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Namespace Prefixes

PrefixIRI
n17http://linked.opendata.cz/resource/drugbank/drug/DB08899/identifier/chebi/
n2http://linked.opendata.cz/resource/drugbank/drug/
dctermshttp://purl.org/dc/terms/
n12http://linked.opendata.cz/resource/AHFS/
n14http://linked.opendata.cz/resource/drugbank/drug/DB08899/identifier/wikipedia/
foafhttp://xmlns.com/foaf/0.1/
n20http://linked.opendata.cz/resource/drugbank/dosage/
n7http://www.rxlist.com/
n9http://bio2rdf.org/drugbank:
admshttp://www.w3.org/ns/adms#
n15http://linked.opendata.cz/resource/drugbank/drug/DB08899/identifier/kegg-drug/
n18http://linked.opendata.cz/resource/drugbank/drug/DB08899/identifier/drugbank/
n5http://linked.opendata.cz/resource/drugbank/patent/
rdfhttp://www.w3.org/1999/02/22-rdf-syntax-ns#
n16http://linked.opendata.cz/resource/drugbank/drug/DB08899/identifier/national-drug-code-directory/
owlhttp://www.w3.org/2002/07/owl#
n3http://linked.opendata.cz/ontology/drugbank/
n19http://www.drugs.com/cdi/
n4http://linked.opendata.cz/resource/drugbank/property/
xsdhhttp://www.w3.org/2001/XMLSchema#
n21http://linked.opendata.cz/resource/atc/
n11http://linked.opendata.cz/ontology/sukl/drug/

Statements

Subject Item
n2:DB08899
rdf:type
n3:Drug
n3:description
Enzalutamide is an androgen receptor inhibitor for the treatment of castration-resistant prostate cancer. FDA approved on August 31, 2012.
n3:dosage
n20:271B5B7C-363D-11E5-9242-09173F13E4C5
n3:generalReferences
# Nadiminty N, Tummala R, Liu C, Yang J, Lou W, Evans CP, Gao AC: NF-kappaB2/p52 induces resistance to Enzalutamide in Prostate Cancer: Role of androgen receptor and its variants. Mol Cancer Ther. 2013 May 22. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/23699654
n3:group
approved
n3:halfLife
The mean terminal half-life (t1/2) for enzalutamide in patients after a single oral dose is 5.8 days (range 2.8 to 10.2 days). Following a single 160 mg oral dose of enzalutamide in healthy volunteers, the mean terminal t1/2 for N-desmethyl enzalutamide is approximately 7.8 to 8.6 days.
n3:indication
Enzalutamide is indicated for the treatment of patients with metastatic castration-resistant prostate cancer who have previously received docetaxel.
owl:sameAs
n9:DB08899
dcterms:title
Enzalutamide
adms:identifier
n14:Enzalutamide n15:D10218 n16:0469-0125-99 n17:68534 n18:DB08899
n3:mechanismOfAction
Enzalutamide is a competitive androgen receptor inhibitor that effects multiple stages of the signalling pathway. It is able to inhibit androgen binding to its receptor, androgen receptor nuclear translocation, and subsequent interaction with DNA. As a result, proliferation of prostate cancer cells decreases which ultimately leads to apoptosis and decreased tumour volume.
n3:patent
n5:8183274 n5:7709517
n3:routeOfElimination
Enzalutamide is primarily eliminated by hepatic metabolism. 71% of the dose is recovered in urine (including only trace amounts of enzalutamide and N-desmethyl enzalutamide), and 14% is recovered in feces (0.4% of dose as unchanged enzalutamide and 1% as N-desmethyl enzalutamide).
n3:synonym
XTANDI MDV 3100 MDV3100 MDV-3100
n3:toxicity
The most common adverse reactions (≥ 5%) are asthenia/fatigue, back pain, diarrhea, arthralgia, hot flush, peripheral edema, musculoskeletal pain, headache, upper respiratory infection, muscular weakness, dizziness, insomnia, lower respiratory infection, spinal cord compression and cauda equina syndrome, hematuria, paresthesia, anxiety, and hypertension.
n3:volumeOfDistribution
Apparent volume of distribution (Vd/F), single oral dose = 110 L
n11:hasAHFSCode
n12:10-00
n3:proteinBinding
Enzalutamide is 97% to 98% bound to plasma proteins, primarily albumin. N-desmethyl enzalutamide is 95% bound to plasma proteins.
foaf:page
n7:xtandi-drug.htm n19:enzalutamide.html
n3:IUPAC-Name
n4:271B5B81-363D-11E5-9242-09173F13E4C5
n3:InChI
n4:271B5B87-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n4:271B5B86-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n4:271B5B83-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n4:271B5B84-363D-11E5-9242-09173F13E4C5
n3:SMILES
n4:271B5B85-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n4:271B5B7F-363D-11E5-9242-09173F13E4C5 n4:271B5B97-363D-11E5-9242-09173F13E4C5
n3:logP
n4:271B5B7D-363D-11E5-9242-09173F13E4C5 n4:271B5B80-363D-11E5-9242-09173F13E4C5
n3:logS
n4:271B5B7E-363D-11E5-9242-09173F13E4C5
n11:hasATCCode
n21:L02BB04
n3:H-Bond-Acceptor-Count
n4:271B5B8D-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n4:271B5B8E-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n4:271B5B88-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n4:271B5B89-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n4:271B5B8B-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n4:271B5B8A-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n4:271B5B8C-363D-11E5-9242-09173F13E4C5
n3:absorption
The pharmacokinetic profile of enzalutamide and N-desmethyl enzalutamide (its major active metabolite) is described by a linear two-compartment model with first-order absorption. Enzalutamide also accumulates. Food does not affect its absorption. Tmax, prostate cancer patients = 1 hour (range of 0.5-3 hours); Cmax, steady state, enzalutamide = 16.6 μg/mL; Cmax, steady state, N-desmethyl enzalutamide = 12.7 μg/mL; Time to steady state, daily dosing = 28 days;
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
915087-33-1
n3:category
n3:clearance
Apparent clearance (CL/F), single oral dose = 0.56 L/h (range of 0.33 - 1.02 L/h)
n3:Bioavailability
n4:271B5B93-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n4:271B5B95-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n4:271B5B96-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n4:271B5B92-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n4:271B5B91-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n4:271B5B94-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n4:271B5B82-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n4:271B5B8F-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n4:271B5B90-363D-11E5-9242-09173F13E4C5