[18F]Tetrafluoroborate([18F]Tetrafluoroborate) - 药物靶点：NIS_在研适应症：子宫内膜癌，子宫内膜透明细胞癌，子宫内膜样腺癌_专利_临床

概要

基本信息

药物类型

小分子化药

别名-

靶点

NIS

作用方式

调节剂、增强剂

作用机制

NIS调节剂(solute carrier family 5 member 5 modulators)、PET imaging(正电子发射断层成像术增强剂)

治疗领域

肿瘤泌尿生殖系统疾病

在研适应症

子宫内膜癌子宫内膜透明细胞癌子宫内膜样腺癌+ [8]

非在研适应症

多发性骨髓瘤

原研机构

Mayo Clinic

在研机构

National Cancer Institute

Mayo Clinic

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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关联

3

项与 [18F]Tetrafluoroborate 相关的临床试验

NCT03120624

/ Active, not recruiting临床1期IIT

Phase I Trial of Intravenous Administration of Vesicular Stomatitis Virus Genetically Engineered to Express Thyroidal Sodium Iodide Symporter (NIS) and Human Interferon Beta (hIFNb), in Patients With Metastatic or Recurrent Endometrial Cancer

This phase I trial studies the side effects and best dose of vesicular stomatitis virus-human interferon beta-sodium iodide symporter (VSV-hIFNbeta-NIS) with or without ruxolitinib phosphate in treating patients with stage IV endometrial cancer or endometrial cancer that has come back. The study virus, VSV-hIFNbeta-NIS, has been changed so that it has restricted ability to spread to tumor cells and not to healthy cells. It also contains a gene for a protein, NIS, which helps the body concentrate iodine making it possible to track where the virus goes. VSV-hIFNbeta-NIS may be able to kill tumor cells without damaging normal cells. Ruxolitinib phosphate may stop the growth of tumor cells by blocking some of the enzymes needed for cell growth. Giving VSV-hIFNbeta-NIS with ruxolitinib phosphate may work better in treating patients with endometrial cancer compared to VSV-hIFNbeta-NIS alone.

开始日期2017-09-15

申办/合作机构

Mayo Clinic

[+1]

NCT02907073

/ Terminated临床1/2期IIT

First In-human PET Imaging Studies With NIS Reporter [18F]BF4

The goal of this proposal is to perform first-in-man evaluation of and experimental imaging agent F-18 tetrafluoroborate (BF4) or (TFB).

开始日期2016-09-01

申办/合作机构

Mayo Clinic

ISRCTN75827286

/ Completed临床1期

A phase I trial of [18F]-tetrafluoroborate in patients with primary thyroid cancer or salivary cancer to study biodistribution and uptake in tumours and normal NIS expressing tissue

开始日期2015-09-14

申办/合作机构

King's College London

100 项与 [18F]Tetrafluoroborate 相关的临床结果

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100 项与 [18F]Tetrafluoroborate 相关的转化医学

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100 项与 [18F]Tetrafluoroborate 相关的专利（医药）

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13

项与 [18F]Tetrafluoroborate 相关的文献（医药）

2023-01-01·Medicinal chemistry (Shariqah (United Arab Emirates))

Naphthofuran Derivative BF4, a New Potent SIRT1 Activator, Regulates Lipid Metabolism in 3T3-L1 Adipocytes via the SIRT1-AMPK Pathway.

Article

作者: Lin, Qisi ; Li, Fan ; Huang, Ye ; Li, Shihao ; Gao, Jian

AIMOur previously reported naphthofuran derivative BF4, identified as a potent silent information regulator 1 (SIRT1) activator, could alleviate high glucose stimulating apoptosis and inflammation response in human renal tubular epithelial (HK-2) cells.INTRODUCTIONIn this study, the underlying effects of BF4 on lipid metabolism in 3T3-L1 adipocytes were investigated.METHODSThe effects of BF4 on pre-adipocyte differentiation and adipocyte lipolysis were studied using oil red O staining and quantitative glycerol and triglyceride content assay kits. Moreover, the molecular mechanism of BF4 on adipogenesis and lipid metabolism in 3T3-L1 adipocytes was investigated by real-time quantitative PCR and Western blotting analysis.RESULTSWe found that compound BF4 significantly decreased adipogenesis and lipid accumulation and inhibited the differentiation of 3T3-L1 pre-adipocytes into adipocytes. Moreover, compound BF4 decreased the expressions of several key regulators in adipocyte differentiation, including C/EBPβ and PPARγ, and their downstream lipogenesis targets via the activation of the SIRT1/ AMPK pathway.CONCLUSIONOur results demonstrated that the novel SIRT1 activator BF4 might be a potent candidate for regulating lipid metabolism.

