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- The Evolution of Radionanotargeting towards Clinical Precision Oncology: A Festschrift in Honor of Kalevi Kairemo
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Current Status of PSMA Targeted Alpha Therapy in Prostate Cancer Patients

- Authors: Thabo Lengana1, Mike Sathekge2
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View Affiliations Hide AffiliationsAffiliations: 1 Department of Nuclear Medicine, University of Pretoria & Steve Biko Academic Hospital,Pretoria 0001, South Africa 2 Department of Nuclear Medicine, University of Pretoria & Steve Biko Academic Hospital,Pretoria 0001, South Africa
- Source: The Evolution of Radionanotargeting towards Clinical Precision Oncology: A Festschrift in Honor of Kalevi Kairemo , pp 255-264
- Publication Date: March 2022
- Language: English
Despite multiple new agents having been available routinely for men with metastatic castration-resistant prostate cancer (mCRPC), the diagnosis remains fatal, with these agents contributing minimally to over-all survival. Targeting the prostatespecific membrane antigen (PSMA) has been attractive because it is overly expressed in prostate cancer cells with upregulation of the over-expression related to tumour grade, castration status and metastatic disease. To this end novel agents have been developed targeting the PSMA antigen not only for imaging but also for therapy. Actinium-225 (225Ac), an alpha emitter, has been labelled to PSMA ligands as 225Ac- PSMA for targeted alpha therapy (TAT). 225Ac deposits high energy, resulting in irreparable double strand DNA destruction while sparing surrounding normal tissue, making it an attractive anti-tumour agent. Clinical application of 225Ac-PSMA TAT as the last line of therapy in patients with mCRPC has demonstrated an excellent response, especially in the setting of chemotherapy-naive patients. Widespread application of 225Ac-PSMA TAT, though remains hampered by its salivary gland toxicity.
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