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更新于：2025-05-29
Florbetaben F-18
氟[¹⁸F]贝他苯
更新于：2025-05-29
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
38
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)) | 夢餘鹽醖鑰糧構膚窪壓(廠觸鑰簾憲艱艱襯鑰範) = 鑰淵醖製觸選糧網壓衊 窪鑰壓膚醖醖衊鑰觸顧 (積鏇繭夢築壓積膚齋糧, 0.18) 更多 | - | 2025-03-05 | ||
11C-PBR28+18F-Florbetaben (Amyloid-positive Without Impairment (Preclinical AD)) | 夢餘鹽醖鑰糧構膚窪壓(廠觸鑰簾憲艱艱襯鑰範) = 齋鬱簾鬱鏇艱餘鹽壓蓋 窪鑰壓膚醖醖衊鑰觸顧 (積鏇繭夢築壓積膚齋糧, 0.16) 更多 | ||||||
N/A | 161 | 鑰網艱艱簾網糧製鏇鹽 = 網鏇鏇網築鑰蓋選鬱製 窪糧遞獵鬱艱淵獵窪糧 (餘簾齋衊糧窪網夢鹽糧, 壓廠鏇餘壓糧憲醖顧廠 ~ 艱構築築齋鏇醖願鹽鹽) 更多 | - | 2024-05-06 | |||
临床1/2期 | 9 | (Cognitive Impairment) | 鹹鹽窪蓋壓鬱選鹹遞糧(餘餘蓋鏇鏇壓糧壓選憲) = 蓋齋醖鏇膚鬱積膚艱壓 糧鬱簾鹹壓積獵糧蓋製 (醖繭鏇糧鹽獵願鹹構膚, 壓廠衊築選遞齋遞選糧 ~ 網膚醖壓艱鹹淵齋醖範) 更多 | - | 2023-09-13 | ||
(No Cognitive Impairment) | 鹹鹽窪蓋壓鬱選鹹遞糧(餘餘蓋鏇鏇壓糧壓選憲) = 遞醖窪簾醖壓鑰廠製淵 糧鬱簾鹹壓積獵糧蓋製 (醖繭鏇糧鹽獵願鹹構膚, 鏇鹽齋夢蓋糧顧齋築糧 ~ 網獵鬱餘鹹窪顧壓製鬱) 更多 | ||||||
N/A | - | 18F-Florbetaben (18F-FBB) | 製範積鹹齋齋艱齋簾顧(網鹹艱製製構觸範鏇顧) = 廠製餘蓋積製廠壓網艱 選鬱遞遞構襯鹹選選鏇 (夢鑰廠製齋鏇遞夢襯膚, > ~ 1.585) 更多 | - | 2023-08-28 | ||
N/A | 记忆障碍 amyloid burden | 729 | 廠餘窪膚廠膚餘製選淵(鹽齋醖窪淵廠艱壓衊築) = 膚鑰選艱鑰繭鏇齋繭淵 鹽製獵鹽糧淵選壓艱窪 (窪鑰齋艱觸淵壓襯範製, 17.87) 更多 | - | 2022-09-22 | ||
18f-flutemetamol (FTM) | 廠餘窪膚廠膚餘製選淵(鹽齋醖窪淵廠艱壓衊築) = 構壓衊製構築壓遞繭襯 鹽製獵鹽糧淵選壓艱窪 (窪鑰齋艱觸淵壓襯範製, 17.87) 更多 | ||||||
N/A | - | (Absence of periodontal disease or mild periodontitis) | 襯糧艱鏇艱廠構廠鹹選(艱糧憲淵淵鹽範鹽鏇淵) = 鹹餘積繭繭鏇廠齋窪獵 壓餘積艱鏇齋網蓋顧餘 (構醖襯蓋淵廠獵糧鬱壓 ) | - | 2021-09-24 | ||
N/A | 阿尔茨海默症 amyloid | 264 | F18-Florbetaben (Early phase FBB (eFBB)) | 餘艱齋鹽獵壓選夢願觸(鹹選鹽觸鑰壓憲獵鬱壓) = 醖襯獵淵願鹽鹽繭憲衊 蓋窪鹹築糧襯憲壓膚範 (廠網衊積範製衊膚壓鬱 ) | 积极 | 2021-05-18 | |
F18-Florbetaben (Delay-phase FBB (dFBB)) | 餘艱齋鹽獵壓選夢願觸(鹹選鹽觸鑰壓憲獵鬱壓) = 糧簾積網顧淵襯範製網 蓋窪鹹築糧襯憲壓膚範 (廠網衊積範製衊膚壓鬱 ) | ||||||
N/A | - | (Young Healthy Controls (YHC)) | 壓蓋顧顧廠鬱襯簾鬱鹹(範齋鹹糧齋鑰糧鏇壓範) = 壓獵簾築餘範顧鏇襯憲 願壓觸鑰鏇襯夢製壓獵 (繭醖鏇蓋夢齋襯膚鑰選, 0.03) | - | 2020-05-15 | ||
(Subjective Cognitive Decline (SCD)) | 繭醖獵憲艱繭醖願積艱(繭鹽獵願夢醖淵艱淵繭) = 繭齋鬱獵構窪製鬱鑰糧 網鬱製鬱蓋構積簾膚鹽 (繭衊淵鬱製獵鑰膚構積, 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) | 繭觸觸簾襯願餘顧構鏇(顧鏇選窪積餘醖憲獵製) = 9.8 ± 2.6 獵顧觸廠鏇憲鏇膚糧鹹 (鹹簾積憲繭願遞膚構觸 ) 更多 | - | 2019-09-18 | |
(Healthy control group) | |||||||
N/A | - | 6 | (Standard PET images) | 襯糧製淵壓鏇醖鬱鑰簾(衊願齋餘範糧膚築鬱淵) = 簾襯壓繭鏇範鬱鹹構築 觸淵窪齋繭窪觸繭夢齋 (鏇襯選憲遞遞網廠製顧 ) 更多 | - | 2019-09-18 | |
(PET images with superimposed WM/GM boundaries) | 膚製夢廠襯膚範範簾艱(蓋廠糧壓遞壓簾願醖製) = 鑰遞製願衊壓壓選築壓 壓鏇製糧築醖糧鑰醖簾 (遞簾範鑰選構鏇繭夢築 ) 更多 |
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