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诊疗用放射性药物:当前正在使用的已确立的药物。

Theranostic radiopharmaceuticals: established agents in current use.

作者信息

Ballinger James R

机构信息

1 Department of Imaging Chemistry and Biology, School of Biomedical Engineering and Imaging Sciences, King's College London , London , UK.

出版信息

Br J Radiol. 2018 Nov;91(1091):20170969. doi: 10.1259/bjr.20170969. Epub 2018 Mar 12.

Abstract

Although use of the term "theranostic" is relatively recent, the concept goes back to the earliest days of nuclear medicine, with the use of radioiodine for diagnosis and therapy of benign and malignant thyroid disease being arguably the most successful molecular radiotherapy in history. A diagnostic scan with I-, I-, or a low activity of I-iodide is followed by therapy with high activity I-iodide. Similarly, adrenergic tumours such as phaeochromocytoma and neuroblastoma can be imaged with I-metaiodobenzylguanidine and treated with I-metaiodobenzylguanidine. Bone scintigraphy can be used to select patients with painful bone metastases from prostate cancer who may benefit from treatment with beta- or alpha-particle emitting bone seeking agents, the most recent and successful of which is Ra radium chloride. Anti-CD20 monoclonal antibodies can be used to image and treat non-Hodgkins lymphoma, though this has not been as commercially successful as initially predicted. More recently established theranostics include somatostatin receptor targeting peptides for diagnosis and treatment of neuroendocrine tumours with agents such as Ga-DOTATATE and Lu-DOTATATE, respectively. Finally, agents which target prostate-specific membrane antigen are becoming increasingly widely available, despite the current lack of a commercial product. With the recent licensing of the somatostatin peptides and the rapid adoption of Ga- and Lu-labelled prostate-specific membrane antigen targeting agents, we have built upon the experience of radioiodine and are already seeing a great expansion in the availability of widely accepted theranostic radiopharmaceuticals.

摘要

尽管“治疗诊断学”这一术语的使用相对较新,但其概念可追溯到核医学的早期,使用放射性碘诊断和治疗良性及恶性甲状腺疾病可以说是历史上最成功的分子放射疗法。先用I-、I-或低活度的I-碘化物进行诊断扫描,然后用高活度的I-碘化物进行治疗。同样,嗜铬细胞瘤和神经母细胞瘤等肾上腺素能肿瘤可用I-间碘苄胍进行成像,并可用I-间碘苄胍进行治疗。骨闪烁显像可用于挑选可能从发射β或α粒子的亲骨性药物治疗中获益的前列腺癌骨转移疼痛患者,其中最新且最成功的是氯化镭。抗CD20单克隆抗体可用于成像和治疗非霍奇金淋巴瘤,不过其商业成功程度未达最初预期。最近确立的治疗诊断学方法包括分别用Ga-DOTATATE和Lu-DOTATATE等药物靶向生长抑素受体的肽类,用于诊断和治疗神经内分泌肿瘤。最后,尽管目前缺乏商业化产品,但靶向前列腺特异性膜抗原的药物越来越容易获得。随着生长抑素肽类最近获得许可,以及Ga和Lu标记的靶向前列腺特异性膜抗原药物的迅速采用,我们借鉴了放射性碘的经验,目前已看到广泛接受的治疗诊断用放射性药物的可及性大幅增加。

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