Xofigo

The alpha-emitting radionuclide Ra-223 is used in nuclear medicine in form of the commercially available radiopharmaceutical "Xofigo". The direct progeny of Ra-223 is Rn-219, a noble gas with a half-life of approx. four seconds, that might be exhaled by patients treated with Ra-223. For assessing the exhalation of Rn-219, a radon monitor calibrated for this isotope is necessary. This work investigates on the response of the commercially available Alphaguard radon monitor to Rn-219 and proposes for the first time a factor for the calculation of the Rn-219-concentration in the instrument's measurement chamber from the instrument reading suitable for estimating patients exhalations...

The current mainstay of treatment in metastatic prostate cancer is based on hormonal manipulations. Standard androgen deprivation therapy and novel androgen axis drugs are commonly well tolerable and can stabilize metastatic hormone-sensitive prostate cancers for years. However, metastatic castration-resistant prostate cancer is still challenging to treat. Except taxanes, prostate cancer presents intrinsic resistance against conventional chemotherapies. The typically elderly patient population excludes more aggressive treatment regimens...

Background and O bjective : Radium-223 dichloride (Xofigo®) is a calcium mimetic agent approved for the treatment of castration-resistant prostate cancer patients with symptomatic bone metastases and no known visceral metastatic disease. This targeted, α-particle-emitting therapy has demonstrated significant survival benefit accompanied by a favorable safety profile. Nevertheless, recent evidence suggests that its combined use with abiraterone and prednisone/prednisolone may be associated with increased risk of death and fractures...

Radium-223 dichloride (223 Ra) is the first, recently approved, α-particle-emitting radiopharmaceutical for the treatment of patients with bone metastases in castration-resistant prostate cancer (CRPC) and no evidence of visceral metastases. We explored MEDLINE, relevant congresses, and websites for data on 223 Ra and prostate cancer therapies, focusing on therapeutic strategies and timing, bone metastases, and diagnostic assessment. 223 Ra represents the only bone-targeting agent that has significantly extended patients' overall survival while reducing pain and symptomatic skeletal events...

AIM: In this contribution we investigated the potential transfer of an established method for the synthesis of 223 Ra-labelled calixarene complexes to a hospital radiopharmaceutical environment. For this purpose, commercially available [223 Ra]RaCl2 solution in pharmaceutical grade (Xofigo® ) was reacted with three calixarene derivatives. METHODS: A wellestablished two-phase extraction method using a two-phase solvent system was performed for complexation of the radium ions with calixarenes under slightly basic conditions...

BACKGROUND: Radium-223 dichloride (Ra-223 Xofigo) has recently been approved as an addition to the host of available therapies in the USA as a treatment option for metastatic castrate-resistant prostate cancer (mCRPC) with bone metastases. This study describes our initial experience in patients treated with Ra-223 dichloride. It attempts to optimize patients' selection for the best outcome from Ra-223 dichloride therapy. METHODS: Consecutive patients who were referred for treatment with Ra-223 dichloride were prospectively followed...

PURPOSE: Radium-223 (Xofigo) is the first therapy with bone tropism for metastatic castrate-resistant prostate cancer (mCRPC) that has been shown to improve overall survival (OS). Although radium-223 has a positive effect on OS in men with mCRPC, there has been a paucity of reports from community practitioners, especially with regard to concurrent abiraterone and enzalutamide therapy. Significant differences in patient characteristics encountered may exist. PATIENTS AND METHODS: We conducted a retrospective study of men with mCRPC who received at least 1 cycle of radium-223 (n = 35)...

Alpha-emitters are radionuclides that decay through the emission of high linear energy transfer α-particles and possess favorable pharmacologic profiles for cancer treatment. When coupled with monoclonal antibodies, peptides, small molecules, or nanoparticles, the excellent cytotoxic capability of α-particle emissions has generated a strong interest in exploring targeted α-therapy in the pre-clinical setting and more recently in clinical trials in oncology. Multiple obstacles have been overcome by researchers and clinicians to accelerate the development of targeted α-therapies, especially with the recent improvement in isotope production and purification, but also with the development of innovative strategies for optimized targeting...

Radium Ra-223 dichloride (radium-223, Xofigo®) is a targeted alpha therapy approved for the treatment of castration-resistant prostate cancer (CRPC) with symptomatic bone metastases and no known visceral metastatic disease. Radium-223 is the first targeted alpha therapy in this indication providing a new treatment option, with evidence of a significant survival benefit, both in overall survival and in the time to the first symptomatic skeletal-related event. The skeleton is the most common metastatic site in patients with advanced prostate cancer...

Since November 2013, the alpha emitter radium-223 dichloride (Alpharadin/Xofigo®) has been approved for the treatment of men with castration-resistant prostate cancer (CRPC) with symptomatic bone metastases and no known visceral metastatic disease. In the ASYMPCA clinical trial, radium-223 was shown to improve overall survival and to reduce the time to the first symptomatic skeletal event. The use of radium-223 was associated with a reduction of pain and an improvement of health-related quality of life compared to the placebo arm...

