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drugbank:absorption Bioavailability is 100% following injection.
drugbank:affectedOrganism Humans and other mammals
drugbank:ahfsCode 20:12.04.12
drugbank:atcCode B01AE02
drugbank:biotransformation Lepirudin is thought to be metabolized by release of amino acids via catabolic hydrolysis of the parent drug. However, con-clusive data are not available. About 48% of the administration dose is excreted in the urine which consists of unchanged drug (35%) and other fragments of the parent drug.
drugbank:brandName Refludan (Berlex Labs)
drugbank:brandedDrug <http://wifo5-04.informatik.uni-mannheim.de/dailymed/resource/drugs/1681>
drugbank:casRegistryNumber <http://bio2rdf.org/cas:120993-53-5>
drugbank:chemicalFormula C287H440N80O110S6
drugbank:chemicalIupacName (4S)-4-[[(2S)-1-[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S)-1-[(2S,3R)-2-[[2-[[(2S)-2-[[2-[[(2S,3R)-2-[[(2S)-2-[[(2R)-2-[[(2S)-5-amino-2-[[(2S)-4-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S,3S)-2-[[(2R)-2-[[(2S)-6-amino-2-[[(2S)-4-amino-2-[[2-[[(2S)-5-amino-2-[[2-[[(2R)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[2-[[(2S)-2-[[(2R)-2-[[(2S)-2-[[(2R)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-5-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2R)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-amino-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxybutanoyl]amino]-4-hydroxy-4-oxobutanoyl]amino]-3-sulfanylpropanoyl]amino]-3-hydroxybutanoyl]amino]-5-hydroxy-5-oxopentanoyl]amino]-3-hydroxypropanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]-3-sulfanylpropanoyl]amino]-4-methylpentanoyl]amino]-3-sulfanylpropanoyl]amino]-5-hydroxy-5-oxopentanoyl]amino]acetyl]amino]-3-hydroxypropanoyl]amino]-4-oxobutanoyl]amino]-3-methylbutanoyl]amino]-3-sulfanylpropanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]acetyl]amino]-4-oxobutanoyl]amino]hexanoyl]amino]-3-sulfanylpropanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]-3-hydroxypropanoyl]amino]-4-hydroxy-4-oxobutanoyl]amino]acetyl]amino]-5-hydroxy-5-oxopentanoyl]amino]hexanoyl]amino]-4-oxobutanoyl]amino]-5-oxopentanoyl]amino]-3-sulfanylpropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxybutanoyl]amino]acetyl]amino]-5-hydroxy-5-oxopentanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoyl]amino]-3-hydroxypropanoyl]amino]-3-(3H-imidazol-4-yl)propanoyl]amino]-4-oxobutanoyl]amino]-4-hydroxy-4-oxobutanoyl]amino]acetyl]amino]-4-hydroxy-4-oxobutanoyl]amino]-3-cyclohexylpropanoyl]amino]-5-hydroxy-5-oxopentanoyl]amino]-5-hydroxy-5-oxopentanoyl]amino]-3-methylpentanoyl]pyrrolidine-2-carbonyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-hydroxy-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-hydroxy-1,5-dioxopentan-2-yl]amino]-5-oxopentanoic acid
drugbank:chemicalStructure >DB00001 sequence LVYTDCTESGQNLCLCEGSNVCGQGNKCILGSDGEKNQCVTGEGTPKPQSHNDGDFEEIP EEYLQ
drugbank:contraindicationInsert <http://129.128.185.122/drugbank2/drugs/DB00001/inserts/1430/full>
drugbank:creationDate 2005-06-13 13:24:05 UTC
drugbank:description Lepirudin is identical to natural hirudin except for substitution of leucine for isoleucine at the N-terminal end of the molecule and the absence of a sulfate group on the tyrosine at position 63. It is produced via yeast cells.
