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Clinical Applications of Nuclear Medicine Targeted Therapy pp 345–364Cite as

Radiopharmaceuticals for Bone Metastases

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Abstract

Bone-seeking radiopharmaceuticals play a significant role in the treatment of metastatic pain as an alternative, or in addition, to classic palliative treatment.

Until a few years ago, radionuclides for the management of prostate cancer consisted of several beta-emitting agents, such as strontium (89Sr), phosphorus (32P) and samarium (153Sm) as well as rhenium (186Re and 188Re), which only exhibit a palliative effect in patients with extensive skeletal disease.

Radium (223Ra) dichloride represents a new generation of radiopharmaceuticals, being the first targeted alpha-emitting agent approved, which improves overall survival, postpones skeletal-related events (SREs) and controls bone pain.

Conjugates of bisphosphonates (BP) with macrocyclic chelators open new possibilities in bone-targeted radionuclide imaging and therapy, when labelled with positron and beta-emitting radiometals. [68Ga/177Lu]DOTAZOL appears to be the best leading compound showing fast blood clearance, low uptake in soft tissue and high accumulation in the skeleton.

Prostate-specific membrane antigen (PSMA) is an attractive target for diagnosis and therapy of prostate cancer. 177Lu-PSMA-617 is a new treatment option, which is not solely directed to bone metastases, but also demonstrates “antitumour” activity with limited and well-tolerated side effects.

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Authors and Affiliations

  1. Nuclear Medicine Unit, AOU Policlinico “G. Martino”, Messina, Italy

    Benedetta Pagano & Sergio Baldari

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  1. Benedetta Pagano
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  2. Sergio Baldari
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Correspondence to Benedetta Pagano .

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Editors and Affiliations

  1. Department of Nuclear Medicine, Humanitas Gavazzeni Hospital, Bergamo, Italy

    Emilio Bombardieri

  2. Nuclear Medicine Therapy and Endocrinology, Istituto Nazionale dei Tumori, Milano, Italy

    Ettore Seregni

  3. Nuclear Medicine and Molecular Imaging Unit, Veneto Institute of Oncology IOV - IRCCS, Padova, Italy

    Laura Evangelista

  4. Nuclear Medicine Division, Istituto Nazionale dei Tumori, Milano, Italy

    Carlo Chiesa

  5. Nuclear Medicine, Humanitas Research Hospital, Rozzano, Milano, Italy

    Arturo Chiti

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Pagano, B., Baldari, S. (2018). Radiopharmaceuticals for Bone Metastases. In: Bombardieri, E., Seregni, E., Evangelista, L., Chiesa, C., Chiti, A. (eds) Clinical Applications of Nuclear Medicine Targeted Therapy . Springer, Cham. https://doi.org/10.1007/978-3-319-63067-0_26

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