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更新于：2025-06-14
Florbetaben F-18
氟[¹⁸F]贝他苯
更新于：2025-06-14
概要
基本信息
非在研机构- |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评快速通道 (美国)、孤儿药 (美国)、孤儿药 (欧盟) |
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结构/序列
分子式C21H26FNO3 |
InChIKeyNCWZOASIUQVOFA-FWZJPQCDSA-N |
CAS号902143-01-5 |
关联
39
项与 氟[¹⁸F]贝他苯 相关的临床试验NCT05617014
Alzheimer's Disease Neuroimaging Initiative 4 (ADNI4)
NCT06141356
[18F]Florbetazine ([18F]92) for Beta Amyloid PET Imaging in Alzheimer's Disease
EUCTR2022-002585-33-IT
A multi-center phase 3 study of 18F-florbetaben positron emission tomography/computed tomography (PET-CT) - PETAL
100 项与 氟[¹⁸F]贝他苯 相关的临床结果
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100 项与 氟[¹⁸F]贝他苯 相关的转化医学
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100 项与 氟[¹⁸F]贝他苯 相关的专利（医药）
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221
项与 氟[¹⁸F]贝他苯 相关的文献（医药）2025-05-04Journal of Sulfur Chemistry
Small molecule heterocycles: design and synthesis of novel fluorescent Benzothiazoles for early detection of Alzheimer’s disease
作者: Sharma, Vijay ; Sundaram, G.S.M.
Diagnostic agents capable of imaging β-amyloid (Aβ) plaques at prodromal stages could provide noninvasive tools to assess plaque burden and assist in determining efficacy of disease-modifying therapeutic interventions in vivo.To accomplish this goal, FDA approved 18F-incorporated tracers, such as Florbetapir, Flutemetamol, and Florbetaben may allow quant. anal. of therapeutic efficacy of disease-modifying treatments that attenuate Aβ pathophysiol. in vivo.Although promising, these tracers show high off-target binding.Importantly, current anti-amyloid therapy also targets diffuse amyloid plaques (included in revised NIAAA criteria for detecting AD) and other forms of amyloid plaques.Therefore, mols. capable of detecting both diffuse and fibrillar plaque pathol. can potentially offer better quant. tools for interrogating efficacy of anti-amyloid therapy.To achieve this goal, herein, we report synthesis and characterization of new small organic mols.: ((Z,E)-4-(2-(6-(2-Fluoroethoxy)benzo[d]thiazol-2-yl)vinyl)-N,N-dimethylaniline), ((Z)-4-(2-(6-(2-(2-(3-Fluoropropoxy)ethoxy)ethoxy)benzo[d]thiazol-2-yl)vinyl)-N,N-dimethylaniline) and ((E)-4-(2-(6-(2-(2-(3-Fluoropropoxy)ethoxy)ethoxy)benzo[d]thiazol-2-yl)vinyl)-N,N-dimethylaniline) We also report preliminary investigations on binding affinity in vitro.While demonstrated a relatively higher affinity, both and showed moderate affinity for Aβ1-42 aggregates in vitro.Furthermore, all 3 agents showed ability to detect Aβ fibrillar and diffuse plaque pathol. in brain sections of APP/PS1 transgenic mice and post-mortem confirmed AD human brain tissue sections.
2025-04-01JOURNAL OF ALZHEIMERS DISEASE
Synergistic associations of amyloid-β and phosphorylated tau with tau aggregation and cognitive decline in Alzheimer's disease
Article
作者: Ba, Maowen ; Kong, Min ; Ma, Guozhao ; Jia, Pengyuan ; Zhang, Chunhua ; Tai, Yaojun
Background:
The pathological hallmarks of Alzheimer's disease (AD) include the amyloid-β (Aβ) plaques and phosphorylated tau (p-tau) forming neurofibrillary tangles. Understanding the pathophysiological cascade related to Aβ and tau process is crucial.
Objective:
To investigate the impact of Aβ positron emission tomography (PET) and cerebrospinal fluid (CSF) p-tau on tau pathology and cognitive decline in AD.
Methods:
We analyzed 319 older individuals from the Alzheimer's Disease Neuroimaging Initiative (ADNI) who underwent Aβ (
18
F-florbetapir or
18
F-florbetaben) and tau (
18
F-flortaucipir) PET scans, along with CSF and cognitive assessments. Aβ positivity (A+) was determined by global standardized uptake value ratio thresholds of ≥1.11 for
18
F-florbetapir or ≥1.08 for
18
F-florbetaben, while p-tau positivity (T+) was defined as CSF p-tau181 levels ≥23 pg/ml. Linear mixed regression models were used to assess the effects of PET Aβ and CSF p-tau181 levels on tau accumulation in predefined Braak regions and cognitive function over time.
Results:
Our results revealed significant differences in PET tau pathology and cognitive decline between A + and A− individuals. We observed that interactions between Aβ and p-tau proteins were associated with tau accumulation and cognitive decline. Additionally, A−/T + individuals exhibited higher levels of tau accumulation in all Braak regions compared to A−/T− counterparts, suggesting a potential independent role of p-tau in tau pathology in the absence of Aβ.
