Human dosimetry of free (211)At and meta-[(211)At]astatobenzylguanidine ((211)At-MABG) estimated using preclinical biodistribution from normal mice.
Human dosimetry of free (211)At and meta-[(211)At]astatobenzylguanidine ((211)At-MABG) estimated using preclinical biodistribution from normal mice.
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DOI：
10.1186/s40658-020-00326-7
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发表时间：
2020-09-22
期刊：
影响因子：
4
通讯作者：
Ito H
中科院分区：
文献类型：
--
作者：
Ukon N;Zhao S;Washiyama K;Oriuchi N;Tan C;Shimoyama S;Aoki M;Kubo H;Takahashi K;Ito H
211At是放射性核素靶向治疗(TRT)的理想核素之一。~(211)At-间苯基胍(~(211)At-MABG)已被提出用于治疗嗜铬细胞瘤。为了有效地使用这些放射性药物，必须进行剂量测定。重要的是要确定游离~(211)At和~(211)At-MABG的吸收剂量，以确定在使用TRT时可能有危险的器官。本研究的目的是从正常小鼠不同器官中游离~(211)At和~(211)At-MABG在临床前的生物分布估计人体剂量学。雄性C57BL/6 N小鼠尾静脉注射游离~(211)At 0.13 MBq或~(211)At-MABG 0.20 MBq。分别于注射后5 、1、3、6、24 h处死小鼠(每组n = 5只)。测定各脏器和血液中每质量注射活度的百分比(%IA/g)。人体内游离~(211)At和~(211)At-MABG的吸收剂量用器官水平内剂量评估/指数模型(Olinda/exm)2.0版和IDAC-DUD2.1计算。肺、脾、唾液腺、胃和甲状腺对游离~(211)At的摄取较高。游离~(211)At在甲状腺和部分组织的吸收剂量高于~(211)At-MABG。~(211)At-MABG在肾上腺、心壁和肝脏的吸收剂量高于游离~(211)At。~(211)At-MABG在表达去甲肾上腺素转运体的器官中的吸收剂量高于游离~(211)At。此外，游离~(211)At的生物分布与~(211)At-MABG不同。在使用~(211)At-MABG进行TRT时，游离~(211)At的吸收剂量可能有助于预测由于破坏而可能面临危险的器官。
211At is one of the ideal nuclides for targeted radionuclide therapies (TRTs). Meta-[211At]astatobenzylguanidine (211At-MABG) has been proposed for the treatment of pheochromocytoma. To effectively use these radiopharmaceuticals, dosimetry must be performed. It is important to determine the absorbed doses of free 211At and 211At-MABG to determine the organs that may be at risk when using TRTs. The aim of this study was to estimate human dosimetry from preclinical biodistribution of free 211At and 211At-MABG in various organs in normal mice. Male C57BL/6 N mice were administered 0.13 MBq of free 211At or 0.20 MBq of 211At-MABG by tail-vein injection. The mice were sacrificed at 5 min, and at 1, 3, 6, and 24 h after the injection (n = 5 for each group). The percentage of injected activity per mass in organs and blood (%IA/g) was determined. The human absorbed doses of free 211At and 211At-MABG were calculated using the Organ Level INternal Dose Assessment/EXponential Modeling (OLINDA/EXM) version 2.0 and IDAC-Dose 2.1. High uptake of free 211At was observed in the lungs, spleen, salivary glands, stomach, and thyroid. The absorbed doses of free 211At in the thyroid and several tissues were higher than those of 211At-MABG. The absorbed doses of 211At-MABG in the adrenal glands, heart wall, and liver were higher than those of free 211At. The absorbed doses of 211At-MABG in organs expressing the norepinephrine transporter were higher than those of free 211At. In addition, the biodistribution of free 211At was different from that of 211At-MABG. The absorbed dose of free 211At may help predict the organs potentially at risk during TRTs using 211At-MABG due to deastatination.
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影响因子：
3.2
作者：
Andersson M;Johansson L;Eckerman K;Mattsson S
通讯作者：
Mattsson S
影响因子：
158.5
作者：
Parker, C.;Nilsson, S.;Sartor, O.
通讯作者：
Sartor, O.
影响因子：
9.3
作者：
Stabin, Michael G.;Siegel, Jeffry A.
通讯作者：
Siegel, Jeffry A.
DOI：
10.1007/s00259-017-3817-y
发表时间：
2018-01
影响因子：
9.1
作者：
Kratochwil C;Schmidt K;Afshar-Oromieh A;Bruchertseifer F;Rathke H;Morgenstern A;Haberkorn U;Giesel FL
通讯作者：
Giesel FL
影响因子：
3.4
作者：
Spetz, Johan;Rudqvist, Nils;Forssell-Aronsson, Eva
通讯作者：
Forssell-Aronsson, Eva