Division of Nuclear Medicine and Molecular Imaging Center, Department of Radiology, Keck School of Medicine of USC, University of Southern California, 2250 Alcazar St., CSC 102, Los Angeles, CA, 90033, USA.
Eur J Nucl Med Mol Imaging. 2021 Dec;49(1):47-53. doi: 10.1007/s00259-021-05405-0. Epub 2021 May 16.
Progress in unraveling the complex biology of cancer, novel developments in radiochemistry, and availability of relevant α-emitters for targeted therapy have provided innovative approaches to precision cancer management. The approval of Ra dichloride for treatment of men with osseous metastatic castrate-resistant prostate cancer unleashed targeted α-therapy as a safe and effective cancer management strategy. While there is currently active research on new α-therapy regimens for prostate cancer based on the prostate-specific membrane antigen, there is emerging development of radiopharmaceutical therapy with a range of biological targets and α-emitting radioisotopes for malignancies other than the prostate cancer. This article provides a brief review of preclinical and first-in-human studies of targeted α-therapy in the cancers of brain, breast, lung, gastrointestinal, pancreas, ovary, and the urinary bladder. The data on leukemia, melanoma, myeloma, and neuroendocrine tumors will also be presented. It is anticipated that with further research the emerging role of targeted α-therapy in cancer management will be defined and validated.
在揭示癌症复杂生物学、放射化学的新进展,以及可用于靶向治疗的相关 α 发射体方面的进展,为精准癌症管理提供了创新方法。氯化镭获批用于治疗有骨转移的去势抵抗性前列腺癌男性患者,将靶向 α 疗法作为一种安全有效的癌症管理策略释放出来。虽然目前正在基于前列腺特异性膜抗原对前列腺癌的新 α 疗法方案进行积极研究,但针对前列腺癌以外的恶性肿瘤的放射性药物治疗方案也在不断发展,涉及多种生物靶点和 α 发射放射性同位素。本文简要综述了靶向 α 疗法在脑、乳腺、肺、胃肠道、胰腺、卵巢和膀胱等癌症中的临床前和首例人体研究。还将介绍白血病、黑色素瘤、骨髓瘤和神经内分泌肿瘤的数据。预计随着进一步的研究,靶向 α 疗法在癌症管理中的新兴作用将得到定义和验证。