本综述旨在概述最近在前瞻性 1-2 期临床试验中测试或目前用于泌尿生殖系统癌症的新型诊断和治疗放射性药物，总结进展和未来方向。使用 PubMed/MEDLINE 和 ClinicalTrials.gov 进行系统检索遵循系统评价和荟萃分析指南的首选报告项目的原始前瞻性研究数据库。对四十六篇论文进行了系统评价；确定了 74 项正在进行的临床试验。 27 种新型放射性药物（即未经美国食品药品监督管理局/欧洲药品管理局批准且未列入药典）对泌尿生殖系统癌症（主要是前列腺癌）进行前瞻性研究的结果，用于诊断、治疗诊断或治疗目的（21、一、分别介绍了过去 5 年 27 种放射性药物中的 5 种。大多数是前列腺特异性膜抗原靶向药物（17/27）；其他靶标包括胃泌素释放肽受体、碳酸酐酶 IX、Cu、前列腺六跨膜上皮抗原 1、肿瘤相关糖蛋白 42 和尿激酶型纤溶酶原激活剂受体。正在进行的研究证实了同样的趋势。成纤维细胞激活蛋白抑制剂、PD-L1、CD8、nectin-4 和 HER2 是其他正在研究的靶点。在 22 项正在进行的治疗试验（74 项正在进行的临床试验中）中，有 12 项正在探索靶向 α 疗法，其中 5 项正在评估放射性配体疗法与其他治疗的组合。我们确认了放射性药物的安全性（无论诊断/治疗目的如何），并在泌尿生殖系统癌症的诊断准确性和治疗效果方面显示出有希望的结果。泌尿生殖系统癌症的放射性药物方法不断扩展，反映出对改善肿瘤的高度重视检测和治疗，这可能会影响整个疾病谱的未来管理，并有可能改善患者护理和结果。版权所有 © 2024 欧洲泌尿外科协会。由 Elsevier B.V. 出版。保留所有权利。

This review aims to provide an overview of novel diagnostic and therapeutic radiopharmaceuticals tested recently or used currently in genitourinary cancers within prospective phase 1-2 clinical trials, summarizing progresses and future directions.A systematic search was conducted using the PubMed/MEDLINE and ClinicalTrials.gov databases for original prospective research studies following the Preferred Reporting Items for Systematic Reviews and Meta-analyses guidelines.Forty-six papers were systematically reviewed; 74 ongoing clinical trials were identified. The results of 27 novel radiopharmaceuticals (ie, not approved by the Food and Drug Administration/European Medicines Agency and not listed in the Pharmacopeia) prospectively investigated in genitourinary cancers, mostly prostate, for diagnostic, theranostic, or therapeutic purposes (21, one, and five of the 27 radiopharmaceuticals, respectively) over the past 5 yr were presented. Most were prostate-specific membrane antigen-targeting agents (17/27); other targets included gastrin-releasing peptide receptor, carbonic anhydrase IX, Cu, six transmembrane epithelial antigen of the prostate 1, tumor-associated glycoprotein 42, and urokinase-type plasminogen activator receptor. Ongoing research confirms the same trend. Fibroblast activation protein inhibitor, PD-L1, CD8, nectin-4, and HER2 are other targets under investigation. Among the 22 ongoing therapeutic trials (out of the 74 ongoing clinical trials), targeted alpha therapy is being explored in 12, and five are evaluating combinations of radioligand therapy with other treatments. We confirmed the safety of radiopharmaceuticals (regardless of the diagnostic/therapeutic purpose) and showed promising results in terms of diagnostic accuracy and therapeutic efficacy in genitourinary cancers.There continues to be expansion in radiopharmaceutical approaches to genitourinary cancers, reflecting a strong emphasis on improving tumor detection and treatment, which will likely impact future management across the disease spectrum, with the potential for improved patient care and outcomes.Copyright © 2024 European Association of Urology. Published by Elsevier B.V. All rights reserved.