In vivo assessment of safety, biodistribution, and radiation dosimetry of the [¹⁸F]Me4FDG PET-radiotracer in adults.

IF 4.3 3区材料科学 Q1 ENGINEERING, ELECTRICAL & ELECTRONIC ACS Applied Electronic Materials Pub Date : 2024-05-15 DOI:10.1186/s13550-024-01098-2

Barbara Katharina Geist, Juan Carlos Ramirez, Patrick Binder, Holger Einspieler, Harald Ibeschitz, Werner Langsteger, Lukas Nics, Ivo Rausch, Markus Diemling, Antti Sohlberg, Marcus Hacker, Sazan Rasul

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Abstract

Background: Approaches targeting the sodium-glucose cotransporter (SGLT) could represent a promising future therapeutic strategy for numerous oncological and metabolic diseases. In this study, we evaluated the safety, biodistribution and radiation dosimetry of the glucose analogue positron emission tomography (PET) agent [¹⁸F] labeled alpha-methyl-4-deoxy-4-[¹⁸F]fluoro-D-glucopyranoside ([¹⁸F]Me4FDG) with high sodium-glucose cotransporter and low glucose transporter (GLUT) affinity. For this purpose, five healthy volunteers (1 man, 4 women) underwent multiple whole-body PET/computed tomography (CT) examinations starting with injection and up to 4 h after injection of averaged (2.4 ± 0.1) MBq/kg (range: 2.3-2.5 MBq/kg) administered activity. The PET/CT scans were conducted in 5 separate sessions, blood pressure and temperature were measured, and blood and urine samples were collected before the scans and one hour after injection to assess toxicity. Measurements of [¹⁸F]Me4FDG radioactivity in organs of interest were determined from the PET/CT scans at 5 time points. Internal dosimetry was performed on voxel level using a fast Monte Carlo approach.

Results: All studied volunteers could well tolerate the [¹⁸F]Me4FDG and no adverse event was reported. The calculated effective dose was (0.013 ± 0.003) mSv/MBq. The organs with the highest absorbed dose were the kidneys with 0.05 mSv/MBq per kidney. The brain showed almost no uptake. After 60 min, (12 ± 15) % of the administered dose was excreted into the bladder.

Conclusion: Featuring an effective dose of only 0.013 ± 0.003 mSv/MBq and no occurrence of side effects, the glucose analogue [¹⁸F]Me4FDG seems to be a safe radio-tracer with a favorable biodistribution for PET imaging and also within several consecutive scans.

Trial registration number: NCT03557138, Registered 22 February 2017, https://ichgcp.net/clinical-trials-registry/NCT03557138 .

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在成人体内评估[18F]Me4FDG PET-放射性示踪剂的安全性、生物分布和辐射剂量。

背景：针对钠-葡萄糖共转运体（SGLT）的方法可能是未来治疗多种肿瘤和代谢性疾病的一种很有前景的策略。在这项研究中，我们评估了葡萄糖类似物正电子发射断层扫描（PET）制剂[18F]标记的α-甲基-4-脱氧-4-[18F]氟-D-吡喃葡萄糖苷（[18F]Me4FDG）的安全性、生物分布和辐射剂量学，该制剂具有较高的钠-葡萄糖共转运体亲和力和较低的葡萄糖转运体（GLUT）亲和力。为此，5 名健康志愿者（1 名男性，4 名女性）在注射平均（2.4 ± 0.1） MBq/kg（范围：2.3-2.5 MBq/kg）的给药活性后 4 小时内，接受了多次全身 PET/CT（计算机断层扫描）检查。PET/CT 扫描分 5 次进行，测量血压和体温，并在扫描前和注射后一小时采集血液和尿液样本以评估毒性。通过 PET/CT 扫描确定了 5 个时间点相关器官中的[18F]Me4FDG 放射性。内部剂量测定采用快速蒙特卡洛方法在体素水平上进行：结果：所有接受研究的志愿者都能很好地耐受[18F]Me4FDG，没有出现任何不良反应。计算得出的有效剂量为 (0.013 ± 0.003) mSv/MBq。吸收剂量最高的器官是肾脏，每个肾脏的吸收剂量为 0.05 mSv/MBq。大脑几乎没有吸收。60 分钟后，（12 ± 15）%的给药剂量被排入膀胱：结论：葡萄糖类似物[18F]Me4FDG的有效剂量仅为0.013 ± 0.003 mSv/MBq，且无副作用，似乎是一种安全的放射性示踪剂，在PET成像中具有良好的生物分布，可连续扫描数次：NCT03557138，2017年2月22日注册，https://ichgcp.net/clinical-trials-registry/NCT03557138 。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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