In 2004, docetaxel was approved for the treatment of metastatic castration‑resistant prostate cancer (mCRPC). For the next several years, there was a lull in drug approvals. However, from 2010 onwards, 5 additional therapies have been approved on the basis of showing a survival benefit in phase III studies. These agents include sipuleucel‑T, cabazitaxel, abiraterone, enzalutamide and (most recently) radium‑223. Amongst radiopharmaceuticals currently used for advanced prostate cancer (e.g. samarium‑153 and strontium‑89), radium‑223 possesses several unique properties. As an alpha‑emitting compound, the agent produces a high‑energy output over a short range, facilitating selective destruction of tissue within the bone in the region of osteoblastic lesions while sparing surrounding normal tissue. The current review will outline biological rationale for radium‑223 and also provide an overview of preclinical and clinical development of the agent. Rational sequencing of radium‑223 and combinations, in the increasingly complex landscape of mCRPC will be discussed, along with factors influencing clinical implementation.

Keywords: alpharadin; bone metastases; metastatic castration‑resistant prostate cancer; radiopharmaceuticals; radium‑223; Xofigo 1Department of Medical Oncology and Experimental Therapeutics, City of Hope Comprehensive Cancer Center, Duarte, CA; 2Depart

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