Florbenazine F18(Florbenazine F18) - 药物靶点：VMAT2_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

(+)-18FP-DTBZ、18F-FP-Dihydrotatetrabenazine、[18F]FP-(+)- DTBZ

+ [7]

靶点

VMAT2

作用机制

VMAT2抑制剂(突触囊泡单胺转运体抑制剂)、PET imaging(正电子发射断层成像术增强剂)

治疗领域

神经系统疾病内分泌与代谢疾病其他疾病+ [1]

在研适应症-

非在研适应症

阿尔茨海默症胰岛素依赖型糖尿病22型糖尿病+ [6]

原研机构

University of Michigan College of Engineering

在研机构-

非在研机构

Avid Radiopharmaceuticals, Inc.Chang Gung Memorial Hospital

最高研发阶段终止临床2/3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

分子式C21H32FNO3

InChIKeyGNKGXQHHUUEYQV-WTHAECTESA-N

CAS号956903-29-0

关联

17

项与 Florbenazine F18 相关的临床试验

ChiCTR2100046464 / RecruitingN/AIIT

The application value of 18F-FDG and 18F-DTBZ PET imaging in the early diagnosis and evaluation of Parkinson's disease

开始日期2021-05-03

申办/合作机构-

ChiCTR2000036137 / Suspended早期临床1期IIT

Clinical study of 18F-FDG combined with 18F-AV-133 PET/CT imaging in the diagnosis and differentiation of primary Parkinson's disease

开始日期2020-10-01

申办/合作机构-

ChiCTR2200061295 / Recruiting早期临床1期IIT

Comparison of 18F-DOPA and 18F-DTBZ for PET/CT imaging of idiopathic Parkinson’s Disease

开始日期2017-01-01

申办/合作机构

中山大学附属第一医院

100 项与 Florbenazine F18 相关的临床结果

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100 项与 Florbenazine F18 相关的转化医学

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100 项与 Florbenazine F18 相关的专利（医药）

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14

项与 Florbenazine F18 相关的文献（医药）

2022-07-01·European Journal of Nuclear Medicine and Molecular Imaging

Unified spatial normalization method of brain PET images using adaptive probabilistic brain atlas

Article

作者: Liu, Hua ; Zhang, Tianhao ; Shan, Baoci ; Nie, Binbin

PURPOSEA unique advantage of the brain positron emission tomography (PET) imaging is the ability to image different biological processes with different radiotracers. However, the diversity of the brain PET image patterns also makes their spatial normalization challenging. Since structural MR images are not always available in the clinical practice, this study proposed a PET-only spatial normalization method based on adaptive probabilistic brain atlas.METHODSThe proposed method (atlas-based method) consists of two parts, an adaptive probabilistic brain atlas generation algorithm, and a probabilistic framework for registering PET image to the generated atlas. To validate this method, the results of MRI-based method and template-based method (a widely used PET-only method) were treated as the gold standard and control, respectively. A total of 286 brain PET images, including seven radiotracers (FDG, PIB, FBB, AV-45, AV-1451, AV-133, [¹⁸F]altanserin) and four groups of subjects (Alzheimer disease, Parkinson disease, frontotemporal dementia, and healthy control), were spatially normalized using the three methods. The results were then quantitatively compared by using correlation analysis, meta region of interest (meta-ROI) standardized uptake value ratio (SUVR) analysis, and statistical parametric mapping (SPM) analysis.RESULTSThe Pearson correlation coefficient between the images computed by atlas-based method and the gold standard was 0.908 ± 0.005. The relative error of meta-ROI SUVR computed by atlas-based method was 2.12 ± 0.18%. Compared with template-based method, atlas-based method was also more consistent with the gold standard in SPM analysis.CONCLUSIONThe proposed method provides a unified approach to spatially normalize brain PET images of different radiotracers accurately without MR images. A free MATLAB toolbox for this method has been provided.

