• Journal of Radiopharmaceuticals and Molecular Probes
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• v.5 no.2
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• pp.135-144
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• 2019

Targeted alpha therapy (TAT) based on metallic radionuclides has attracted a lot of attention lately due to its impressive therapeutic efficacy displayed in couple of clinical studies for cancer. Representative metallic radionuclides emitting alpha-particle include 225Ac, 213Bi, and 227Th, and there have been variety of TAT formulations based on different targeting moiety and chelating agents. In this review, we introduce strategies to label metallic radioisotopes with biomolecules and look at some of recent preclinical and clinical results of TAT for cancer.

• Journal of radiological science and technology
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• v.46 no.5
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• pp.379-394
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• 2023

Targeted Alpha Therapy (TAT) is a new method of cancer treatment that protects normal tissues while selectively killing tumor cells using high cytotoxicity and short range of alpha particles, and target alpha therapy is a highly specific and effective cancer treatment strategy, and its potential has been proven through many clinical and experimental studies. This treatment method accurately delivers alpha particles by selecting specific molecules present in cancer tissue, which has an effective destruction and tumor suppression effect on cancer cells, and one of the main advantages of target alpha treatment is the physical properties of alpha particles. Alpha particles have a very high energy and short effective distance, interacting with target molecules in cancer tissues and having a fatal effect on cancer cells, which is known to cause DNA damage and cell death in cancer cells. TAT has shown positive results in preclinical and clinical studies for various types of cancers, especially those that resist or are unresponsive to existing treatments, but there are several challenges and limitations to overcome for successful clinical transition and application. These include the provision and production of suitable alpha radioisotopes, optimization of target vectors and delivery formulations, understanding and regulation of radiological effects, accurate dosage calculation and toxicity assessment. Future research should focus on developing new or improved isotopes, target vectors, transfer formulations, radiobiological models, combination strategies, imaging techniques, etc. for TAT. In addition, TAT has the potential to improve the quality of life and survival of cancer patients due to the possibility of a new treatment for overcoming cancer, and to this end, prospective research on more carcinomas and more diverse patient groups is needed.