Conclusions:
Our findings suggest that Aβ positivity and elevated CSF p-tau181 levels were associated with tau accumulation and cognitive decline, highlighting the relevance of soluble p-tau as a potential biomarker for further investigation.
2025-03-01EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Progress in the study of anti-Alzheimer's disease activity of pyrimidine-containing bioactive molecules
Review
作者: Zhang, Di ; Zhang, Qi ; Zhang, Lin-Lin ; Liu, Yu-Lin ; Chui, Rui-Hao ; Zhang, Qian ; Li, Bing-Qian ; Ma, Li-Ying
Pyrimidines are aromatic, heterocyclic organic compounds characterized by a six-membered ring that contains four carbon atoms and two nitrogen atoms. They have been reported to exhibit a variety of biological activities such as antifungal, antiviral, and anti-Parkinsonian effects. Recently, there has been an increased focus on their potential anti-Alzheimer's properties. Several pyrimidine-based drugs and their analogs are currently undergoing various phases of clinical trials, indicating pyrimidine as a promising chemical structure for drug development. Notably, modifications to the pyrimidine structure significantly influence their activity against Alzheimer's disease. For instance, the introduction of heteroatoms into the pyrimidine ring or alternations in the length of the linkage region have been shown to enhance therapeutic efficacy. This review provides a comprehensive overview of pyrimidine derivatives as potential therapeutics for Alzheimer's disease, with a focus on structure-activity relationship (SAR) studies, design strategies, and binding mechanisms. These insights could pave the way for the development of more effective anti-Alzheimer's medications.
100 项与 氟[¹⁸F]贝他苯 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 阿尔茨海默症 | 美国 | 2014-03-19 | |
| 认知功能障碍 | 欧盟 | 2014-02-20 | |
| 认知功能障碍 | 冰岛 | 2014-02-20 | |
| 认知功能障碍 | 列支敦士登 | 2014-02-20 | |
| 认知功能障碍 | 挪威 | 2014-02-20 | |
| 诊断试剂 | 欧盟 | 2014-02-20 | |
| 诊断试剂 | 冰岛 | 2014-02-20 | |
| 诊断试剂 | 列支敦士登 | 2014-02-20 | |
| 诊断试剂 | 挪威 | 2014-02-20 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 免疫球蛋白轻链淀粉样变性 | 临床3期 | 美国 | 2023-01-13 | |
| 免疫球蛋白轻链淀粉样变性 | 临床3期 | 德国 | 2023-01-13 | |
| 免疫球蛋白轻链淀粉样变性 | 临床3期 | 西班牙 | 2023-01-13 | |
| 免疫球蛋白轻链淀粉样变性 | 临床3期 | 英国 | 2023-01-13 | |
| 老年性心脏淀粉样变性 | 临床3期 | 美国 | 2023-01-13 | |
| 老年性心脏淀粉样变性 | 临床3期 | 德国 | 2023-01-13 | |
| 老年性心脏淀粉样变性 | 临床3期 | 西班牙 | 2023-01-13 | |
| 老年性心脏淀粉样变性 | 临床3期 | 英国 | 2023-01-13 | |
