Kalevi Kairemo, Mankgopo Kgatle, Frank Bruchertseifer, Alfred Morgernstern, Mike M Sathekge
{"title":"设计用于前列腺癌α靶向治疗的 225Ac-PSMA","authors":"Kalevi Kairemo, Mankgopo Kgatle, Frank Bruchertseifer, Alfred Morgernstern, Mike M Sathekge","doi":"10.21037/atm-23-1842","DOIUrl":null,"url":null,"abstract":"<p><p>The first alpha emitting radiopharmaceutical, <sup>223</sup>RaCl<sub>2</sub>, radium dichloride, was approved 10 years ago into the clinical armament of treating bone metastases in metastatic castration-resistant prostate cancer (mCRPC). In addition to this, the first beta-emitting radionuclide Lu-177 chelated with a prostate-specific membrane antigen (PSMA) compound, got last year its marketing approval for the third line treatment of mCRPC. Therefore, there is great excitement about combining alpha-emitters and prostate cancer targeting PSMA compounds. This review describes the clinical history of alpha-emitting PSMA in treating mCRPC. Here, we present the potential, current status, and opportunities for <sup>225</sup>Ac-PSMA therapy. The work reviews the basic concepts, current treatment outcome, and toxicity, and areas requiring further investigations such as dosimetric aspects in clinical studies covering more than 400 patients. In general, approximately two-thirds of the patients benefit from this third-line therapy. There is also successful evidence of using <sup>225</sup>Ac-PSMA in the second-line of prostate cancer management. The future potential of <sup>225</sup>Ac-PSMA therapy and targeted alpha therapy (TAT) of cancer in general is enormous. According to our overview the clinical experience with <sup>225</sup>Ac-PSMA therapy to date has shown great benefit and physicians dedicated to theragnostics are anxiously waiting for new applications. Hopefully, this review helps in deeper understanding of the strengths and limitations of TAT and may help in creating effective therapy protocols.</p>","PeriodicalId":8216,"journal":{"name":"Annals of translational medicine","volume":"12 4","pages":"67"},"PeriodicalIF":0.0000,"publicationDate":"2024-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11304416/pdf/","citationCount":"0","resultStr":"{\"title\":\"Design of <sup>225</sup>Ac-PSMA for targeted alpha therapy in prostate cancer.\",\"authors\":\"Kalevi Kairemo, Mankgopo Kgatle, Frank Bruchertseifer, Alfred Morgernstern, Mike M Sathekge\",\"doi\":\"10.21037/atm-23-1842\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>The first alpha emitting radiopharmaceutical, <sup>223</sup>RaCl<sub>2</sub>, radium dichloride, was approved 10 years ago into the clinical armament of treating bone metastases in metastatic castration-resistant prostate cancer (mCRPC). In addition to this, the first beta-emitting radionuclide Lu-177 chelated with a prostate-specific membrane antigen (PSMA) compound, got last year its marketing approval for the third line treatment of mCRPC. Therefore, there is great excitement about combining alpha-emitters and prostate cancer targeting PSMA compounds. This review describes the clinical history of alpha-emitting PSMA in treating mCRPC. Here, we present the potential, current status, and opportunities for <sup>225</sup>Ac-PSMA therapy. The work reviews the basic concepts, current treatment outcome, and toxicity, and areas requiring further investigations such as dosimetric aspects in clinical studies covering more than 400 patients. In general, approximately two-thirds of the patients benefit from this third-line therapy. There is also successful evidence of using <sup>225</sup>Ac-PSMA in the second-line of prostate cancer management. The future potential of <sup>225</sup>Ac-PSMA therapy and targeted alpha therapy (TAT) of cancer in general is enormous. According to our overview the clinical experience with <sup>225</sup>Ac-PSMA therapy to date has shown great benefit and physicians dedicated to theragnostics are anxiously waiting for new applications. Hopefully, this review helps in deeper understanding of the strengths and limitations of TAT and may help in creating effective therapy protocols.</p>\",\"PeriodicalId\":8216,\"journal\":{\"name\":\"Annals of translational medicine\",\"volume\":\"12 4\",\"pages\":\"67\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2024-08-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11304416/pdf/\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Annals of translational medicine\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.21037/atm-23-1842\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2024/3/6 0:00:00\",\"PubModel\":\"Epub\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Annals of translational medicine","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.21037/atm-23-1842","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2024/3/6 0:00:00","PubModel":"Epub","JCR":"","JCRName":"","Score":null,"Total":0}
Design of 225Ac-PSMA for targeted alpha therapy in prostate cancer.
The first alpha emitting radiopharmaceutical, 223RaCl2, radium dichloride, was approved 10 years ago into the clinical armament of treating bone metastases in metastatic castration-resistant prostate cancer (mCRPC). In addition to this, the first beta-emitting radionuclide Lu-177 chelated with a prostate-specific membrane antigen (PSMA) compound, got last year its marketing approval for the third line treatment of mCRPC. Therefore, there is great excitement about combining alpha-emitters and prostate cancer targeting PSMA compounds. This review describes the clinical history of alpha-emitting PSMA in treating mCRPC. Here, we present the potential, current status, and opportunities for 225Ac-PSMA therapy. The work reviews the basic concepts, current treatment outcome, and toxicity, and areas requiring further investigations such as dosimetric aspects in clinical studies covering more than 400 patients. In general, approximately two-thirds of the patients benefit from this third-line therapy. There is also successful evidence of using 225Ac-PSMA in the second-line of prostate cancer management. The future potential of 225Ac-PSMA therapy and targeted alpha therapy (TAT) of cancer in general is enormous. According to our overview the clinical experience with 225Ac-PSMA therapy to date has shown great benefit and physicians dedicated to theragnostics are anxiously waiting for new applications. Hopefully, this review helps in deeper understanding of the strengths and limitations of TAT and may help in creating effective therapy protocols.
期刊介绍:
The Annals of Translational Medicine (Ann Transl Med; ATM; Print ISSN 2305-5839; Online ISSN 2305-5847) is an international, peer-reviewed Open Access journal featuring original and observational investigations in the broad fields of laboratory, clinical, and public health research, aiming to provide practical up-to-date information in significant research from all subspecialties of medicine and to broaden the readers’ vision and horizon from bench to bed and bed to bench. It is published quarterly (April 2013- Dec. 2013), monthly (Jan. 2014 - Feb. 2015), biweekly (March 2015-) and openly distributed worldwide. Annals of Translational Medicine is indexed in PubMed in Sept 2014 and in SCIE in 2018. Specific areas of interest include, but not limited to, multimodality therapy, epidemiology, biomarkers, imaging, biology, pathology, and technical advances related to medicine. Submissions describing preclinical research with potential for application to human disease, and studies describing research obtained from preliminary human experimentation with potential to further the understanding of biological mechanism underlying disease are encouraged. Also warmly welcome are studies describing public health research pertinent to clinic, disease diagnosis and prevention, or healthcare policy. With a focus on interdisciplinary academic cooperation, ATM aims to expedite the translation of scientific discovery into new or improved standards of management and health outcomes practice.