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Namespace Prefixes

PrefixIRI
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n9http://linked.opendata.cz/resource/drugbank/drug/DB08913/identifier/drugbank/
n11http://www.drugs.com/
n6http://www.rxlist.com/
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n8http://linked.opendata.cz/resource/drugbank/drug/DB08913/identifier/wikipedia/

Statements

Subject Item
n2:DB08913
rdf:type
n3:Drug
n3:description
Radium Ra 223 Dichloride is a radiopharmaceutical containing the radioisotope radium-223 that emits short range but high linear energy alpha particles. As a cation, radium mimics calicum and binds to hydroxyapatite, which is a bone mineral found in areas of high bone turnover as seen in bone metastases. It was first approved by the FDA in May 2013 and is currently marketed under the brand name Xofigo, which was formerly called Alpharadin. Xofigo is indicated in patients who have metastatic bone cancer that is symptomatic with no visceral metastases and patients who have prostate cancer that is castration resistant. The FDA label includes a warning that Radium Ra 223 Dichloride should not be used in women who are pregnant or may become pregnant due to the high risk of fetal harm.
n3:dosage
n13:271B5CCA-363D-11E5-9242-09173F13E4C5
n3:generalReferences
# Suominen MI, Rissanen JP, Kakonen R, Fagerlund KM, Alhoniemi E, Mumberg D, Ziegelbauer K, Halleen JM, Kakonen SM, Scholz A: Survival benefit with radium-223 dichloride in a mouse model of breast cancer bone metastasis. J Natl Cancer Inst. 2013 Jun 19;105(12):908-16. doi: 10.1093/jnci/djt116. Epub 2013 May 16. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/23682134 # Nilsson S, Franzen L, Parker C, Tyrrell C, Blom R, Tennvall J, Lennernas B, Petersson U, Johannessen DC, Sokal M, Pigott K, Yachnin J, Garkavij M, Strang P, Harmenberg J, Bolstad B, Bruland OS: Bone-targeted radium-223 in symptomatic, hormone-refractory prostate cancer: a randomised, multicentre, placebo-controlled phase II study. Lancet Oncol. 2007 Jul;8(7):587-94. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17544845 # Bruland OS, Nilsson S, Fisher DR, Larsen RH: High-linear energy transfer irradiation targeted to skeletal metastases by the alpha-emitter 223Ra: adjuvant or alternative to conventional modalities? Clin Cancer Res. 2006 Oct 15;12(20 Pt 2):6250s-6257s. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17062709 # FDA label.
n3:group
investigational approved
n3:halfLife
The half-life is relatively long at 11.4 days for radium-223.
n3:indication
Used in patients who have metastatic bone cancer that is symptomatic with no visceral metastases and patients who have prostate cancer that is castration resistant.
owl:sameAs
n15:DB08913
dcterms:title
Radium Ra 223 Dichloride
adms:identifier
n8:Radium-223_chloride n9:DB08913 n10:50419-208-01
n3:mechanismOfAction
Radium Ra 223 Dichloride is the radioisotope radium-223 that emits short range but high linear energy alpha particles. As a cation, radium mimics calicum and binds to hydroxyapatite, which is a bone mineral found in areas of high bone turnover as seen in bone metastases. The high energy damages bone cells by introducing double-stranded DNA breaks. This leads to cell death and prevention of the spread of the bone cancer cells. As well because of the alpha particle's short range of less than 10 cell diameters, its damaging effects would less likely affect the non-cancerous cells nearby.
n3:routeOfElimination
Radium-223 is mainly eliminated through the feces (13%) and to a lesser extent in the urine (2%). It is also noted that the elimination rate of radium-223 from the intestines is variable due to the high variability of intestinal transit rates among patients. Therefore there could be more intestinal radiation exposure in patients with slower intestinal transit rates, but the significance of this in relation to toxicity is not known.
n3:synonym
Xofigo Radium-223 dichloride Radium-223 chloride
n3:toxicity
Because of its cytotoxic actions that have a high potential to cause fetal harm, Radium Ra 223 Dichloride is contraindicated in women who are pregnant or are of child bearing age. Other side effects include several hematological lab abnormalities, peripheral edema, nausea, vomiting, and diarrhea.
n3:volumeOfDistribution
The volume of distribution was not quantified, but after 24 hours, there is only 1% radium-223 remaining in the blood. The rest of the radium-223 is distributed to bone (61% of the radioactive dose after 4 hours) and intestine (49% of the radioactive dose after 4 hours). No other organs were found to have significant uptake.
n3:foodInteraction
Since radium Ra 223 dichloride is administered intravenously, no food effects should occur.
n3:proteinBinding
There is negligible plasma protein binding.
foaf:page
n6:xofigo-drug.htm n11:xofigo.html
n3:IUPAC-Name
n4:271B5CCF-363D-11E5-9242-09173F13E4C5
n3:InChI
n4:271B5CD5-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n4:271B5CD4-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n4:271B5CD1-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n4:271B5CD2-363D-11E5-9242-09173F13E4C5
n3:SMILES
n4:271B5CD3-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n4:271B5CCD-363D-11E5-9242-09173F13E4C5
n3:logP
n4:271B5CCB-363D-11E5-9242-09173F13E4C5 n4:271B5CCE-363D-11E5-9242-09173F13E4C5
n3:logS
n4:271B5CCC-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Acceptor-Count
n4:271B5CDB-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n4:271B5CDC-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n4:271B5CD6-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n4:271B5CD7-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n4:271B5CD9-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n4:271B5CD8-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n4:271B5CDA-363D-11E5-9242-09173F13E4C5
n3:absorption
Since Radium Ra 223 Dichloride is administered I.V., the bioavailability should be 100%.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
444811-40-9
n3:category
n3:clearance
The clearance rate of radium-223 was not quantified.
n3:Bioavailability
n4:271B5CDF-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n4:271B5CE1-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n4:271B5CE2-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n4:271B5CDE-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n4:271B5CDD-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n4:271B5CE0-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n4:271B5CD0-363D-11E5-9242-09173F13E4C5