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Namespace Prefixes

PrefixIRI
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dctermshttp://purl.org/dc/terms/
foafhttp://xmlns.com/foaf/0.1/
n8http://linked.opendata.cz/resource/drugbank/drug/DB08932/identifier/wikipedia/
n5http://linked.opendata.cz/resource/drugbank/dosage/
n15http://www.rxlist.com/
n17http://bio2rdf.org/drugbank:
n18http://www.drugs.com/cons/
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n10http://linked.opendata.cz/resource/drugbank/drug/DB08932/identifier/kegg-drug/
n9http://linked.opendata.cz/resource/drugbank/drug/DB08932/identifier/drugbank/
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n7http://linked.opendata.cz/resource/drugbank/drug/DB08932/identifier/national-drug-code-directory/
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n12http://linked.opendata.cz/resource/atc/
n11http://linked.opendata.cz/ontology/sukl/drug/

Statements

Subject Item
n2:DB08932
rdf:type
n3:Drug
n3:description
Macitentan was approved in October 2013. It is indicated for patients with pulmonary arterial hypertension, and is marketed under the brand name Opsumit. Macitentan is an antagonist/blocker of endothelin receptors on blood vessels and smooth muscle, and, thus, blocks the stimulation of vasculature hypertrophy, inflammation, fibrosis, proliferation, and vasoconstriction. Similar to all drugs acting on the renin-angiotensin system, macitentan is associated with embryo and fetal toxicity, so it should not be used in pregnancy and has special precautions that must be followed for all females of child-bearing age.
n3:dosage
n5:271B5DB7-363D-11E5-9242-09173F13E4C5 n5:271B5DB8-363D-11E5-9242-09173F13E4C5
n3:generalReferences
# Bolli MH, Boss C, Binkert C, Buchmann S, Bur D, Hess P, Iglarz M, Meyer S, Rein J, Rey M, Treiber A, Clozel M, Fischli W, Weller T: The discovery of N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-p ropylsulfamide (Macitentan), an orally active, potent dual endothelin receptor antagonist. J Med Chem. 2012 Sep 13;55(17):7849-61. doi: 10.1021/jm3009103. Epub 2012 Aug 16. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/22862294 # FDA label. # Lexicomp.
n3:group
approved
n3:halfLife
The half life of macitentan is 16 hours, and the half life of it's active metabolite is 48 hours.
n3:indication
Macitentan is indicated for patients with pulmonary arterial hypertension.
owl:sameAs
n17:DB08932
dcterms:title
MACITENTAN
adms:identifier
n7:66215-501-30 n8:Macitentan n9:DB08932 n10:D10135
n3:mechanismOfAction
Macitentan is an antagonist/blocker of endothelin receptors. Endothelin receptors are found in the endothelial cells of blood vessels and smooth muscle. Macitentan binds to the receptors, endothelin A and B (ETA and ETB), which prevents the agonist endothelin -1 (ET-1) from binding and stimulating the ETA and ETB receptors.
n3:routeOfElimination
Eliminated 50% through urine and 24% through feces.
n3:synonym
OPSUMIT ACT-064992 ACT 064992 ACT064992 Macitentanum
n3:toxicity
Macitentan has a black box warning of embryo-fetal toxicity. Special precautions must be taken for all females of child-bearing age, and women who are pregnant must not be given macitentan.
n3:volumeOfDistribution
Macitentan has a volume of distribution of 50L.
n3:foodInteraction
Can be taken with or without food.
n3:proteinBinding
Macitentan is >99% bound to plasma proteins, which are mainly albumin
n3:synthesisReference
Bolli MH, Boss C, Binkert C, Buchmann S, Bur D, Hess P, Iglarz M, Meyer S, Rein J, Rey M, Treiber A, Clozel M, Fischli W, Weller T: The discovery of N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-p ropylsulfamide (Macitentan), an orally active, potent dual endothelin receptor antagonist. J Med Chem. 2012 Sep 13;55(17):7849-61. doi: 10.1021/jm3009103. Epub 2012 Aug 16. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/22862294
foaf:page
n15:opsumit-drug.htm n18:macitentan.html
n3:IUPAC-Name
n4:271B5DBD-363D-11E5-9242-09173F13E4C5
n3:InChI
n4:271B5DC3-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n4:271B5DC2-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n4:271B5DBF-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n4:271B5DC0-363D-11E5-9242-09173F13E4C5
n3:SMILES
n4:271B5DC1-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n4:271B5DBB-363D-11E5-9242-09173F13E4C5 n4:271B5DD3-363D-11E5-9242-09173F13E4C5
n3:logP
n4:271B5DB9-363D-11E5-9242-09173F13E4C5 n4:271B5DBC-363D-11E5-9242-09173F13E4C5
n3:logS
n4:271B5DBA-363D-11E5-9242-09173F13E4C5
n11:hasATCCode
n12:C02KX04
n3:H-Bond-Acceptor-Count
n4:271B5DC9-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n4:271B5DCA-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n4:271B5DC4-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n4:271B5DC5-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n4:271B5DC7-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n4:271B5DC6-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n4:271B5DC8-363D-11E5-9242-09173F13E4C5
n3:absorption
Macitentan is administered orally, and it take about 8 hours for maximum plasma concentrations to be reached.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
441798-33-0
n3:category
n3:clearance
Clearance data was not found.
n3:Bioavailability
n4:271B5DCF-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n4:271B5DD1-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n4:271B5DD2-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n4:271B5DCE-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n4:271B5DCD-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n4:271B5DD0-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n4:271B5DBE-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n4:271B5DCB-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n4:271B5DCC-363D-11E5-9242-09173F13E4C5