Delving into the Latest Updates on [18F]Tetrafluoroborate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

NIS

Action

modulators, enhancers

Mechanism

NIS modulators(solute carrier family 5 member 5 modulators), PET imaging(Positron-emission tomography enhancers)

Therapeutic Areas

NeoplasmsUrogenital Diseases

Active Indication

Endometrial Carcinomaendometrial clear cell carcinomaEndometrial Endometrioid Adenocarcinoma+ [8]

Inactive Indication

Multiple Myeloma

Originator Organization

Mayo Clinic

Active Organization

National Cancer Institute

Mayo Clinic

Inactive Organization-

Drug Highest PhasePhase 2

First Approval Date-

Regulation-

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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.

Start Date15 Sep 2017

Sponsor / Collaborator

Mayo Clinic

[+1]

NCT02907073

/ TerminatedPhase 1/2IIT

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).

Start Date01 Sep 2016

Sponsor / Collaborator

Mayo Clinic

ISRCTN75827286

/ CompletedPhase 1

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

Start Date14 Sep 2015

Sponsor / Collaborator

King's College London

100 Clinical Results associated with [18F]Tetrafluoroborate

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100 Translational Medicine associated with [18F]Tetrafluoroborate

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100 Patents (Medical) associated with [18F]Tetrafluoroborate

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13

Literatures (Medical) associated with [18F]Tetrafluoroborate

01 Jan 2023·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

Author: 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.

01 Dec 2021·Biochimica et Biophysica Acta (BBA) - General SubjectsQ3 · BIOLOGY

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

Q3 · BIOLOGY

Article

Author: 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.

01 Dec 2016·Journal of Immunological Methods

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

Article

Author: 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 Deals associated with [18F]Tetrafluoroborate

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Endometrial Carcinoma	Phase 2	-	Mayo Clinic	-
endometrial clear cell carcinoma	Phase 1	United States	National Cancer Institute	15 Sep 2017
Endometrial Endometrioid Adenocarcinoma	Phase 1	United States	National Cancer Institute	15 Sep 2017
Endometrial Mixed Carcinoma	Phase 1	United States	National Cancer Institute	15 Sep 2017
Recurrent Endometrial Cancer	Phase 1	United States	National Cancer Institute	15 Sep 2017
Relapsed Uterine Corpus Sarcoma	Phase 1	United States	National Cancer Institute	15 Sep 2017
Uterine Corpus Cancer	Phase 1	United States	National Cancer Institute	15 Sep 2017
Uterine Serous Carcinoma	Phase 1	United States	National Cancer Institute	15 Sep 2017
uterus adenocarcinoma	Phase 1	United States	National Cancer Institute	15 Sep 2017
Multiple Myeloma	Preclinical	United States	Mayo Clinic	01 Sep 2016

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03120624 (Voyager-V1, CTgov)	Phase 1	Uterine Corpus Cancer \| Endometrial Endometrioid Adenocarcinoma \| Relapsed Uterine Corpus Sarcoma \| endometrial clear cell carcinoma \| Endometrial Mixed Carcinoma \| Uterine Serous Carcinoma \| Metastatic endometrial cancer \| Endometrial Undifferentiated Carcinoma \| Recurrent Endometrial Cancer \| uterus adenocarcinoma	34	TFB+technetium Tc-99m sodium pertechnetate+fluorine F18 tetrafluoroborate+VSV-hIFNbeta-NIS (Cohort A Dose Level 1)	czzmhwsubq(wyvtbuzydg) = pmznkijvkm ulxccvxrrw (uisbldqayx, wrkbwkllyi - aaontawedr) View more	-	29 Oct 2024
				TFB+technetium Tc-99m sodium pertechnetate+fluorine F18 tetrafluoroborate+VSV-hIFNbeta-NIS (Cohort A Dose Level 2)	czzmhwsubq(wyvtbuzydg) = zdtnvgnjuz ulxccvxrrw (uisbldqayx, kjuzqftlas - veikufnvwy) View more
NCT02907073 (CTgov)	Phase 1/2	Endometrial Carcinoma \| Multiple Myeloma	8	BF4 (Healthy Volunteers)	gmxhgwvtjx(uqtbsdyqfq) = iqrvconhwx ttaiqsethb (abojginnay, wzjizqdoxx - fmrgnbhqrq) View more	-	17 May 2019
				BF4 (Myeloma Patients)	byjounhjvn(yplhumxkmh) = agsmvadpbs oetdbpomat (bxxnkhujqf, izxllwpctf - romurvrvwq) View more