2018-05-01·Journal of Pharmaceutical and Biomedical Analysis3区 · 医学

Developing a cassette microdosing approach to enhance the throughput of PET imaging agent screening

3区 · 医学

Article

作者: Zhao, Ruiyue ; Liu, Yajing ; Zhang, Yan ; Hong, Haiyan ; Zhang, Aili ; Zhu, Lin ; Sun, Mingyue ; Xiao, Hao ; Zhang, Shuxian ; Qiao, Jinping ; Kung, Hank F ; Liu, Futao

Cassette dosing is also known as N-in-One dosing: several compounds are simultaneously administrated to a single animal and then the samples are rapidly detected by LC-MS/MS. This approach is a successful strategy to enhance the efficiency of drug discovery and reduce animal usage. However, no report on the utility of the cassette approach in radiotracer discovery has appeared in the literature. This study designed a cassette microdose with LC-MS/MS method to enhance the throughput for screening radiopharmaceutical biodistribution in the rat brain directly. Three unradiolabeled compounds (FPBM FPBM2 and AV-133) were chosen as model drugs administrated intravenously to the rats as a cassette as opposed to discrete study. The rat brain biodistribution data, target localization, the differential uptake ratio (%ID/g) and the brain tissue-specific binding ratio were obtained by the LC-MS/MS analysis. These data matched very well with the values obtained by the standard radioactivity measurements. Moreover, no significant differences between discrete dosing and cassette dosing were observed. By circumventing the need for radiolabeled molecules, this method may be high-throughput and safe for the research and development of new PET imaging agents. The combination of cassette microdosing and LC-MS/MS would be a medium throughput screening tool at an early stage in the discovery/development process of PET imaging agents.

2016-06-06·ChemMedChem3区 · 医学

Pancreas‐Specific Delivery of β‐Cell Proliferating Small Molecules

3区 · 医学

Article

作者: Va, Porino ; Li, Chun ; Hao, Xueshi ; Wu, Tom Y.‐H. ; Laffitte, Bryan ; Shen, Weijun ; Jin, Qihui

AbstractOur research groups recently described a series of small‐molecule inducers of β‐cell proliferation that could be used to increase β‐cell mass. To mitigate the risk of nonspecific proliferation of other cell types, we devised a delivery strategy built on the tissue specificity observed in the experimental β‐cell imaging agent (+)‐dihydrotetrabenazine (DTBZ). The β‐cell proliferator agent aminopyrazine (AP) was covalently linked with (+)‐DTBZ to afford conjugates that retain both the proliferation activity and binding affinity for vesicular monoamine transporter‐2 (VMAT2). In vivo mouse tissue distribution studies of a prototypical AP–DTBZ conjugate showed 15‐fold pancreas exposure over plasma. Tissue‐to‐plasma ratios in liver and kidneys were two‐ and five‐fold, respectively. This work is the first demonstration of enhanced delivery of β‐cell‐proliferating molecules to the pancreas by leveraging the intrinsic tissue specificity of a β‐cell imaging agent.

100 项与 Florbenazine F18 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB14945

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
糖尿病前期	临床3期	美国	Avid Radiopharmaceuticals, Inc.	2012-12-01
神经变性	临床3期	美国	Avid Radiopharmaceuticals, Inc.	2012-04-01
神经变性	临床3期	澳大利亚	Avid Radiopharmaceuticals, Inc.	2012-04-01
帕金森病	临床3期	澳大利亚	Avid Radiopharmaceuticals, Inc.	2012-04-01
帕金森病	临床3期	美国	Avid Radiopharmaceuticals, Inc.	2012-04-01
胰岛素依赖型糖尿病2	临床3期	美国	Avid Radiopharmaceuticals, Inc.	2010-06-01
2型糖尿病	临床3期	美国	Avid Radiopharmaceuticals, Inc.	2010-06-01
阿尔茨海默症	临床3期	美国	Avid Radiopharmaceuticals, Inc.	2010-03-01
路易体病	临床3期	美国	Avid Radiopharmaceuticals, Inc.	2010-03-01
纹状体黑质变性	临床3期	美国	Avid Radiopharmaceuticals, Inc.	2010-03-01

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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


NCT01556100 (CTgov)	临床2期	帕金森病	40	18F-DTBZ AV-133	製餘範糧鬱觸夢網鹹網(鑰鬱糧襯壓鹽襯憲艱廠) = 鬱鏇夢製鹽積構衊願製築憲憲積憲網網鹽鏇觸 (築鬱壓齋膚齋蓋淵鏇製, 膚艱選築壓餘衊範鹹鏇 ~ 繭鑰壓齋襯蓋醖糧艱積) 更多	-	2017-12-15
NCT01838785 (CTgov)	临床2期	-	25	18F-DTBZ AV-133	廠鬱製壓範簾窪糧窪願(範壓窪網蓋夢範鹽顧鏇) = 遞膚襯鏇窪夢齋簾構糧蓋鬱艱鹹觸鑰構範壓簾 (壓淵鹹憲壓艱鏇鹹獵遞, 壓蓋顧糧廠糧範築衊鹹 ~ 艱構襯壓餘壓廠壓膚簾) 更多	-	2017-09-25