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Auger Emitting Radiopharmaceuticals for Cancer Therapy

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Radiation Damage in Biomolecular Systems

Part of the book series: Biological and Medical Physics, Biomedical Engineering ((BIOMEDICAL))

Abstract

Radionuclides that emit Auger electrons have been of particular interest as therapeutic agents. This is primarily due to the short range in tissue, controlled linear paths and high linear energy transfer of these particles. Taking into consideration that ionizations are clustered within several cubic nanometers around the point of decay the possibility of incorporating an Auger emitter in close proximity to the cancer cell DNA has immense therapeutic potential thus making nuclear targeted Auger-electron emitters ideal for precise targeting of cancer cells. Furthermore, many Auger-electron emitters also emit γ-radiation, this property makes Auger emitting radionuclides a very attractive option as therapeutic and diagnostic agents in the molecular imaging and management of tumors. The first requirement for the delivery of Auger emitting nuclides is the definition of suitable tumor-selective delivery vehicles to avoid normal tissue toxicity. One of the main challenges of targeted radionuclide therapy remains in matching the physical and chemical characteristics of the radionuclide and targeting moiety with the clinical character of the tumor. Molecules and molecular targets that have been used in the past can be classified according to the carrier molecule used to deliver the Auger-electron-emitting radionuclide. These include (1) antibodies, (2) peptides, (3) small molecules, (4) oligonucleotides and peptide nucleic acids (PNAs), (5) proteins, and (6) nanoparticles. The efficacy of targeted radionuclide therapy depends greatly on the ability to increase intranuclear incorporation of the radiopharmaceutical without compromising toxicity. Several strategies to achieve this goal have been proposed in literature. The possibility of transferring tumor therapy based on the emission of Auger electrons from experimental models to patients has vast therapeutic potential, and remains a field of intense research.

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Authors and Affiliations

  1. Gray Institute For Radiation Oncology and Biology, Department of Oncology, Radiobiology Research Institute, Churchill Hospital, Headington, Oxford, OX3 7LJ, UK

    Nadia Falzone, Bart Cornelissen & Katherine A. Vallis

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  1. Nadia Falzone
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  2. Bart Cornelissen
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  3. Katherine A. Vallis
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Correspondence to Nadia Falzone .

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  1. , Consejo Superior de Investigaciones Cien, Instituto de Física Fundamental (IFF), Serrano 113-bis, Madrid, 28006, Spain

    Gustavo García Gómez-Tejedor

  2. Consejo Superior de Investigaciones Cien, Instituto de Física Fundamental (IFF), Serrano 113bis, Madrid, 28006, Spain

    Martina Christina Fuss

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Falzone, N., Cornelissen, B., Vallis, K.A. (2012). Auger Emitting Radiopharmaceuticals for Cancer Therapy. In: García Gómez-Tejedor, G., Fuss, M. (eds) Radiation Damage in Biomolecular Systems. Biological and Medical Physics, Biomedical Engineering. Springer, Dordrecht. https://doi.org/10.1007/978-94-007-2564-5_28

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