ArticleEJNMMI research2016
[(18)F]tetrafluoroborate as a PET tracer for the sodium/iodide symporter: the importance of specific activity.
Article in EJNMMI research, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed, 42 citations in OpenAlex.
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- Advances in the Development of Positron Emission Tomography Tracers for Improved Detection of Differentiated Thyroid Cancer.Cancers · 2024Review
- Synthesis, Characterization, and Computational Studies on Gallium(III) and Iron(III) Complexes with a Pentadentate MacrocyclicInorganic chemistry · 2023Article
- Interleukin-6-controlled, mesenchymal stem cell-based sodium/iodide symporter gene therapy improves survival of glioblastoma-bearing mice.Molecular therapy oncolytics · 2023Article
- Article
- Dual EGFR- and TfR-targeted gene transfer for sodium iodide symporter gene therapy of glioblastoma.Molecular therapy oncolytics · 2022Article
- High molar activity [EJNMMI radiopharmacy and chemistry · 2022Article
- Positron Emission Tomography Radiopharmaceuticals in Differentiated Thyroid Cancer.Molecules (Basel, Switzerland) · 2022Review
- The sodium iodide symporter (NIS) as theranostic gene: its emerging role in new imaging modalities and non-viral gene therapy.EJNMMI research · 2022Review
- Evaluation of [Molecular imaging · 2022Article
- Options for imaging cellular therapeutics in vivo: a multi-stakeholder perspective.Cytotherapy · 2021Review
- Non-invasive Reporter Gene Imaging of Cell Therapies, including T Cells and Stem Cells.Molecular therapy : the journal of the American Society of Gene Therapy · 2020Review
- How Non-invasiveFrontiers in physiology · 2020Review
- Imaging of T-cells and their responses during anti-cancer immunotherapy.Theranostics · 2019Review
- The Human Sodium Iodide Symporter as a Reporter Gene for Studying Middle East Respiratory Syndrome Coronavirus Pathogenesis.mSphere · 2018Article
- Cousins at work: How combining medical with optical imaging enhances in vivo cell tracking.The international journal of biochemistry & cell biology · 2018Review
- Rapid Aqueous Late-Stage Radiolabelling of [GaFAngewandte Chemie (International ed. in English) · 2018Article
- Radionuclide-fluorescence Reporter Gene Imaging to Track Tumor Progression in Rodent Tumor Models.Journal of visualized experiments : JoVE · 2018Article
- [Theranostics · 2018Review
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Authors and funding
10 authors at 2 institutions in 1 country.
Funding
Abstract
background[(18)F]BF4 (-), the first (18)F-labelled PET imaging agent for the sodium/iodide symporter (NIS), was produced by isotopic exchange yielding a product with limited specific activity (SA, ca. 1 GBq/μmol) posing a risk of sub-optimal target-to-background ratios (TBR) in PET images due to saturation of NIS in vivo. We sought to quantify this risk and to develop a method of production of [(18)F]BF4 (-) with higher SA.
methodsA new radiosynthesis of [(18)F]BF4 (-) was developed, involving reaction of [(18)F]F(-) with boron trifluoride diethyl etherate under anhydrous conditions, guided by (11)B and (19)F NMR studies of equilibria involving BF4 (-) and BF3. The SA of the product was determined by ion chromatography. The IC50 of [(19)F]BF4 (-) as an inhibitor of [(18)F]BF4 (-) uptake was determined in vitro using HCT116-C19 human colon cancer cells expressing the human form of NIS (hNIS). The influence of [(19)F]BF4 (-) dose on biodistribution in vivo was evaluated in normal mice by nanoPET imaging and ex vivo tissue counting.
resultsAn IC50 of 4.8 μΜ was found in vitro indicating a significant risk of in vivo NIS saturation at SA achieved by the isotopic exchange labelling method. In vivo thyroid and salivary gland uptake decreased significantly with [(19)F]BF4 (-) doses above ca. 10 μg/kg. The new radiosynthesis gave high radiochemical purity (>99 %) and moderate yield (15 %) and improved SA (>5 GBq/μmol) from a starting activity of only 1.5 GBq.
conclusions[(18)F]BF4 (-) produced at previously reported levels of SA (1 GBq/μmol) can lead to reduced uptake in NIS-expressing tissues in mice. This is much less likely in humans. The synthetic approach described provides an alternative for production of [(18)F]BF4 (-) at higher SA with sufficient yield and without need for unusually high starting activity of [(18)F]fluoride, removing the risk of NIS saturation in vivo even in mice.
trial registrationISRCTN75827286 .
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.