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Namespace Prefixes

PrefixIRI
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n15http://www.drugs.com/ppa/
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n5http://linked.opendata.cz/ontology/drugbank/
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n4http://linked.opendata.cz/resource/drugbank/drug/DB06210/identifier/national-drug-code-directory/

Statements

Subject Item
n2:DB06210
rdf:type
n5:Drug
n5:description
Eltrombopag is used to treat low blood platelet counts in adults with chronic immune (idiopathic) thrombocytopenia (ITP), when certain other medicines, or surgery to remove the spleen, have not worked well enough. ITP is a condition that may cause unusual bruising or bleeding due to an abnormally low number of platelets in the blood. Eltrombopag has also been recently approved (late 2012) for the treatment of thrombocytopenia (low blood platelet counts) in patients with chronic hepatitis C to allow them to initiate and maintain interferon-based therapy.
n5:dosage
n11:271B4A55-363D-11E5-9242-09173F13E4C5 n11:271B4A56-363D-11E5-9242-09173F13E4C5 n11:271B4A57-363D-11E5-9242-09173F13E4C5 n11:271B4A58-363D-11E5-9242-09173F13E4C5 n11:271B4A59-363D-11E5-9242-09173F13E4C5 n11:271B4A53-363D-11E5-9242-09173F13E4C5 n11:271B4A54-363D-11E5-9242-09173F13E4C5
n5:generalReferences
# http://www.gsk.com/media/press-releases/2012/FDA-approves-new-indication-for-PROMACTA-eltrombopag.html # Zekry A, Freiman J: Eltrombopag: Is this "24 karat gold platelet" treatment for thrombocytopenia in cirrhosis associated with hepatitis C? Hepatology. 2008 Apr;47(4):1418-21. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/18366111 # Mondelli MU: Eltrombopag: An effective remedy for thrombocytopaenia? J Hepatol. 2008 Jun;48(6):1030-2. Epub 2008 Mar 31. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/18433923 # Tarantino MD, Fogarty P, Mayer B, Vasey SY, Brainsky A: Efficacy of eltrombopag in management of bleeding symptoms associated with chronic immune thrombocytopenia. Blood Coagul Fibrinolysis. 2013 Apr;24(3):284-96. doi: 10.1097/MBC.0b013e32835fac99. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/ 23492914 # Kiang TK, Ensom MH, Chang TK: UDP-glucuronosyltransferases and clinical drug-drug interactions. Pharmacol Ther. 2005 Apr;106(1):97-132. Epub 2005 Jan 12. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15781124 # Deng Y, Madatian A, Wire MB, Bowen C, Park JW, Williams D, Peng B, Schubert E, Gorycki F, Levy M, Gorycki PD: Metabolism and disposition of eltrombopag, an oral, nonpeptide thrombopoietin receptor agonist, in healthy human subjects. Drug Metab Dispos. 2011 Sep;39(9):1734-46. doi: 10.1124/dmd.111.040170. Epub 2011 Jun 6. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/21646437 # Kuter DJ: The biology of thrombopoietin and thrombopoietin receptor agonists. Int J Hematol. 2013 Jul;98(1):10-23. doi: 10.1007/s12185-013-1382-0. Epub 2013 Jul 3. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/23821332
n5:group
approved
n5:halfLife
About 21-32 hours in healthy patients. About 26-35 hours in patients with idiopathic thrombocytopenic purpura.
n5:indication
Thrombopoietin receptor agonists are pharmaceutical agents that stimulate platelet production in the bone marrow. In this, they differ from the previously discussed agents that act by attempting to curtail platelet destruction.
