Abstract

Background and Purpose. Radium-223 dichloride (Xofigo®, Bayer HealthCare Pharmaceuticals Inc.) is the first α-particle emitter therapeutic agent approved by the FDA, with benefits in overall survival and delay in symptomatic skeletal event for patients with metastatic castrate-resistant prostate cancer (CRPC). Recent post hoc analyses of the phase III ALSYMPCA trial support the previously established safety profile as well as therapeutic effect and clinical outcome of Radium-223. Currently, Radium-223 is approved as a single agent therapy for metastatic CRPC. Clinical trials are currently investigating Radium-223 in additional clinical settings such as earlier asymptomatic disease and in combination with other agents including hormonal therapeutic agents and immunotherapeutic as well as chemotherapeutic agents. Trials are also ongoing in patients with other primary cancers such as breast cancer, thyroid cancer, and renal cancer metastatic to bone. In this article, the physics and radiobiology, as well as a literature update on the use of Radium-223, are provided along with case presentations, aiming at a better appreciation of research data as well as the assimilation of research data into clinical practice.

Highlights

  • Prostate cancer is the most common cancer in men in the United States and the third leading cause of cancer death among men after lung cancer and colon cancer

  • Trials are ongoing in patients with other primary cancers such as breast cancer, thyroid cancer, and renal cancer metastatic to bone

  • We summarize the physics and radiobiology of Radium-223 and provide a literature update on its use along with case presentations to facilitate at a better appreciation of research data as well as assimilation of research data into clinical practice

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Summary

Introduction

Prostate cancer is the most common cancer in men in the United States and the third leading cause of cancer death among men after lung cancer and colon cancer. Among bone-seeking radiopharmaceuticals, beta- (β-) emitting radionuclides such as Strontium-89 and Samarium-153 EDTMP have been used successfully for bone pain therapy in CRPC. In spite of their palliative benefit, these agents have not been found to have a positive impact on survival [6, 7]. A new bone-seeking radiopharmaceutical based on the alpha- (α-) particle emitter Radium-223 dichloride (Xofigo, Bayer HealthCare Pharmaceuticals Inc.) has shown promise in bone pain relief and in improving survival. Radium-223 received FDA approval in May 2013 following the phase III ALSYMPCA trial (ALpharadin in SYMptomatic Prostate CAncer), which was an international, multicenter, randomized, double-blind, placebo-controlled study of patients with symptomatic progressive CRPC who had previously received or were unfit for docetaxel chemotherapy [3]. We summarize the physics and radiobiology of Radium-223 and provide a literature update on its use along with case presentations to facilitate at a better appreciation of research data as well as assimilation of research data into clinical practice

Radium-223 Physics and Radiobiology
Pharmacokinetics
Safety
Clinical Trials
Clinical Indications
Case Series
Findings
Discussion
Conclusion
Full Text
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