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Radionuclide-based Diagnosis and Therapy of Prostate Cancer
Published in Michael Ljungberg, Handbook of Nuclear Medicine and Molecular Imaging for Physicists, 2022
Sven-Erik Strand, Mohamed Altai, Joanna Strand, David Ulmert
Radionuclide therapy with the α-emitting bone seeker 223Ra, initially intended for pain palliation, has shown some therapy efficacy. 223Ra-dichloride is accumulating in areas of increased bone turnover and due to the high LET causing cytotoxicity independent of absorbed dose rate, cell-cycle growth phase, and oxygen concentration. 223Ra localizes to areas of osteoblastic activity, and the hydroxyapatite crystal structure is thought to be the target for the 223Ra ions. These ions are taken up into bone by ionic exchange with the calcium ions. 223RaCl2 results in reduction of bone pain and overall survival advantage of 3.6 months in castration-resistant PCa patients with bone metastases. The use of 223Ra is limited to the treatment of bone metastases and not generalized metastasized PCa. The palliation/therapy activity is usually six cycles of 50 kBq/kg, given with 4 weeks intervals. The safety and efficacy of palliation with 223RaCl2 is associated with low myelosuppression rates and few adverse events. 223Ra (as chloride salt, Xofigo) has received marketing approval from the US Food and Drug Administration (FDA) and the European Medicines Agency (EMA) for the treatment of castration-resistant PCa (CRPC) with bone metastases in patients with symptomatic bone metastases and without known visceral disease. In Bieth and colleagues, a Figure 19 is shown, with 68Ga-PSMA PET images of a patient before and after 223RaCl2 radionuclide therapy. Bone lesions showing response to therapy, seen as decreasing PSMA expression, are clearly shown. However, also a few new lesions appear on late PET images [67]. In Figure 19.19 is shown whole body images of 223Ra uptake up to 6 days after injection [116].
Theranostic approaches in nuclear medicine: current status and future prospects
Published in Expert Review of Medical Devices, 2020
Luca Filippi, Agostino Chiaravalloti, Orazio Schillaci, Roberto Cianni, Oreste Bagni
As concerns the therapeutic aspects, it has to be pointed out that CRPC is an aggressive disease, with limited treatment options including chemotherapy, hormonal treatment with enzalutamide/abiraterone or the most recently introduced cellular therapy (sipuleucel-T). In case of patients with symptomatic bone metastases, the alpha-emitter radiopharmaceutical 223Radium-dichloride (Xofigo®) has been recently introduced in the clinical practice after the promising results obtained from the registrative clinical trial ALSYMPCA [62,63]. However, 223Radium-dichloride is not adequate for treating CRPC patients with visceral metastases, since its action is limited only to the skeletal lesions.