title: 18F-Tetrafluoroborate, a PET Probe for Imaging Sodium/Iodide Symporter Expression: Whole-Body Biodistribution, Safety, and Radiation Dosimetry in Thyroid Cancer Patients.
abstract: We report the safety, biodistribution, and internal radiation dosimetry, in humans with thyroid cancer, of18F-tetrafluoroborate (18F-TFB), a novel PET radioligand for imaging the human sodium/iodide symporter (hNIS).Methods:Serial whole-body PET scans of 5 subjects with recently diagnosed thyroid cancer were acquired before surgery for up to 4 h after injection of 184 ± 15 MBq of18F-TFB. Activity was determined in whole blood, plasma, and urine. Mean organ-absorbed doses and effective doses were calculated via quantitative image analysis and using OLINDA/EXM software.Results:Images showed a high uptake of18F-TFB in known areas of high hNIS expression (thyroid, salivary glands, and stomach). Excretion was predominantly renal. No adverse effects in relation to safety of the radiopharmaceutical were observed. The effective dose was 0.0326 ± 0.0018 mSv/MBq. The critical tissues/organs receiving the highest mean sex-averaged absorbed doses were the thyroid (0.135 ± 0.079 mSv/MBq), stomach (0.069 ± 0.022 mSv/MBq), and salivary glands (parotids, 0.031 ± 0.011 mSv/MBq; submandibular, 0.061 ± 0.031 mSv/MBq). Other organs of interest were the bladder (0.102 ± 0.046 mSv/MBq) and kidneys (0.029 ± 0.009 mSv/MBq).Conclusion:Imaging using18F-TFB imparts a radiation exposure similar in magnitude to many other18F-labeled radiotracers.18F-TFB shows a biodistribution similar to99mTc-pertechnetate, a known nonorganified hNIS tracer, and is pharmacologically and radiobiologically safe in humans. Phase 2 trials for18F-TFB as an hNIS imaging agent are warranted.
authors.affiliation: PET Imaging Centre, Division of Imaging Sciences and Biomedical Engineering, King's College London, St. Thomas' Hospital, London, United Kingdom; and.
authors.forename: Jim
authors.initials: J
authors.lastname: O'Doherty
authors.affiliation: PET Imaging Centre, Division of Imaging Sciences and Biomedical Engineering, King's College London, St. Thomas' Hospital, London, United Kingdom; and.
authors.forename: Maite
authors.initials: M
authors.lastname: Jauregui-Osoro
authors.affiliation: Department of Nuclear Medicine, Guy's & St. Thomas' Hospital NHS Foundation Trust, Great Maze Pond, London, United Kingdom.
authors.forename: Teresa
authors.initials: T
authors.lastname: Brothwood
authors.affiliation: PET Imaging Centre, Division of Imaging Sciences and Biomedical Engineering, King's College London, St. Thomas' Hospital, London, United Kingdom; and.
authors.forename: Teresa
authors.initials: T
authors.lastname: Szyszko
authors.affiliation: PET Imaging Centre, Division of Imaging Sciences and Biomedical Engineering, King's College London, St. Thomas' Hospital, London, United Kingdom; and.
authors.forename: Paul K
authors.initials: PK
authors.lastname: Marsden
authors.affiliation: PET Imaging Centre, Division of Imaging Sciences and Biomedical Engineering, King's College London, St. Thomas' Hospital, London, United Kingdom; and.
authors.forename: Michael J
authors.initials: MJ
authors.lastname: O'Doherty
authors.affiliation: PET Imaging Centre, Division of Imaging Sciences and Biomedical Engineering, King's College London, St. Thomas' Hospital, London, United Kingdom; and.
authors.forename: Gary J R
authors.initials: GJR
authors.lastname: Cook
authors.affiliation: PET Imaging Centre, Division of Imaging Sciences and Biomedical Engineering, King's College London, St. Thomas' Hospital, London, United Kingdom; and.
authors.forename: Philip J
authors.initials: PJ
authors.lastname: Blower
authors.affiliation: Department of Nuclear Medicine, Guy's & St. Thomas' Hospital NHS Foundation Trust, Great Maze Pond, London, United Kingdom val.lewington@gstt.nhs.uk.
authors.forename: Val
authors.initials: V
authors.lastname: Lewington
mesh_terms: D001881:Borates / Q000009:adverse effects / Q000378:metabolism / Q000493:pharmacokinetics*; D001888:Boric Acids / Q000009:adverse effects / Q000378:metabolism / Q000493:pharmacokinetics*; D005260:Female; D015972:Gene Expression Regulation, Neoplastic; D006801:Humans; D008297:Male; D008875:Middle Aged; D000072078:Positron Emission Tomography Computed Tomography / Q000379:methods*; D011874:Radiometry; D012449:Safety; D027981:Symporters / Q000378:metabolism*; D013964:Thyroid Neoplasms / Q000000981:diagnostic imaging* / Q000378:metabolism*; D014018:Tissue Distribution; D000099209:Sodium-Iodide Symporters
chemical_list: D001881:Borates; D001888:Boric Acids; D027981:Symporters; D000099209:Sodium-Iodide Symporters; C098759:fluoroboric acid
keywords: 18F-TFB; PET/CT; thyroid imaging