Abstract

Bone metastasis develops in multiple malignancies with a wide range of incidence. The presence of multiple bone metastases, leading to a multitude of complications and poorer prognosis. The corresponding refractory bone pain is still a challenging issue managed through multidisciplinary approaches to enhance the quality of life. Radiopharmaceuticals are mainly used in the latest courses of the disease. Bone-pain palliation with easy-to-administer radionuclides offers advantages, including simultaneous treatment of multiple metastatic foci, the repeatability and also the combination with other therapies. Several β¯- and α-emitters as well as pharmaceuticals, from the very first [89Sr]strontium-dichloride to recently introduced [223Ra]radium-dichloride, are investigated to identify an optimum agent. In addition, the combination of bone-seeking radiopharmaceuticals with chemotherapy or radiotherapy has been employed to enhance the outcome. Radiopharmaceuticals demonstrate an acceptable response rate in pain relief. Nevertheless, survival benefits have been documented in only a limited number of studies. In this review, we provide an overview of bone-seeking radiopharmaceuticals used for bone-pain palliation, their effectiveness and toxicity, as well as the results of the combination with other therapies. Bone-pain palliation with radiopharmaceuticals has been employed for eight decades. However, there are still new aspects yet to be established.

Highlights

  • Bone metastasis is a common feature of malignancies, in late stages [1,2]

  • Bone metastases are found using various imaging modalities, namely, plane radiography, computed tomography (CT) and magnetic resonance imaging (MRI), as well as functional examinations employing a wide range of targeted radioligands with single photon emission tomography (SPECT), positron emission tomography (PET) and hybrid SPECT/CT and PET/CT imaging [6,7]

  • We aimed to provide an overview of a number of long-established and novel bone-seeking radiopharmaceuticals used for bone-pain palliation, including [89Sr]strontium-dichloride, [153Sm]samarium, [186Re]rhenium, [188Re]rhenium, [177Lu]lutetium and [166Ho]holmium labeled with bone-seeking agents, as well as [223Ra]radium-dichloride

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Summary

Introduction

Bone metastasis is a common feature of malignancies, in late stages [1,2]. The presence of bone metastases implies poorer prognosis, shortens survival and is associated with a multitude of complications, including severe bone pain, pathological fracture, spinal cord compression, hypercalcemia, etc. Bone metastases are found using various imaging modalities, namely, plane radiography, computed tomography (CT) and magnetic resonance imaging (MRI), as well as functional examinations employing a wide range of targeted radioligands with single photon emission tomography (SPECT), positron emission tomography (PET) and hybrid SPECT/CT and PET/CT imaging [6,7]. One of the disabling presentations of bone metastases is refractory bone pain. Bone pain is managed through multidisciplinary approaches using analgesics, bisphosphonates, chemotherapy, external beam radiotherapy (EBRT), immunotherapy, surgery, hormonal treatments and bone-targeted radionuclide therapy [8,9,10]

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