18F-FPYBF-2, a new F-18 labelled amyloid imaging PET tracer: biodistribution and radiation dosimetry assessment of first-in-man 18F-FPYBF-2 PET imaging
18F-FPYBF-2, a new F-18 labelled amyloid imaging PET tracer: biodistribution and radiation dosimetry assessment of first-in-man 18F-FPYBF-2 PET imaging
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18F-FPYBF-2，一种新型 F-18 标记淀粉样蛋白成像 PET 示踪剂：首次人体 18F-FPYBF-2 PET 成像的生物分布和辐射剂量测定评估
DOI：
10.1007/s12149-018-1240-5
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发表时间：
2018
期刊：
影响因子：
2.6
通讯作者：
Yamauchi Hiroshi
中科院分区：
文献类型：
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作者：
Nishii Ryuichi;Higashi Tatsuya;Kagawa Shinya;Okuyama Chio;Kishibe Yoshihiko;Takahashi Masaaki;Okina Tomoko;Suzuki Norio;Hasegawa Hiroshi;Nagahama Yasuhiro;Ishizu Koichi;Oishi Naoya;Kimura Hiroyuki;Watanabe Hiroyuki;Ono Masahiro;Saji Hideo;Yamauchi Hiroshi
最近，用于β-淀粉样蛋白斑块成像的苯并呋喃衍生物，5-（5-（2-（2-（2- 18 F-氟乙氧基）乙氧基）苯并呋喃-2-基）-N-甲基吡啶-2-胺（18 F-FPYBF-2）已被验证为淀粉样蛋白成像的示踪剂，并且发现18 F-FPYBF-2 PET/CT是用于评估AD的有用且可靠的诊断工具（Higashi等人，Ann Nucl Med， https://doi.org/10.1007/s12149-018-1236-1 ，2018年）。本研究的目的是评估诊断剂量的18 F-FPYBF-2在正常健康志愿者中的生物分布和辐射剂量学，作为首次人体研究。方法4名正常健康志愿者（男：3名，女：1名;平均年龄：40 ± 17;年龄范围25-56），并进行18 F-FPYBF-2 PET/CT研究，以评估辐射暴露和药代动力学。在注射18 F-FPYBF-2后0-10 min进行10 min的全身（胸部和腹部）动态PET/CT扫描，并在注射后6 min进行15 min的全身静态扫描。在重建PET和CT图像数据后，通过拟合来自动态扫描和全身扫描的感兴趣体积数据来估计单个器官的时间-活性曲线。OLINDA/EXM 2.0版软件被用来确定全身有效dose.ResultsDynamic PET成像表明，肝胆和肾脏系统的清除of 18 F-FPYBF-2的主要途径。在肝脏和胆囊、胃和肾脏中显示出高摄取，其次是肠和膀胱。成人剂量测定模型的艾德ED估计为8.48 ± 1.25 µSv/MBq。估计肝脏的吸收剂量较高（28.98 ± 12.49和36.21 ± 15.64 μ戈伊/MBq），脑（20.93 ± 4.56和23.05 ± 5.03μ戈伊/MBq），成骨细胞小肠（9.67 ± 1.67和10.29 ± 1.70 µ戈伊/MBq）（9.12 ± 2.61和11.12 ± 3.15 µ戈伊/MBq），肾脏（7.81 ± 2.62和8.71 ± 2.90 μ戈伊/MBq.ConclusionsThe艾德为成人剂量测定模型是相似的其他代理人用于淀粉样蛋白PET成像。18F-FPYBF-2的诊断剂量185-370 MBq被认为是可接受的，可用于患者给药，作为评价AD的诊断工具。
ObjectiveRecently, a benzofuran derivative for the imaging of β-amyloid plaques, 5-(5-(2-(2-(2-18F-fluoroethoxy)ethoxy)ethoxy)benzofuran-2-yl)-N-methylpyridin-2-amine (18F-FPYBF-2) has been validated as a tracer for amyloid imaging and it was found that18F-FPYBF-2 PET/CT is a useful and reliable diagnostic tool for the evaluation of AD (Higashi et al. Ann Nucl Med, https://doi.org/10.1007/s12149-018-1236-1 , 2018). The aim of this study was to assess the biodistribution and radiation dosimetry of diagnostic dosages of18F-FPYBF-2 in normal healthy volunteers as a first-in-man study.MethodsFour normal healthy volunteers (male: 3, female: 1; mean age: 40 ± 17; age range 25–56) were included and underwent18F-FPYBF-2 PET/CT study for the evaluation of radiation exposure and pharmacokinetics. A 10-min dynamic PET/CT scan of the body (chest and abdomen) was performed at 0–10 min and a 15-min whole-body static scan was performed six times after the injection of18F-FPYBF-2. After reconstructing PET and CT image data, individual organ time–activity curves were estimated by fitting volume of interest data from the dynamic scan and whole-body scans. The OLINDA/EXM version 2.0 software was used to determine the whole-body effective doses.ResultsDynamic PET imaging demonstrated that the hepatobiliary and renal systems were the principal pathways of clearance of18F-FPYBF-2. High uptake in the liver and the gall bladder, the stomach, and the kidneys were demonstrated, followed by the intestines and the urinary bladder. The ED for the adult dosimetric model was estimated to be 8.48 ± 1.25 µSv/MBq. The higher absorbed doses were estimated for the liver (28.98 ± 12.49 and 36.21 ± 15.64 µGy/MBq), the brain (20.93 ± 4.56 and 23.05 ± 5.03µ Gy/MBq), the osteogenic cells (9.67 ± 1.67 and 10.29 ± 1.70 µGy/MBq), the small intestines (9.12 ± 2.61 and 11.12 ± 3.15 µGy/MBq), and the kidneys (7.81 ± 2.62 and 8.71 ± 2.90 µGy/MBq) for male and female, respectively.ConclusionsThe ED for the adult dosimetric model was similar to those of other agents used for amyloid PET imaging. The diagnostic dosage of 185–370 MBq of18F-FPYBF-2 was considered to be acceptable for administration in patients as a diagnostic tool for the evaluation of AD.
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DOI：
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发表时间：
2013
期刊：
Mol Imaging Biol.
影响因子：
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作者：
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9.3
作者：
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通讯作者：
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影响因子：
2.2
作者：
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通讯作者：
Kase, KR
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影响因子：
9.3
作者：
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DOI：
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发表时间：
2001
期刊：
影响因子：
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作者：
D. Macey;Lawrence E. Williams;Hazel B. Breitz;An Liu;Timothy K. Johnson;Pat B. Zanzonico
通讯作者：
Pat B. Zanzonico