Journal of Isotopes ›› 2021, Vol. 34 ›› Issue (1): 78-88.DOI: 10.7538/tws.2021.34.01.0078

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Research Progress of 64Cu-Radiopharmaceuticals in Clinical Trial for Tumor Diagnosis

ZHAO Hailong;LI Hongyu   

  1. HTA Co., Ltd., Beijing 102413, China
  • Online:2021-02-20 Published:2021-02-20



  1. 原子高科股份有限公司,北京102413


Positron computed emission tomography (PET) is an important diagnosis and imaging tool for nuclear medicine with the advantages of high sensitivity, resolution, and safety. It is widely used in the diagnosis of tumors, cardiovascular and cerebrovascular diseases, and so on. 64Cu nuclide has become the focus of research in the field of PET molecular probe and theranostic radiopharmaceuticals due to its suitable half-life (12.7 h), unique decay properties (β+, 0.653 MeV, 17.4%; β-, 0.579 MeV, 39%; electron capture) and the ability to form stable complexes with multiple ligands. Currently, more than 30 clinical studies of 64Cu-radiopharmaceuticals are on going with focus on neuroendocrine tumors, prostate cancer and hypoxic tumors. The results of these clinical trials of 64Cu-radiopharmaceuticals showed that 64Cu-radiopharmaceuticals had high resolution, detection rate and good safety. In addition, the long half-life of 64Cu nuclide allows 64Cu nuclide and 64Cu-radiopharmaceuticals to be transported to distant medical units, which is convenient for dose preparation and clinical practice. This paper selectively reviewed the progresses in clinical research conducted on 64Cu-radiopharmaceuticals in the past decade, hoping to provide some references and ideas for the future research and development of 64Cu-radiopharmaceuticals. It is expected that 64Cu-radiopharmaceuticals will be approved for the diagnosis of neuroendocrine tumors, prostate cancer and other diseases in the near future.

Key words: 64Cu-radiopharmaceuticals, clinical trial, neuroendocrine tumors, hypoxia, prostate cancer


正电子发射型计算机断层显像(positron emission computed tomography, PET)是核医学重要的诊断及显像工具,具有良好的灵敏度、分辨率和安全性,广泛应用于肿瘤、心脑血管等疾病的诊断。64Cu核素因其适宜的半衰期(12.7 h)、独特的衰变性质(β+衰变、β-衰变、电子俘获),以及可与多种配体配位形成配合物等特点,现已成为PET分子探针及诊疗一体化药物领域的研究热点。目前,有30多项针对64Cu标记药物的临床研究正在开展,主要集中在神经内分泌肿瘤、肿瘤乏氧、前列腺癌等方面;结果表明,64Cu标记药物的PET显像具有较高的分辨率、检出率,以及良好的安全性,另外64Cu相对较长的半衰期使得64Cu核素及其药物可运输至距离较远的医疗单位,方便药物制备及临床使用。本文对近十年来64Cu标记药物在肿瘤诊断方面的临床研究进展进行了总结,以期为今后64Cu标记药物的研发提供参考及思路;预期在不久的未来,将会有64Cu标记药物获批应用于神经内分泌肿瘤、前列腺癌等疾病的诊断。

关键词: 64Cu标记药物, 临床研究, 神经内分泌肿瘤, 乏氧, 前列腺癌