About: MACITENTAN     Goto   Sponge   NotDistinct   Permalink

An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz associated with source document(s)

AttributesValues
rdf:type
http://linked.open...gbank/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. (en)
http://linked.open...y/drugbank/dosage
http://linked.open...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. (en)
http://linked.open...gy/drugbank/group
  • approved (en)
http://linked.open...drugbank/halfLife
  • The half life of macitentan is 16 hours, and the half life of it's active metabolite is 48 hours. (en)
http://linked.open...ugbank/indication
  • Macitentan is indicated for patients with pulmonary arterial hypertension. (en)
sameAs
Title
  • MACITENTAN (en)
adms:identifier
http://linked.open...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. (en)
http://linked.open...outeOfElimination
  • Eliminated 50% through urine and 24% through feces. (en)
http://linked.open.../drugbank/synonym
  • ACT 064992 (en)
  • ACT-064992 (en)
  • ACT064992 (en)
  • Macitentanum (en)
  • OPSUMIT (en)
http://linked.open...drugbank/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. (en)
http://linked.open...umeOfDistribution
  • Macitentan has a volume of distribution of 50L. (en)
http://linked.open...k/foodInteraction
  • Can be taken with or without food. (en)
http://linked.open...nk/proteinBinding
  • Macitentan is >99% bound to plasma proteins, which are mainly albumin (en)
http://linked.open...ynthesisReference
  • 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 (en)
foaf:page
http://linked.open...ugbank/IUPAC-Name
http://linked.open...gy/drugbank/InChI
http://linked.open...Molecular-Formula
http://linked.open.../Molecular-Weight
http://linked.open...noisotopic-Weight
http://linked.open...y/drugbank/SMILES
http://linked.open.../Water-Solubility
http://linked.open...ogy/drugbank/logP
http://linked.open...ogy/drugbank/logS
http://linked.open...l/drug/hasATCCode
http://linked.open...nd-Acceptor-Count
http://linked.open...-Bond-Donor-Count
http://linked.open...drugbank/InChIKey
http://linked.open...urface-Area--PSA-
http://linked.open...nk/Polarizability
http://linked.open...bank/Refractivity
http://linked.open...atable-Bond-Count
http://linked.open...ugbank/absorption
  • Macitentan is administered orally, and it take about 8 hours for maximum plasma concentrations to be reached. (en)
http://linked.open.../affectedOrganism
  • Humans and other mammals (en)
http://linked.open...casRegistryNumber
  • 441798-33-0 (en)
http://linked.open...drugbank/category
  • (en)
http://linked.open...rugbank/clearance
  • Clearance data was not found. (en)
http://linked.open...k/Bioavailability
http://linked.open...bank/Ghose-Filter
http://linked.open...nk/MDDR-Like-Rule
http://linked.open...k/Number-of-Rings
http://linked.open...siological-Charge
http://linked.open...bank/Rule-of-Five
http://linked.open...tional-IUPAC-Name
http://linked.open...strongest-acidic-
http://linked.open...-strongest-basic-
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