PURPOSE To assess the safety, biodistribution, and radiation dosimetry of the novel positron emission tomography (PET) radiopharmaceutical 1-((2-fluoro-6-[[18F]]fluorophenyl)sulfonyl)-4-((4-methoxyphenyl)sulfonyl)piperazine ([18F]DASA-23) in healthy volunteers. METHODS We recruited 5 healthy volunteers who provided a written informed consent. Volunteers were injected with 295.0 ± 8.2 MBq of [18F]DASA-23 intravenously. Immediately following injection, a dynamic scan of the brain was acquired for 15 min. This was followed by serial whole-body PET/MRI scans acquired up to 3 h post-injection. Blood samples were collected at regular intervals, and vital signs monitored pre- and post-radiotracer administration. Regions of interest were drawn around multiple organs, time-activity curves were calculated, and organ uptake and dosimetry were estimated with OLINDA/EXM (version 1.1) software. RESULTS All subjects tolerated the PET/MRI examination, without adverse reactions to [18F]DASA-23. [18F]DASA-23 passively crossed the blood-brain barrier, followed by rapid clearance from the brain. High accumulation of [18F]DASA-23 was noted in organs such as the gallbladder, liver, small intestine, and urinary bladder, suggesting hepatobiliary and urinary clearance. The effective dose of [18F]DASA-23 was 23.5 ± 5.8 μSv/MBq. CONCLUSION We successfully completed a pilot first-in-human study of [18F]DASA-23. Our results indicate that [18F]DASA-23 can be used safely in humans to evaluate pyruvate kinase M2 levels. Ongoing studies are evaluating the ability of [18F]DASA-23 to visualize intracranial malignancies, NCT03539731. TRIAL REGISTRATION ClinicalTrials.gov, NCT03539731 (registered 28 May 2018).

中文翻译：

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[18F]DASA-23（一种靶向丙酮酸激酶 M2 的 PET 探针）的人体生物分布和辐射剂量测定。

目的 评估新型正电子发射断层扫描 (PET) 放射性药物 1-((2-fluoro-6-[[18F]]fluorophenyl)sulfonyl)-4-((4-methoxyphenyl)sulfonyl) 的安全性、生物分布和辐射剂量学) 健康志愿者中的哌嗪 ([18F]DASA-23)。方法 我们招募了 5 名提供书面知情同意书的健康志愿者。志愿者静脉注射 295.0 ± 8.2 MBq [18F] DASA-23。注射后立即对大脑进行 15 分钟的动态扫描。随后是在注射后 3 小时内采集的系列全身 PET/MRI 扫描。定期收集血样，并监测放射示踪剂给药前后的生命体征。在多个器官周围绘制感兴趣区域，计算时间-活动曲线，使用 OLINDA/EXM（1.1 版）软件估计器官摄取和剂量测定。结果 所有受试者均耐受 PET/MRI 检查，对 [18F]DASA-23 无不良反应。[18F]DASA-23 被动地穿过血脑屏障，然后迅速从大脑中清除。在胆囊、肝脏、小肠和膀胱等器官中注意到 [18F]DASA-23 的高积累，表明肝胆和尿液清除。[18F]DASA-23 的有效剂量为 23.5 ± 5.8 μSv/MBq。结论 我们成功地完成了 [18F]DASA-23 的首次人体试验研究。我们的结果表明，[18F]DASA-23 可以安全地用于人类评估丙酮酸激酶 M2 水平。正在进行的研究正在评估 [18F]DASA-23 可视化颅内恶性肿瘤的能力，NCT03539731。试验注册 ClinicalTrials.gov,