We report the safety, biodistribution, and internal radiation dosimetry, in humans with thyroid cancer, of ¹⁸F-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 of ¹⁸F-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 of ¹⁸F-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 using ¹⁸F-TFB imparts a radiation exposure similar in magnitude to many other ¹⁸F-labeled radiotracers. ¹⁸F-TFB shows a biodistribution similar to ^99mTc-pertechnetate, a known nonorganified hNIS tracer, and is pharmacologically and radiobiologically safe in humans. Phase 2 trials for ¹⁸F-TFB as an hNIS imaging agent are warranted.

^{我们报告了18} F-四氟硼酸盐 ( ¹⁸ F-TFB)在人类甲状腺癌中的安全性、生物分布和内部辐射剂量测定，18 F-四氟硼酸盐 ( 18 F-TFB) 是一种用于对人类钠/碘同向转运蛋白 (hNIS) 进行成像的新型 PET 放射性配体。方法：在手术前注射 184 ± 15 MBq ¹⁸ F-TFB后长达 4 小时内，对 5 名最近诊断出甲状腺癌的受试者进行了连续全身 PET 扫描。测定全血、血浆和尿液中的活性。通过定量图像分析并使用 OLINDA/EXM 软件计算平均器官吸收剂量和有效剂量。结果：图像显示hNIS 高表达的已知区域（甲状腺、唾液腺和胃）对¹⁸ F-TFB的高摄取。排泄主要通过肾脏。没有观察到与放射性药物安全性相关的副作用。有效剂量为0.0326±0.0018 mSv/MBq。接受最高平均性别平均吸收剂量的关键组织/器官是甲状腺（0.135 ± 0.079 mSv/MBq）、胃（0.069 ± 0.022 mSv/MBq）和唾液腺（腮腺，0.031 ± 0.011 mSv/MBq；颌下腺） ，0.061 ± 0.031 毫西弗/MBq）。其他感兴趣的器官是膀胱 (0.102 ± 0.046 mSv/MBq) 和肾脏 (0.029 ± 0.009 mSv/MBq)。结论：使用^{18 F-TFB 成像所产生的辐射暴露程度与许多其他18} F 标记放射性示踪剂相似。^{18 F-TFB 显示出与99m} Tc-pertechnetate（一种已知的非有机 hNIS 示踪剂）类似的生物分布，并且对人体具有药理学和放射生物学安全性。¹⁸ F-TFB 作为 hNIS 显像剂的2 期试验是有必要的。