Features and benefits of 223-Ra radiopharmaceuticals for treatment of cancer

Janeva, Andonela and Smilkov, Katarina (2016) Features and benefits of 223-Ra radiopharmaceuticals for treatment of cancer. In: First International Students’ Symposium of Faculty of Medical Sciences “Celebrating achievements in medicine, promoting health and sharing knowledge”, 20 Apr 2016, Stip, Macedonia.

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Abstract

Important consideration in development of effective radiotherapy is the nature of the radiation emitted by the radionuclide. Radionuclides that decay by emitting α-particles offer the possibility of high controlled therapeutic modality that can be targeted to selected malignant cells. α-Particles present 4He nuclei, and are cytotoxic owing to their short path length (<100 μm) and high linear energy transfer (~100 keV/μm). In addition to their cytotoxicity, these features provide reduced toxic effect to the adjacent tissue, thus overcoming some limitations that are usually associated with conventional chemo- and radiotherapy. In addition, α-particle therapy offers the potential for more specific tumour cell killing with less damage to surrounding normal tissues than β-emitters, making this therapeutic modality ideal for elimination of minimal residual or micrometastatic disease. Radiopharmaceuticals with the α-emitter radium-223 have shown potential for treatment of different types of cancer. Its favourable radiobiological and radiochemical properties, with predominant alpha emission (α emission of 5,78MeV with 93.5%, and <4% β particles and <2% γ radiation) and t1/2=11,4 days, render this alpha-emitting radionuclide promising for targeted cancer therapy. Together with its short-living daughters, each 223Ra decay produces four α-particle emissions which enhance therapy effectiveness at cellular level. 223Ra localized onto the bone surfaces and/or in calcified tumors can, together with its daughter nuclides, deliver an intense and highly localized dose of α-particles with less bone marrow dose compared to currently used β-emitting and/or electron emitting radiopharmaceuticals. Skeletal diseases, e.g., primary or metastatic cancer to the bone may be treated with the 223Ra radiopharmaceuticals. Radium-223 was the first agent used in this class that increased the overall survival in castration-resistant prostate cancer (CRPC) patients with bone metastases. As such, it has recently been approved by the FDA in the form of 223RaCl2,for the treatment of patients with symptomatic bone metastases and no known visceral disease, since Phase III clinical trial in 922 patients showed significantly improved overall survival vs placebo (14.0 vs 11.2 months). Furthermore, a recent-date case report revealed success in treatment of osseous metastases in breast cancer. It is left to be seen whether the reported successful treatments will elicit further development of radiopharmaceuticals containing radium-223.

Item Type: Conference or Workshop Item (Speech)
Subjects: Medical and Health Sciences > Clinical medicine
Medical and Health Sciences > Health sciences
Medical and Health Sciences > Other medical sciences
Divisions: Faculty of Medical Science
Depositing User: Katarina Smilkov
Date Deposited: 30 Jan 2017 08:27
Last Modified: 30 Jan 2017 08:27
URI: http://eprints.ugd.edu.mk/id/eprint/17069

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