Prostate cancer is the most common malignant disease in men. Several therapeutic agents have been approved during the last 10 years. Among them, radium-223 dichloride (Xofigo® ) is a radioactive isotope that induces irreversible DNA double-strand breaks and consequently tumor cell death. Radium-223 dichloride is a calcium-mimetic agent that specifically targets bone lesions. Radium-223 dichloride has been approved for the treatment of metastatic castration-resistant prostate cancer with symptomatic bone metastases, without known visceral metastases...

PURPOSE: Radium Ra 223 dichloride (radium-223, Xofigo®) is the first targeted alpha therapy for patients with castration-resistant prostate cancer and symptomatic bone metastases. Radium-223 provides a new treatment option for this setting, but also necessitates a new treatment management approach. We provide straightforward and practical recommendations for European nuclear medicine centres to optimize radium-223 service provision. METHODS: An independent research consultancy agency observed radium-223 procedures and conducted interviews with all key staff members involved in radium-223 treatment delivery in 11 nuclear medicine centres across six countries (Germany, Italy, the Netherlands, Spain, Switzerland and the UK) experienced in administering radium-223...

PURPOSE: Defining an optimal imaging modality for assessment of therapy and the best time of evaluation are pivotal for ideal patient's management. METHODS: 223 Ra (Xofigo®, formerly Alpharadin) has been approved by the FDA and European Medicines Agency for treatment of metastatic castration-resistant prostate cancer with painful osseous involvement. RESULTS: PET/CT imaging using various radiotracers such as 18 F-FDG, 18 F-FCH, 68 Ga-PSMA and 18 F-NaF have been investigated to mitigate the limitations of conventional imaging modalities...

Using tailor-made sub-mm dimension doped-silica fibres, thermoluminescent dosimetric studies have been performed for α-emitting sources of 223 RaCl2 (the basis of the Bayer Healthcare product Xofigo®). The use of 223 RaCl2 in the palliative treatment of bone metastases resulting from late-stage castration-resistant prostate cancer focuses on its favourable uptake in metabolically active bone metastases. Such treatment benefits from the high linear energy transfer (LET) and associated short path length (<100µm) of the α-particles emitted by 223 Ra and its decay progeny...

Purpose: Radium-223 dichloride (radium-223, Xofigo), a targeted alpha therapy, is currently used for the treatment of patients with castration-resistant prostate cancer (CRPC) with bone metastases. This study examines the mode-of-action and antitumor efficacy of radium-223 in two prostate cancer xenograft models. Experimental Design: Mice bearing intratibial LNCaP or LuCaP 58 tumors were randomized into groups ( n = 12-17) based on lesion grade and/or serum PSA level and administered radium-223 (300 kBq/kg) or vehicle, twice at 4-week intervals...

(223)Ra-dichloride was approved with the commercial name of Xofigo in 2014 for treatment of metastatic castration-resistant prostate cancer. (223)Ra is obtained by neutron irradiation of (226)Ra yielding (227)Ac, which decays to (227)Th and (223)Fr, both decaying to (223)Ra. Since (223)Ra is predominantly (95.3%) an alpha emitter with a 11.42days long half-life, the radiopharmaceutical, its remnants, the patient, and waste material can be managed and disposed with low radiation protection requirements. (227)Ac is a long-lived (T1/2=21...

Radium-223 dichloride (Xofigo®, Alpharadin) is approved for the treatment of metastatic castration-resistant prostate cancer with symptomatic bone metastases and no known visceral metastases. As a calcium mimetic, it is integrated into osteoplastic bone lesions and emits alpha particles with high energy which leads to local destruction of tumor cells. In the 2013 published ALSYMPCA trial, a significant advantage for overall survival and quality of life in comparison to placebo was found. Recent data suggest an increased potential in combination with next generation hormonal treatment...

Radium-223 dichloride (Xofigo®; 223Ra) is an alpha-emitting radiopharmaceutical FDA-approved for the treatment of bone metastases in patients with advanced castration-resistant prostate cancer. It is also being examined clinically in patients with breast and lung carcinoma and patients with multiple myeloma. As with other forms of radiation, the aim of 223Ra is to reduce tumor burden by directly killing tumor cells. External beam (photon) and proton radiation have been shown to augment tumor sensitivity to antigen-specific CD8+ cytotoxic T lymphocytes (CTLs)...

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...

A 66-year-old man with castration-resistant prostate carcinoma and multiple symptomatic bone mestastases was considered for Ra-dichloride (Xofigo) therapy. Staging with Ga-PSMA-PET/CT revealed additional extensive tumor involvement of the spine without relevant uptake in bone scintigraphy. Based on this imaging result, the patient was rescheduled for a PSMA-targeted therapy. Additional Ga-PSMA-PET/CT may have a considerable benefit for patients considered for Xofigo.