Copper is essential for enzymatic processes throughout the body. [64Cu]copper (64Cu) positron emission tomography (PET) has been investigated as a diagnostic tool for certain malignancies, but has not yet been used to study copper homeostasis in humans. In this study, we determined the hepatic removal kinetics, biodistribution and radiation dosimetry of 64Cu in healthy humans by both intravenous and oral administration. Six healthy participants underwent PET/CT studies with intravenous or oral administration of 64Cu. A 90 min dynamic PET/CT scan of the liver was followed by three whole-body PET/CT scans at 1.5, 6, and 20 h after tracer administration. PET data were used for estimation of hepatic kinetics, biodistribution, effective doses, and absorbed doses for critical organs. After intravenous administration, 64Cu uptake was highest in the liver, intestinal walls and pancreas; the gender-averaged effective dose was 62 ± 5 μSv/MBq (mean ± SD). After oral administration, 64Cu was almost exclusively taken up by the liver while leaving a significant amount of radiotracer in the gastrointestinal lumen, resulting in an effective dose of 113 ± 1 μSv/MBq. Excretion of 64Cu in urine and faeces after intravenous administration was negligible. Hepatic removal kinetics showed that the clearance of 64Cu from blood was 0.10 ± 0.02 mL blood/min/mL liver tissue, and the rate constant for excretion into bile or blood was 0.003 ± 0.002 min− 1. 64Cu biodistribution and radiation dosimetry are influenced by the manner of tracer administration with high uptake by the liver, intestinal walls, and pancreas after intravenous administration, while after oral administration, 64Cu is rapidly absorbed from the gastrointestinal tract and deposited primarily in the liver. Administration of 50 MBq 64Cu yielded images of high quality for both administration forms with radiation doses of approximately 3.1 and 5.7 mSv, respectively, allowing for sequential studies in humans. EudraCT no. 2016–001975-59. Registration date: 19/09/2016.

中文翻译：

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通过[64Cu]铜PET / CT研究了健康人的静脉和口服铜动力学，生物分布和剂量学。

铜对于整个人体的酶促过程至关重要。已经研究了[64Cu]铜（64Cu）正电子发射断层扫描（PET）作为某些恶性肿瘤的诊断工具，但尚未用于研究人类体内铜稳态的研究。在这项研究中，我们通过静脉内和口服给药确定了健康人体内64Cu的肝清除动力学，生物分布和放射剂量。六名健康参与者通过静脉或口服64Cu进行了PET / CT研究。示踪剂给药后1.5、6和20小时，对肝脏进行90分钟动态PET / CT扫描，然后进行三次全身PET / CT扫描。PET数据用于评估关键器官的肝动力学，生物分布，有效剂量和吸收剂量。静脉内给药后，肝脏中64Cu摄取最高，肠壁和胰腺；性别平均有效剂量为62±5μSv/ MBq（平均值±SD）。口服后，64Cu几乎完全被肝脏吸收，同时在胃肠道腔内留下大量放射性示踪剂，导致有效剂量为113±1μSv/ MBq。静脉给药后尿液和粪便中64Cu的排泄量可以忽略不计。肝清除动力学表明，血液中64Cu的清除率为0.10±0.02 mL血液/ min / mL肝组织，排泄到胆汁或血液中的速率常数为0.003±0.002 min-1。64Cu的生物分布和辐射剂量受到以下因素的影响静脉内给药后，口服后肝脏，肠壁和胰腺高摄取示踪剂的方式，64Cu从胃肠道迅速吸收并主要沉积在肝脏中。分别以大约3.1和5.7 mSv的辐射剂量施用50 MBqq 64Cu可以产生高质量的两种给药形式的图像，从而可以在人体中进行顺序研究。EudraCT号 2016–001975-59。报名日期：19/09/2016。