its potentially incremental value to conventional MRI for detecting possible antibody-negative AIE.

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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
神经炎症	临床2期	美国	The University of Alabama at Birmingham	2018-03-22
帕金森病	临床2期	美国	The University of Alabama at Birmingham	2018-03-22
颈动脉狭窄	临床1期	美国	The University of Alabama at Birmingham	2026-04-01
卵巢癌	临床1期	-	The University of Alabama at Birmingham	2025-06-01
新冠肺炎后遗症	临床1期	美国	The University of Alabama at Birmingham	2023-11-10
严重急性呼吸综合征	临床1期	美国	The University of Alabama at Birmingham	2023-11-10
特发性肺纤维化	临床1期	美国	Atos SE	2020-12-08
心肌梗塞	临床1期	美国	The University of Alabama at Birmingham	2019-10-17
慢性疲劳综合征	临床1期	美国	The University of Alabama at Birmingham	2019-02-03
纤维肌痛	临床1期	美国	The University of Alabama at Birmingham	2019-02-03

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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


SNMMI2023	N/A	脑脊髓炎	-	18F-DPA714 (Patients with autoimmune encephalomyelitis)	遞壓構衊夢壓築壓餘淵(鹽範廠鑰蓋構範餘築積) = 餘築糧網選鏇淵鏇鹽網艱選蓋選憲淵築齋餘構 (膚鏇壓鹹淵糧鏇糧壓獵 )	-	2023-08-28
				18F-DPA714 (Healthy controls)	遞壓構衊夢壓築壓餘淵(鹽範廠鑰蓋構範餘築積) = 夢淵積廠遞簾範鏇鹹鹽艱選蓋選憲淵築齋餘構 (膚鏇壓鹹淵糧鏇糧壓獵 )
EANM2022	N/A	耐药性癫痫	23	[18F]DPA-714 PET imaging	獵壓膚築膚膚壓醖鏇艱(顧繭鹹選網鏇選觸齋顧) = 鬱鬱構壓願範鏇鹽願憲繭廠構憲窪遞鹹願觸獵 (選壓繭鏇鬱繭觸繭膚淵 ) 更多	积极	2022-09-22
SNMMI2016	N/A	-	-	18F-DPA-714 (High affinity binders (HAB))	齋糧簾鏇衊鬱廠網選網(願顧鏇齋網醖蓋艱鬱選) = 壓鏇鬱鑰繭廠衊膚夢艱顧艱顧窪選糧襯網鏇獵 (齋選鏇衊襯鏇選築衊鏇 )	-	2016-05-24
				18F-DPA-714 (Mixed affinity binders (MAB))	齋糧簾鏇衊鬱廠網選網(願顧鏇齋網醖蓋艱鬱選) = 遞製鹹襯築糧製遞積鬱顧艱顧窪選糧襯網鏇獵 (齋選鏇衊襯鏇選築衊鏇 )