Tadashi Watabe, Sadahiro Naka, Yoshifumi Shirakami, Kazuko Kaneda, Masashi Murakami, Atsushi Toyoshima, Jens Cardinale, Frederik L Giesel
{"title":"Development of PSMA-Targeted Alpha Therapy Using [<sup>211</sup>At]PSMA-5.","authors":"Tadashi Watabe, Sadahiro Naka, Yoshifumi Shirakami, Kazuko Kaneda, Masashi Murakami, Atsushi Toyoshima, Jens Cardinale, Frederik L Giesel","doi":"10.1053/j.semnuclmed.2025.09.005","DOIUrl":null,"url":null,"abstract":"<p><p>Astatine (<sup>211</sup>At) is an alpha-emitting nuclide with a 7.2-hour half-life that can be produced using a 30-MeV cyclotron. In recent years, the number of production sites worldwide has been increasing, attracting growing attention to <sup>211</sup>At. We have developed a novel <sup>211</sup>At-labeled PSMA-targeted agent ([<sup>211</sup>At]PSMA-5). After conducting preclinical evaluations of its antitumor efficacy and safety, we initiated a first-in-human, investigator-initiated clinical trial in patients with metastatic castration-resistant prostate cancer. To date, the drug has been administered to a total of nine patients, and we have reported high accumulation of [<sup>211</sup>At]PSMA-5 in recurrent and metastatic lesions. While further efforts are required for the social implementation of <sup>211</sup>At-based targeted alpha therapy, including the establishment of a supply chain and the accumulation of additional clinical evidence, PSMA-targeted alpha therapy using <sup>211</sup>At represents a promising treatment modality owing to its cyclotron-based production, sustainability, and clean decay characteristics.</p>","PeriodicalId":21643,"journal":{"name":"Seminars in nuclear medicine","volume":" ","pages":""},"PeriodicalIF":5.9000,"publicationDate":"2025-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Seminars in nuclear medicine","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1053/j.semnuclmed.2025.09.005","RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING","Score":null,"Total":0}
引用次数: 0
Abstract
Astatine (211At) is an alpha-emitting nuclide with a 7.2-hour half-life that can be produced using a 30-MeV cyclotron. In recent years, the number of production sites worldwide has been increasing, attracting growing attention to 211At. We have developed a novel 211At-labeled PSMA-targeted agent ([211At]PSMA-5). After conducting preclinical evaluations of its antitumor efficacy and safety, we initiated a first-in-human, investigator-initiated clinical trial in patients with metastatic castration-resistant prostate cancer. To date, the drug has been administered to a total of nine patients, and we have reported high accumulation of [211At]PSMA-5 in recurrent and metastatic lesions. While further efforts are required for the social implementation of 211At-based targeted alpha therapy, including the establishment of a supply chain and the accumulation of additional clinical evidence, PSMA-targeted alpha therapy using 211At represents a promising treatment modality owing to its cyclotron-based production, sustainability, and clean decay characteristics.
期刊介绍:
Seminars in Nuclear Medicine is the leading review journal in nuclear medicine. Each issue brings you expert reviews and commentary on a single topic as selected by the Editors. The journal contains extensive coverage of the field of nuclear medicine, including PET, SPECT, and other molecular imaging studies, and related imaging studies. Full-color illustrations are used throughout to highlight important findings. Seminars is included in PubMed/Medline, Thomson/ISI, and other major scientific indexes.