owl:sameAs
n20:DB06210
dcterms:title
Eltrombopag
adms:identifier
n4:0007-4640-13 n16:DB06210 n17:Eltrombopag n18:D03978
n5:mechanismOfAction
Eltrombopag is an orally bioavailable, small-molecule TPO-receptor agonist that interacts with the transmembrane domain of the human TPO-receptor. Eltrombopag is a stimulator of STAT and JAK phosphorylation. Unlike recombinant TPO or romiplostim, Eltrombopag does not activate the AKT pathway in any way. It should be noted that when given to patients with aplastic anemia, other lineages besides platelet count were increased, suggesting that either eltrombopag enhanced the effect of TPO in vivo; or there is a yet uncovered mechanism of action at work.
n5:patent
n12:7547719 n12:6280959
n5:routeOfElimination
Eltrombopag is eliminated primarily via the feces (59%), along with 31% being renally excreted.
n5:synonym
Promacta Eltrombopagum Eltrombopag
n5:toxicity
Eltrombopag may cause hepatotoxicity, especially if administered in combination with interferon and ribavirin in patients with chronic hepatitis C (may increase the risk of hepatic decompensation).
n5:volumeOfDistribution
Based on a radiolabel study, the concentration of eltrombopag in blood cells is approximately 50% to 79% of plasma concentrations.
n9:hasAHFSCode
n14:20-16
n5:proteinBinding
Eltrombopag is highly protein bound (>99%).
n5:salt
n5:synthesisReference
http://doc.sciencenet.cn/upload/file/2011531154034454.pdf
foaf:page
n8:promacta-drug.htm n15:eltrombopag.html
n5:IUPAC-Name
n6:271B4A5E-363D-11E5-9242-09173F13E4C5
n5:InChI
n6:271B4A64-363D-11E5-9242-09173F13E4C5
n5:Molecular-Formula
n6:271B4A63-363D-11E5-9242-09173F13E4C5
n5:Molecular-Weight
n6:271B4A60-363D-11E5-9242-09173F13E4C5
n5:Monoisotopic-Weight
n6:271B4A61-363D-11E5-9242-09173F13E4C5
n5:SMILES
n6:271B4A62-363D-11E5-9242-09173F13E4C5
n5:Water-Solubility
n6:271B4A5C-363D-11E5-9242-09173F13E4C5 n6:271B4A74-363D-11E5-9242-09173F13E4C5
n5:logP
n6:271B4A5A-363D-11E5-9242-09173F13E4C5 n6:271B4A5D-363D-11E5-9242-09173F13E4C5
n5:logS
n6:271B4A5B-363D-11E5-9242-09173F13E4C5
n9:hasATCCode
n10:B02BX05
n5:H-Bond-Acceptor-Count
n6:271B4A6A-363D-11E5-9242-09173F13E4C5
n5:H-Bond-Donor-Count
n6:271B4A6B-363D-11E5-9242-09173F13E4C5
n5:InChIKey
n6:271B4A65-363D-11E5-9242-09173F13E4C5
n5:Polar-Surface-Area--PSA-
n6:271B4A66-363D-11E5-9242-09173F13E4C5
n5:Polarizability
n6:271B4A68-363D-11E5-9242-09173F13E4C5
n5:Refractivity
n6:271B4A67-363D-11E5-9242-09173F13E4C5
n5:Rotatable-Bond-Count
n6:271B4A69-363D-11E5-9242-09173F13E4C5
n5:absorption
Peak absorption of Eltrombopag occurs around 2-6 hours following oral administration, and the total oral absorption of drug-related material following a 75 mg dose was estimated to be at least 52%.
n5:affectedOrganism
Humans and other mammals
n5:casRegistryNumber
496775-61-2
n5:category
n5:Bioavailability
n6:271B4A70-363D-11E5-9242-09173F13E4C5
n5:Ghose-Filter
n6:271B4A72-363D-11E5-9242-09173F13E4C5
n5:MDDR-Like-Rule
n6:271B4A73-363D-11E5-9242-09173F13E4C5
n5:Number-of-Rings
n6:271B4A6F-363D-11E5-9242-09173F13E4C5
n5:Physiological-Charge
n6:271B4A6E-363D-11E5-9242-09173F13E4C5
n5:Rule-of-Five
n6:271B4A71-363D-11E5-9242-09173F13E4C5
n5:Traditional-IUPAC-Name
n6:271B4A5F-363D-11E5-9242-09173F13E4C5
n5:pKa--strongest-acidic-
n6:271B4A6C-363D-11E5-9242-09173F13E4C5
n5:pKa--strongest-basic-
n6:271B4A6D-363D-11E5-9242-09173F13E4C5