18 F-Tetrafluoroborate, a PET Probe for Imaging Sodium/Iodide Symporter Expression: Whole-Body Biodistribution, Safety, and Radiation Dosimetry in Thyroid Cancer Patients

• Published in: Journal of Nuclear Medicine Vol. 58; no. 10; pp. 1666 - 1671
• Main Authors: O’Doherty, Jim, Jauregui-Osoro, Maite, Brothwood, Teresa, Szyszko, Teresa, Marsden, Paul K., O’Doherty, Michael J., Cook, Gary J.R., Blower, Philip J., Lewington, Val
• Format: Journal Article
• Language: English
• Published: United States 01.10.2017
• Subjects: Borates - adverse effects; Borates - metabolism; Borates - pharmacokinetics; Boric Acids - adverse effects; Boric Acids - metabolism; Boric Acids - pharmacokinetics; Female; Gene Expression Regulation, Neoplastic; Humans; Male; Middle Aged; Positron Emission Tomography Computed Tomography - methods; Radiometry; Safety; Symporters - metabolism; Thyroid Neoplasms - diagnostic imaging; Thyroid Neoplasms - metabolism; Tissue Distribution; 18F-TFB; thyroid imaging; PET/CT
• DOI: 10.2967/jnumed.117.192252
• ISSN: 0161-5505

We report the safety, biodistribution, and internal radiation dosimetry, in humans with thyroid cancer, of F-tetrafluoroborate ( F-TFB), a novel PET radioligand for imaging the human sodium/iodide symporter (hNIS). 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 of F-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. Images showed a high uptake of F-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). Imaging using F-TFB imparts a radiation exposure similar in magnitude to many other F-labeled radiotracers. F-TFB shows a biodistribution similar to Tc-pertechnetate, a known nonorganified hNIS tracer, and is pharmacologically and radiobiologically safe in humans. Phase 2 trials for F-TFB as an hNIS imaging agent are warranted.