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Tc-IDA-D-[c(RGDfK)](BIK-505)的生物分布与体内辐射剂量学研究,一种新型 SPECT 放射性示踪剂用于整合素 αβ 表达的成像。

Biodistribution and Internal Radiation Dosimetry of Tc-IDA-D-[c(RGDfK)] (BIK-505), a Novel SPECT Radiotracer for the Imaging of Integrin αβ Expression.

机构信息

1 Department of Nuclear Medicine, Seoul National University Bundang Hospital, Seoul National University College of Medicine , Seongnam, Republic of Korea.

2 Division of Chemical and Medical Metrology, Center for Ionizing Radiation, Korea Research Institute of Standards and Science , Daejeon, Republic of Korea.

出版信息

Cancer Biother Radiopharm. 2018 Nov;33(9):396-402. doi: 10.1089/cbr.2018.2505. Epub 2018 Aug 22.

Abstract

BACKGROUND

Integrin αβ is a molecular marker for the estimation of tumor angiogenesis. Tc-IDA-D-[c(RGDfK)] (also known as BIK-505) is a recently developed radiotracer for single-photon emission computed tomography, with good affinity for integrin αβ. In this study, the authors investigated the whole-body distribution and internal radiation dosimetry of Tc-IDA-D-[c(RGDfK)] in elderly human participants.

MATERIALS AND METHODS

Six healthy volunteers underwent whole-body simultaneous anterior and posterior scans, preceded by transmission scans using cobalt-57 flood source, with a dual head gamma camera system, at 0, 1, 2, 4, 8, and 24 h postinjection of Tc-IDA-D-[c(RGDfK)] (injected radioactivity [mean ± SD] = 388.7 ± 29.3 MBq). Anterior and posterior images were geometrically averaged and attenuation corrected to delineate the regions of interest in the liver, gallbladder, kidneys, urinary bladder, spleen, brain, and large intestine. Radiation dose for each organ and the effective doses (EDs) were estimated using OLINDA/EXM 1.1 software.

RESULTS

High radiation doses of renal and biliary excretion tracks such as the urinary bladder wall, upper large intestine, kidneys, liver, and gallbladder wall (19.15 ± 6.84, 19.28 ± 4.78, 15.67 ± 0.90, 9.13 ± 1.71, and 9.09 ± 2.03 μGy/MBq, respectively) were observed. The ED and effective dose equivalent were 5.08 ± 0.53 and 7.11 ± 0.58 μSv/MBq, respectively.

CONCLUSIONS

Dosimetry results were comparable to other radiolabeled peptides and were considered safe and efficient for clinical usage.

摘要

背景

整合素 αβ 是评估肿瘤血管生成的分子标志物。Tc-IDA-D-[c(RGDfK)](也称为 BIK-505)是一种最近开发的用于单光子发射计算机断层扫描的放射性示踪剂,对整合素 αβ 具有良好的亲和力。在这项研究中,作者研究了 Tc-IDA-D-[c(RGDfK)]在老年人体参与者中的全身分布和内部辐射剂量。

材料和方法

六名健康志愿者在前瞻性和后向性全身扫描前,使用钴-57 洪水源进行透射扫描,使用双头伽马相机系统,在注射 Tc-IDA-D-[c(RGDfK)](注射放射性[平均值±标准差] = 388.7 ± 29.3 MBq)后 0、1、2、4、8 和 24 小时进行。前向和后向图像进行几何平均和衰减校正,以描绘肝脏、胆囊、肾脏、膀胱、脾脏、大脑和大肠的感兴趣区域。使用 OLINDA/EXM 1.1 软件估算每个器官的辐射剂量和有效剂量(ED)。

结果

观察到高辐射剂量的肾和胆道排泄途径,如膀胱壁、大肠上部、肾脏、肝脏和胆囊壁(19.15 ± 6.84、19.28 ± 4.78、15.67 ± 0.90、9.13 ± 1.71 和 9.09 ± 2.03 μGy/MBq)。ED 和有效剂量当量分别为 5.08 ± 0.53 和 7.11 ± 0.58 μSv/MBq。

结论

剂量学结果与其他放射性标记肽相似,被认为对临床应用是安全有效的。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/30ae/6241326/0764ebb012c6/fig-1.jpg

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