| 转甲状腺素蛋白淀粉样变性心肌病 | 临床3期 | 美国 | 2023-01-13 | |
| 转甲状腺素蛋白淀粉样变性心肌病 | 临床3期 | 德国 | 2023-01-13 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床2期 | 60 | 11C-PBR28+18F-Florbetaben (Amyloid-positive With Cognitive Impairment (AD)) | 網糧網艱艱鬱獵憲鬱壓(範顧壓遞觸憲築壓選獵) = 獵襯淵衊淵糧襯鏇願繭 鏇淵鏇構鑰淵衊願鑰鹽 (範繭鏇築窪糧範鏇蓋鹹, 0.18) 更多 | - | 2025-03-05 | ||
11C-PBR28+18F-Florbetaben (Amyloid-positive Without Impairment (Preclinical AD)) | 網糧網艱艱鬱獵憲鬱壓(範顧壓遞觸憲築壓選獵) = 廠糧製範願餘齋襯蓋醖 鏇淵鏇構鑰淵衊願鑰鹽 (範繭鏇築窪糧範鏇蓋鹹, 0.16) 更多 | ||||||
N/A | 161 | 範淵繭廠範鹽獵艱鑰糧 = 築膚齋顧淵憲膚壓構構 積憲選膚顧顧襯構糧齋 (糧夢齋醖廠鹽鏇窪網鹹, 艱製廠膚憲獵艱構鹹繭 ~ 襯觸膚鬱鏇蓋齋糧淵構) 更多 | - | 2024-05-06 | |||
临床1/2期 | 9 | (Cognitive Impairment) | 鹹構糧網襯構顧膚鹹壓(顧顧鬱廠壓獵構蓋鏇壓) = 餘願齋製醖築艱製蓋淵 鹽願艱遞齋選鹹築觸膚 (獵艱構淵遞襯壓憲鏇顧, 鑰範夢醖簾齋網積積範 ~ 衊獵鏇網餘醖繭鏇鹽積) 更多 | - | 2023-09-13 | ||
(No Cognitive Impairment) | 鹹構糧網襯構顧膚鹹壓(顧顧鬱廠壓獵構蓋鏇壓) = 構糧衊積獵餘齋觸淵鹹 鹽願艱遞齋選鹹築觸膚 (獵艱構淵遞襯壓憲鏇顧, 觸蓋構簾網艱糧鏇衊鏇 ~ 窪艱糧憲鏇衊糧夢選窪) 更多 | ||||||
N/A | - | 18F-Florbetaben (18F-FBB) | 顧壓蓋壓鑰鹽衊衊鹽襯(廠鑰窪糧艱鑰鬱艱淵構) = 餘壓遞製製簾製構簾蓋 顧蓋鬱襯選鹹襯窪齋構 (鹹鹽積鬱膚簾壓衊醖蓋, > ~ 1.585) 更多 | - | 2023-08-28 | ||
N/A | 记忆障碍 amyloid burden | 729 | 夢簾顧獵構襯窪衊獵齋(製壓壓構構製壓製網鹽) = 鬱衊壓齋淵窪製夢襯壓 鏇遞衊繭鬱鏇糧選衊蓋 (醖艱糧範蓋鏇壓醖鏇齋, 17.87) 更多 | - | 2022-09-22 | ||
18f-flutemetamol (FTM) | 夢簾顧獵構襯窪衊獵齋(製壓壓構構製壓製網鹽) = 繭淵網齋衊壓膚鹹壓觸 鏇遞衊繭鬱鏇糧選衊蓋 (醖艱糧範蓋鏇壓醖鏇齋, 17.87) 更多 | ||||||
N/A | - | (Absence of periodontal disease or mild periodontitis) | 鹹窪觸願簾淵餘艱鹹願(選糧遞積積齋廠願鹽範) = 襯獵鹹築鹽衊夢積窪淵 鹽築餘觸選構繭醖夢簾 (簾願淵齋衊選網觸淵鹹 ) | - | 2021-09-24 | ||
N/A | 阿尔茨海默症 amyloid | 264 | F18-Florbetaben (Early phase FBB (eFBB)) | 網鹽觸廠衊膚願築觸遞(膚顧製齋簾鹽艱遞鬱鬱) = 糧繭簾夢壓觸網醖膚蓋 獵積觸餘鹽蓋鹹繭鏇憲 (窪窪壓網鬱製襯築構範 ) | 积极 | 2021-05-18 | |
F18-Florbetaben (Delay-phase FBB (dFBB)) | 網鹽觸廠衊膚願築觸遞(膚顧製齋簾鹽艱遞鬱鬱) = 襯觸積淵蓋積簾築窪壓 獵積觸餘鹽蓋鹹繭鏇憲 (窪窪壓網鬱製襯築構範 ) | ||||||
N/A | - | (Young Healthy Controls (YHC)) | 膚簾鏇壓糧顧獵膚範構(鹽構積憲繭積齋艱鏇網) = 糧鏇築鏇廠淵鑰觸襯鏇 醖艱獵鏇觸襯夢廠遞鹹 (壓鹽願襯糧夢憲積鏇糧, 0.03) | - | 2020-05-15 | ||
(Subjective Cognitive Decline (SCD)) | 獵糧網網積遞遞鹹鬱獵(鏇餘顧鑰鹹鹽艱鬱鹽獵) = 餘醖襯餘繭蓋糧鬱顧願 襯餘積鑰鬱願餘壓夢簾 (鬱淵夢簾積鏇鏇蓋糧窪, 2.1) 更多 | ||||||
N/A | 过氧物酶体病 gene defect | very long chain fatty acids (VLVFA) | 4 | (X-linked adulthood cerebral adrenoleukodystrophy (X-ACALD) patients) | 簾繭鏇繭醖構築網餘醖(鹹鹹遞窪襯襯淵夢憲鑰) = 9.8 ± 2.6 膚窪齋鏇鬱膚齋襯範襯 (鑰餘遞鹽繭鬱構廠艱憲 ) 更多 | - | 2019-09-18 | |
(Healthy control group) | |||||||
N/A | - | 6 | (Standard PET images) | 獵遞夢顧遞憲餘範壓選(鑰廠鏇艱鏇壓鹽衊網積) = 膚憲網膚淵廠鬱淵鹽醖 窪醖壓憲築壓鏇糧遞鹽 (鹹觸憲繭廠構襯壓遞簾 ) 更多 | - | 2019-09-18 | |
(PET images with superimposed WM/GM boundaries) | 鹽鹹範淵觸鑰蓋網餘願(觸願願顧壓簾網顧鑰齋) = 網夢醖衊齋構願遞齋製 築範壓遞構鏇蓋選蓋壓 (鬱夢淵衊夢選鹹構窪憲 ) 更多 |
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