drugbank:dosageForm <http://wifo5-04.informatik.uni-mannheim.de/drugbank/resource/dosageforms/powderForSolutionIntravenous>
drugbank:dpdDrugIdNumber 02240996
drugbank:drugCategory <http://wifo5-04.informatik.uni-mannheim.de/drugbank/resource/drugcategory/anticoagulants>
drugbank:drugCategory <http://wifo5-04.informatik.uni-mannheim.de/drugbank/resource/drugcategory/antithromboticAgents>
drugbank:drugCategory <http://wifo5-04.informatik.uni-mannheim.de/drugbank/resource/drugcategory/fibrinolyticAgents>
drugbank:drugIdNumberPage <http://205.193.93.51/dpdonline/searchRequest.do?din=02240996>
drugbank:drugType <http://wifo5-04.informatik.uni-mannheim.de/drugbank/resource/drugtype/approved>
drugbank:drugType <http://wifo5-04.informatik.uni-mannheim.de/drugbank/resource/drugtype/biotech>
drugbank:experimentalLogpHydrophobicity -0.777
drugbank:fdaLabelFiles 1997-09-01 /drugs/1/fda_labels/402
drugbank:genericName Lepirudin
drugbank:halfLife Approximately 1.3 hours
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drugbank:inchiKey XYWBJDRHGNULKG-JWTJQKDBDD
drugbank:indication For the treatment of heparin-induced thrombocytopenia
drugbank:interactionInsert <http://129.128.185.122/drugbank2/drugs/DB00001/inserts/2428/full>
rdfs:label Lepirudin
drugbank:limsDrugId 1
drugbank:massSpecFile 0
drugbank:mechanismOfAction Lepirudin forms a stable non-covalent complex with alpha-thrombin, thereby abolishing its ability to cleave fibrinogen and initiate the clotting cascade.
drugbank:meltingPoint 65 oC (Otto, A. & Seckler, R. Eur. J. Biochem. 202:67-73 (1991))
drugbank:molecularWeightAverage 6963.425
drugbank:molecularWeightMono 6958.962
foaf:page <http://dbpedia.org/page/Lepirudin>
foaf:page <http://en.wikipedia.org/wiki/Lepirudin>
foaf:page <http://www.drugbank.ca/drugs/DB00001>
drugbank:patientInformationInsert http://129.128.185.122/drugbank2/drugs/DB00001/inserts/501/full
drugbank:pdbExperimentalId 5HIR
drugbank:pharmacology Lepirudin is used to break up clots and to reduce thrombocytopenia. It binds to thrombin and prevents thrombus or clot formation. It is a highly potent, selective, and essentially irreversible inhibitor of thrombin and clot-bond thrombin. Lepirudin requires no cofactor for its anticoagulant action.
drugbank:pharmgkbId PA450195
drugbank:pkaIsoelectricPoint 4.04
drugbank:possibleDiseaseTarget <http://wifo5-04.informatik.uni-mannheim.de/diseasome/resource/diseases/2210>
drugbank:possibleDiseaseTarget <http://wifo5-04.informatik.uni-mannheim.de/diseasome/resource/diseases/2695>
drugbank:possibleDiseaseTarget <http://wifo5-04.informatik.uni-mannheim.de/diseasome/resource/diseases/2760>
drugbank:possibleDiseaseTarget <http://wifo5-04.informatik.uni-mannheim.de/diseasome/resource/diseases/345>
drugbank:possibleDiseaseTarget <http://wifo5-04.informatik.uni-mannheim.de/diseasome/resource/diseases/560>
drugbank:possibleDiseaseTarget <http://wifo5-04.informatik.uni-mannheim.de/diseasome/resource/diseases/592>
drugbank:primaryAccessionNo DB00001
drugbank:pubchemCompoundId 16132441
drugbank:pubchemSubstanceId 14818038
drugbank:reference
drugbank:rxlistLink <http://www.rxlist.com/cgi/generic/lepirudin.htm>
owl:sameAs <http://data.linkedct.org/resource/intervention/18464>
owl:sameAs <http://data.linkedct.org/resource/intervention/8242>
owl:sameAs <http://dbpedia.org/resource/Lepirudin>
owl:sameAs <http://www.dbpedia.org/resource/Lepirudin>
drugbank:secondaryAccessionNumber biod00024
drugbank:secondaryAccessionNumber btd00024
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drugbank:state Liquid
drugbank:structure 1
drugbank:swissprotId <http://bio2rdf.org/uniprot:P01050>
drugbank:swissprotName ITH1_HIRME
drugbank:swissprotPage <http://www.uniprot.org/uniprot/P01050>
drugbank:synonym Hirudin variant-1
drugbank:target <http://wifo5-04.informatik.uni-mannheim.de/drugbank/resource/targets/54>
drugbank:toxicity In case of overdose (eg, suggested by excessively high aPTT values) the risk of bleeding is increased.
rdf:type drugbank:drugs
rdf:type vocabClass:Offer
drugbank:updateDate 2008-08-26 20:56:02 UTC