Alpha particles as radiopharmaceuticals in the treatment of bone metastases: mechanism of action of radium-223 chloride (Alpharadin) and radiation protection.
Approximately 85% to 90% of men with castration-resistant prostate cancer (CRPC) have radiological evidence of bone metastases. To date, however, therapies to manage bone metastases have been primarily palliative. Among CRPC patients with bone metastases, there is a significant unmet need for active antitumor treatment options that are highly efficacious and have a favorable safety profile. This article will present current information about alpha-pharmaceuticals, a new class of targeted cancer therapy for the treatment of patients with CRPC and bone metastases. It will review preclinical and clinical studies of the experimental radiopharmaceutical radium-223 chloride (Alpharadin), a first-in-class, highly targeted and well-tolerated alpha-pharmaceutical under development to improve survival in patients with bone metastases from advanced prostate cancer. Alpharadin kills cancer cells via alpha radiation from the decay of radium-223, a calcium mimetic that naturally self-targets to bone metastases. The mechanism of action of Alpharadin and specifics of administration, radiation protection, and patient management will be discussed.
Herbert Irving Comprehensive Cancer Center at Columbia University Medical Center, New York, New York 10032, USA.
Philippa J
PJ
Cheetham
Daniel P
DP
Petrylak
D000512:Alpha Particles / Q000627:therapeutic use*; D001859:Bone Neoplasms / Q000532:radiotherapy* / Q000556:secondary*; D002986:Clinical Trials as Topic; D006801:Humans; D008297:Male; D011471:Prostatic Neoplasms / Q000473:pathology*; D011835:Radiation Protection; D019275:Radiopharmaceuticals / Q000627:therapeutic use*; D011883:Radium / Q000494:pharmacology* / Q000627:therapeutic use
D019275:Radiopharmaceuticals; D011883:Radium