Al18F-PSMA-BCH制备工艺的改进及其初步影像学研究

中华核医学与分子影像杂志 Pub Date : 2019-12-25 DOI:10.3760/CMA.J.ISSN.2095-2848.2019.12.008

Te-li Liu, Chen Liu, Lei Xia, Xiaoyi Guo, Jinquan Jiang, Hua Zhu, Nan Li, Tie Wang, Zhi Yang

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引用次数: 0

摘要

目的优化前列腺特异性膜抗原（PSMA）靶向探针Al18F-PSMA-BCH（北京癌症医院）的放射性标记，评价其临床试验和转化潜力。方法将PSMA-BCH、AlCl3、邻苯二甲酸钾和未负载18F-载体的混合物在110℃下反应15min，然后用Sep-Pak Light C18柱纯化，用0.22μm无菌过滤器过滤，得到Al18F-PSMA BCH。测定了放射性标记的产率和放射化学纯度。对5名健康志愿者（年龄：（68±7）岁）和1名患有复发性前列腺癌症的患者（65岁）进行了Al18F-PSMA-BCH PET/CT成像，以进行生物分布和辐射剂量测定。结果Al18F-PSMA-BCH的非衰变校正放射化学产率为（38.0±3.5）%，放射化学纯度>99%，比活性为（16.4±4.4）MBq/nmol。Al18F PSMA BCH在室温下在生理盐水中是稳定的。在健康志愿者中，放射性主要积聚在膀胱、肾脏、泪腺、腮腺和下颌下腺，其中肾脏是最关键的器官，剂量为（152.89±33.43）μGy/MBq，而骨骼的摄取量（11.10±1.23）μGy/MBq）低于大多数器官。全身有效剂量为（0.0135±0.0025）mSv/MBq。通过Al18F-PSMA-BCH PET/CT成像观察了一例复发性前列腺癌症患者的多发骨转移。结论用邻苯二甲酸钾pH控制器制备的Al18F-PSMA-BCH具有诊断、分期和监测癌症复发的潜力。关键词：前列腺肿瘤；前列腺特异性膜抗原；同位素标记；氟放射性同位素；正电子发射断层扫描；层析成像，X射线计算机

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Improvement of Al18F-PSMA-BCH preparation and its preliminary imaging study

Objective To optimize the radiolabeling of prostate specific membrane antigen (PSMA)-targeted probe Al18F-PSMA-BCH (Beijing Cancer Hospital) and to evaluate its potential for clinical trial and translation. Methods The mixture of PSMA-BCH, AlCl3, potassium biphthalate and no-carrier loaded 18F- was reacted at 110 ℃ for 15 min, then purified by Sep-Pak Light C18 column and filtered through 0.22 μm sterile filter to obtain Al18F-PSMA-BCH. The radiolabeled yield and radiochemical purity were determined. Al18F-PSMA-BCH PET/CT imaging was performed on 5 healthy volunteers (age: (68±7) years) for biodistribution and radiation dosimetry estimate and on 1 patient (65 years) with recurrent prostate cancer. Results The non-decay-corrected radiochemical yield of Al18F-PSMA-BCH was (38.0±3.5)% with the radiochemical purity >99% and the specific activity of (16.4±4.4) MBq/nmol. Al18F-PSMA-BCH was stable in saline at room temperature. In healthy volunteers, radioactivity was mainly accumulated in the bladder, kidneys, lacrimal glands, parotid glands and submandibular glands, of which kidneys were the most critical organs with the dosimetry of (152.89±33.43) μGy/MBq, while bones showed lower uptake ((11.10±1.23) μGy/MBq) than most organs. The effective dose of whole body was (0.013 5 ±0.002 5) mSv/MBq. Multiple bone metastases were observed by Al18F-PSMA-BCH PET/CT imaging in a patient with recurrent prostate cancer. Conclusions Al18F-PSMA-BCH prepared with the pH controller of potassium biphthalate holds the potential for the diagnosis, staging and monitoring recurrence of prostate cancer. Key words: Prostatic neoplasms; Prostate-specific membrane antigen; Isotope labeling; Fluorine radioisotopes; Positron-emission tomography; Tomography, X-ray computed

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来源期刊

中华核医学与分子影像杂志核医学，分子影像

自引率

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发文量

5088

期刊介绍： Chinese Journal of Nuclear Medicine and Molecular Imaging (CJNMMI) was established in 1981, with the name of Chinese Journal of Nuclear Medicine, and renamed in 2012. As the specialized periodical in the domain of nuclear medicine in China, the aim of Chinese Journal of Nuclear Medicine and Molecular Imaging is to develop nuclear medicine sciences, push forward nuclear medicine education and basic construction, foster qualified personnel training and academic exchanges, and popularize related knowledge and raising public awareness. Topics of interest for Chinese Journal of Nuclear Medicine and Molecular Imaging include: -Research and commentary on nuclear medicine and molecular imaging with significant implications for disease diagnosis and treatment -Investigative studies of heart, brain imaging and tumor positioning -Perspectives and reviews on research topics that discuss the implications of findings from the basic science and clinical practice of nuclear medicine and molecular imaging - Nuclear medicine education and personnel training - Topics of interest for nuclear medicine and molecular imaging include subject coverage diseases such as cardiovascular diseases, cancer, Alzheimer’s disease, and Parkinson’s disease, and also radionuclide therapy, radiomics, molecular probes and related translational research.