Delving into the Latest Updates on BAY-85-8102 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug, Diagnostic radiopharmaceuticals

Synonyms

Target

TSPO

Action

inhibitors, enhancers

Mechanism

TSPO inhibitors(Translocator protein inhibitors), PET imaging(Positron-emission tomography enhancers), Translocator protein (TSPO; PBR) ligands

Therapeutic Areas

Nervous System DiseasesEndocrinology and Metabolic DiseaseImmune System Diseases+ [5]

Active Indication

Parkinson DiseaseNeuroinflammationCarotid Stenosis+ [6]

Inactive Indication

Alzheimer DiseaseAmyotrophic Lateral SclerosisIdiopathic Pulmonary Fibrosis+ [1]

Originator Organization

Bayer AG

Active Organization

The University of Alabama at Birmingham

Bayer AG

Atos SE

Inactive Organization-

License Organization-

Drug Highest PhasePhase 2

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC22H27FN4O2

InChIKeyFLZZFWBNYJNHMY-VNRZBHCFSA-N

CAS Registry958233-09-5

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.

Start Date01 Apr 2026

Sponsor / Collaborator

The University of Alabama at Birmingham

NCT04542603

/ WithdrawnPhase 1IIT

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.

Start Date01 Jun 2025

Sponsor / Collaborator

The University of Alabama at Birmingham

NCT06453915

/ Not yet recruitingEarly Phase 1IIT

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

Start Date30 Apr 2025

Sponsor / Collaborator

University of California, Davis

100 Clinical Results associated with BAY-85-8102

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100 Translational Medicine associated with BAY-85-8102

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100 Patents (Medical) associated with BAY-85-8102

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161

Literatures (Medical) associated with BAY-85-8102

01 Feb 2025·Epilepsia

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

Article

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

AbstractObjectivesResective 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.MethodsPatients 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.ResultsWe 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.SignificanceThese 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.

01 Feb 2025·CNS Neuroscience & Therapeutics

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

Article

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

ABSTRACTPurposeSurgery 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.MethodsThe 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.ResultsA 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).Conclusion18F‐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.

01 Dec 2024·Journal of Neurology

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

Article

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

BACKGROUND AND OBJECTIVESConventional 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.METHODSIn 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.RESULTSThe 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.CONCLUSION¹⁸F-DPA714 PET demonstrated its potentially incremental value to conventional MRI for detecting possible antibody-negative AIE.

100 Deals associated with BAY-85-8102

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Neuroinflammation	Phase 2	United States	The University of Alabama at Birmingham	22 Mar 2018
Parkinson Disease	Phase 2	-	Bayer AG	-
Myocardial Infarction	Phase 1	United States	The University of Alabama at Birmingham	17 Oct 2019
Fatigue Syndrome, Chronic	Phase 1	United States	The University of Alabama at Birmingham	03 Feb 2019
Fibromyalgia	Phase 1	United States	The University of Alabama at Birmingham	03 Feb 2019
Multiple Sclerosis	Phase 1	United States	The University of Alabama at Birmingham	03 Feb 2019
Idiopathic Pulmonary Fibrosis	Discovery	United States	Atos SE	08 Dec 2020
Alzheimer Disease	Discovery	Netherlands	Bayer AG	01 Oct 2009
Alzheimer Disease	Discovery	Finland	Bayer AG	01 Oct 2009
Amyotrophic Lateral Sclerosis	Discovery	France	Atos SE	16 Jun 2008

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


SNMMI2023	Not Applicable	Encephalomyelitis	-	18F-DPA714 (Patients with autoimmune encephalomyelitis)	qdvkrulgby(royfqrpyjm) = drwyrvarjy eaoyjnwoyb (mhzdthtaog )	-	28 Aug 2023
				18F-DPA714 (Healthy controls)	qdvkrulgby(royfqrpyjm) = eapkrzqyxb eaoyjnwoyb (mhzdthtaog )
EANM2022	Not Applicable	Drug Resistant Epilepsy	23	[18F]DPA-714 PET imaging	kkaetctysi(tphlsmakho) = cbsgcwnbnk fkihsylynq (oeasaitgsz ) View more	Positive	22 Sep 2022
SNMMI2016	Not Applicable	-	-	18F-DPA-714 (High affinity binders (HAB))	zunwptdkdo(mufnivcbon) = itxyghbjkb qwiuoaqwgp (yryzaudgdt )	-	24 May 2016
				18F-DPA-714 (Mixed affinity binders (MAB))	zunwptdkdo(mufnivcbon) = mqhlgkgzln qwiuoaqwgp (yryzaudgdt )