2021-12-01·Biochimica et Biophysica Acta (BBA) - General Subjects3区 · 生物学

Semysinthetic biflavonoid Morelloflavone-7,4′,7″,3‴,4‴-penta-O-butanoyl is a more potent inhibitor of Proprotein Convertases Subtilisin/Kexin PC1/3 than Kex2 and Furin

3区 · 生物学

Article

作者: Tersariol, Ivarne Luis Dos Santos ; de Souza, Aline Aparecida ; Veloso, Marcia Paranho ; Juliano, Luiz ; Judice, Wagner Alves de Souza ; Gontijo, Vanessa Silva ; Meneghetti, Maria Cecília Zorél ; de Andrade, Débora Martins ; Juliano, Maria Aparecida ; Viegas Junior, Claudio ; Dos Santos, Marcelo Henrique ; Siqueira, Fábio da Silva ; Di Iorio, Juliana Fortes ; Coelho, Camila de Morais ; Nader, Helena Bonciani

BACKGROUNDGarcinia brasiliensis is a species native to the Amazon forest. The white mucilaginous pulp is used in folk medicine as a wound healing agent and for peptic ulcer, urinary, and tumor disease treatments. The activity of the proprotein convertases (PCs) Subtilisin/Kex is associated with the development of viral, bacterial and fungal infections, osteoporosis, hyperglycemia, atherosclerosis, cardiovascular, neurodegenerative and neoplastic diseases.METHODSMorelloflavone (BF1) and semisynthetic biflavonoid (BF2, 3 and 4) from Garcinia brasiliensis were tested as inhibitor of PCs Kex2, PC1/3 and Furin, and determined IC₅₀, K_i, human proinflammatory cytokines secretion in Caco-2 cells, mechanism of inhibition, and performed molecular docking studies.RESULTSBiflavonoids were more effective in the inhibition of neuroendocrine PC1/3 than mammalian Furin and fungal Kex2. BF1 presented a mixed inhibition mechanism for Kex2 and PC1, and competitive inhibition for Furin. BF4 has no good interaction with Kex2 and Furin since carboxypropyl groups results in steric hindrance to ligand-protein interactions. Carboxypropyl groups of BF4 promote steric hindrance with Kex2 and Furin, but effective in the affinity of PC1/3. BF4 was more efficient at inhibiting PCl/3 (IC₅₀ = 1.13 μM and K_i = 0,59 μM, simple linear competitive mechanism of inhibition) than Kex2, Furin. Also, our results strongly suggested that BF4 also inhibits the endogenous cellular PC1/3 activity in Caco-2 cells, since PC1/3 inhibition by BF4 causes a large increase in IL-8 and IL-1β secretion in Caco-2 cells.CONCLUSIONSBF4 is a potent and selective inhibitor of PC1/3.GENERAL SIGNIFICANCEBF4 is the best candidate for further clinical studies on inhibition of PC1/3.

2016-12-01·Journal of Immunological Methods

Determining antigen specificity of a monoclonal antibody using genome-scale CRISPR-Cas9 knockout library

