Turku PET Centre, University of Turku and Turku University Hospital, Turku, Finland
Turku PET Centre, University of Turku and Turku University Hospital, Turku, Finland.
J Nucl Med. 2021 May 10;62(5):679-684. doi: 10.2967/jnumed.120.252114. Epub 2020 Oct 16.
This first-in-humans study investigated the safety, biodistribution, and radiation dosimetry of a novel F-labeled radiohybrid prostate-specific membrane antigen (rhPSMA) PET imaging agent, F-rhPSMA-7.3. Six healthy volunteers (3 men, 3 women) underwent multiple whole-body PET acquisitions at scheduled time points up to 248 min after the administration of F-rhPSMA-7.3 (mean activity, 220; range, 210-228 MBq). PET scans were conducted in 3 separate sessions, and subjects were encouraged to void between sessions. Blood and urine samples were collected for up to 4 h after injection to assess metabolite-corrected radioactivity in whole blood, plasma, and urine. Quantitative measurements of F radioactivity in volumes of interest over target organs were determined directly from the PET images at 8 time points, and normalized time-activity concentration curves were generated. These normalized cumulated activities were then inputted into the OLINDA/EXM package to calculate the internal radiation dosimetry and the subjects' effective dose. F-rhPSMA-7.3 was well tolerated. One adverse event (mild headache, not requiring medication) was considered possibly related to F-rhPSMA-7.3. The calculated effective dose was 0.0141 mSv/MBq when using a 3.5-h voiding interval. The organs with the highest mean absorbed dose per unit of administered radioactivity were the adrenals (0.1835 mSv/MBq), the kidneys (0.1722 mSv/MBq), the submandibular glands (0.1479 mSv), and the parotid glands (0.1137 mSv/MBq). At the end of the first scanning session (mean time, 111 min after injection), an average of 7.2% (range, 4.4%-9.0%) of the injected radioactivity of F-rhPSMA-7.3 was excreted into urine. The safety, biodistribution, and internal radiation dosimetry of F-rhPSMA-7.3 are considered favorable for PET imaging.
这项首例人体研究调查了新型 F 标记放射性前列腺特异性膜抗原（rhPSMA）PET 成像剂 F-rhPSMA-7.3 的安全性、生物分布和辐射剂量学。6 名健康志愿者（3 名男性，3 名女性）在注射 F-rhPSMA-7.3 后至 248 分钟的预定时间点进行了多次全身 PET 采集（平均活度为 220；范围为 210-228MBq）。PET 扫描分 3 个阶段进行，鼓励受试者在各阶段之间排尿。在注射后 4 小时内采集血液和尿液样本，以评估全血、血浆和尿液中代谢校正放射性。通过直接从 PET 图像在 8 个时间点测量目标器官中 F 放射性的体积感兴趣区的定量测量，并生成归一化时间-活性浓度曲线。然后将这些归一化累积活动输入到 OLINDA/EXM 包中，以计算内部辐射剂量和受试者的有效剂量。F-rhPSMA-7.3 耐受性良好。1 例不良事件（轻度头痛，无需药物治疗）被认为可能与 F-rhPSMA-7.3 有关。使用 3.5 小时的排空间隔时，计算出的有效剂量为 0.0141mSv/MBq。单位放射性活度吸收剂量最高的器官依次为肾上腺（0.1835mSv/MBq）、肾脏（0.1722mSv/MBq）、颌下腺（0.1479mSv）和腮腺（0.1137mSv/MBq）。在第一次扫描阶段结束时（平均时间为注射后 111 分钟），平均有 7.2%（范围为 4.4%-9.0%）的 F-rhPSMA-7.3 放射性在尿液中排泄。F-rhPSMA-7.3 的安全性、生物分布和内部辐射剂量学被认为适合 PET 成像。