Article

作者: Mazurov, Dmitriy ; Filatov, Alexander ; Zotov, Ivan ; Zotova, Anastasia

An essential step in monoclonal antibody (mAb) development is the characterization and final identification of the specific target antigen and its epitope. Antibody validation is rather straightforward when immunization is carried out with peptide or purified protein, but is more difficult when whole cells or other complex antigens are used for the immunization. Determining antigen specificity of a mAb is further complicated, when reactivity of an antibody is not detected in Western blotting and/or immunoprecipitation assay. In addition to protein-based methods used for antibody characterization, a number of gene-based techniques, such as cDNA expression or short-interfering RNA (siRNA) knockdown have been applied for validation of antibodies with restricted reactivities. Earlier we have generated, characterized, but not identified the BF4 mAb that specifically stains viral biofilms on the surface of the Human T-lymphotropic Virus Type I (HTLV-1) infected T cells. In this study, using the recently developed genome-scale CRISPR-Cas9 knockout (GeCKO) library vectors, we have established the CEM T- and the Raji B cell lines with pooled libraries. After immunofluorescent staining of these cells, negative cell sorting, and guide-RNA (gRNA) sequencing, we have identified BF4 as an anti-CD82 mAb. A deep sequence analysis of GeCKO library transferred to the cells shows that the chance to succeed in the selection of antibody-negative cells and, therefore, to identify a mAb depends on the quality of cell library preparation. We believe that the described method is applicable for identification of many other hybridomas and represents a good alternative to the current protein- and gene-based methods used for mAb validation.

100 项与 [18F]Tetrafluoroborate 相关的药物交易

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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
子宫内膜癌	临床2期	-	Mayo Clinic	-
子宫内膜透明细胞癌	临床1期	美国	National Cancer Institute	2017-09-15
子宫内膜样腺癌	临床1期	美国	National Cancer Institute	2017-09-15
子宫内膜混合上皮癌	临床1期	美国	National Cancer Institute	2017-09-15
复发性子宫内膜癌	临床1期	美国	National Cancer Institute	2017-09-15
复发性子宫体肉瘤	临床1期	美国	National Cancer Institute	2017-09-15
子宫体癌	临床1期	美国	National Cancer Institute	2017-09-15
子宫浆液性癌	临床1期	美国	National Cancer Institute	2017-09-15
子宫腺癌	临床1期	美国	National Cancer Institute	2017-09-15
多发性骨髓瘤	临床前	美国	Mayo Clinic	2016-09-01

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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


NCT03120624 (Voyager-V1, CTgov)	临床1期	子宫体癌 \| 子宫内膜样腺癌 \| 复发性子宫体肉瘤 \| 子宫内膜透明细胞癌 \| 子宫内膜混合上皮癌 \| 子宫浆液性癌 \| 转移性子宫内膜恶性肿瘤 \| 子宫内膜未分化癌 \| 复发性子宫内膜癌 \| 子宫腺癌	34	TFB+technetium Tc-99m sodium pertechnetate+fluorine F18 tetrafluoroborate+VSV-hIFNbeta-NIS (Cohort A Dose Level 1)	鬱鏇艱築獵淵築夢鹽衊(餘衊艱衊鏇築餘廠鏇糧) = 蓋艱衊願鹽廠獵繭繭遞鑰願網艱窪衊範簾簾蓋 (製範顧鹹蓋鬱窪蓋鹹淵, 選鑰夢壓鹽顧廠觸鏇顧 ~ 壓遞網膚壓簾網艱鹽壓) 更多	-	2024-10-29
				TFB+technetium Tc-99m sodium pertechnetate+fluorine F18 tetrafluoroborate+VSV-hIFNbeta-NIS (Cohort A Dose Level 2)	鬱鏇艱築獵淵築夢鹽衊(餘衊艱衊鏇築餘廠鏇糧) = 築獵構壓簾網願壓製膚鑰願網艱窪衊範簾簾蓋 (製範顧鹹蓋鬱窪蓋鹹淵, 襯鹹選壓獵夢憲艱淵膚 ~ 選積齋鹽餘憲積襯網製) 更多
NCT02907073 (CTgov)	临床1/2期	子宫内膜癌 \| 多发性骨髓瘤	8	BF4 (Healthy Volunteers)	積廠憲遞選繭鏇積選構(選艱壓壓鬱鹹憲膚網鹹) = 襯憲淵壓膚夢壓範願簾積齋淵襯遞襯積蓋觸積 (淵夢觸蓋簾艱網襯鏇齋, 繭築選鏇選顧選鹽製選 ~ 獵餘蓋網襯觸繭膚範顧) 更多	-	2019-05-17
				BF4 (Myeloma Patients)	觸遞繭構範淵蓋觸鬱鏇(鬱齋積鏇憲製願憲獵繭) = 繭糧鹽觸簾積網鹽蓋鹹顧構積獵鏇願膚糧餘醖 (餘繭獵觸鬱蓋簾餘鹹齋, 遞鬱壓衊製鏇壓獵網鬱 ~ 淵獵餘糧願製簾襯鬱衊) 更多