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Namespace Prefixes

PrefixIRI
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dctermshttp://purl.org/dc/terms/
n18http://linked.opendata.cz/resource/AHFS/
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n14http://linked.opendata.cz/resource/drugbank/drug/DB06616/identifier/chebi/
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n11http://linked.opendata.cz/resource/drugbank/drug/DB06616/identifier/wikipedia/
n20http://www.rxlist.com/
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n7http://linked.opendata.cz/resource/drugbank/patent/
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xsdhhttp://www.w3.org/2001/XMLSchema#
n21http://linked.opendata.cz/resource/atc/
n17http://linked.opendata.cz/ontology/sukl/drug/

Statements

Subject Item
n2:DB06616
rdf:type
n3:Drug
n3:description
Bosutinib is a Bcr-Abl kinase inhibitor for the treatment of Philadelphia chromosome-positive (Ph+) chronic myelogenous leukemia (CML). Compared to other tyrosine kinase inhibitors, it has a more favourable hematologic toxicity profile. FDA approved on September 4, 2012.
n3:dosage
n19:271B4D63-363D-11E5-9242-09173F13E4C5 n19:271B4D64-363D-11E5-9242-09173F13E4C5 n19:271B4D65-363D-11E5-9242-09173F13E4C5 n19:271B4D66-363D-11E5-9242-09173F13E4C5
n3:generalReferences
# http://en.wikipedia.org/wiki/Philadelphia_chromosome # FDA label # Amsberg GK, Schafhausen P: Bosutinib in the management of chronic myelogenous leukemia. Biologics. 2013;7:115-22. doi: 10.2147/BTT.S30182. Epub 2013 May 6. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/23674887 # Keller-V Amsberg G, Brummendorf TH: Novel aspects of therapy with the dual Src and Abl kinase inhibitor bosutinib in chronic myeloid leukemia. Expert Rev Anticancer Ther. 2012 Sep;12(9):1121-7. doi: 10.1586/era.12.84. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/23098112
n3:group
approved
n3:halfLife
Terminal phase elimination half-life, single oral dose, fed-state = 22.5 hours
n3:indication
Treatment of chronic, accelerated, or blast phase Philadelphia chromosome-positive (Ph+) chronic myelogenous leukemia (CML) with resistance or intolerance to prior therapy in adult patients.
owl:sameAs
n6:DB06616
dcterms:title
Bosutinib
adms:identifier
n11:Bosutinib n12:D03252 n13:0069-0136-01 n14:39112 n15:DB06616
n3:mechanismOfAction
Bosutinib is a tyrosine kinase inhibitor. Although it is able to inhibit several tyrosine kinases such as Src, Lyn, and Hck, which are members of the Src-family of kinases, its primary target is the Bcr-Abl kinase. The Bcr-Abl gene is a chimeric oncogene created from the fusion of the breakpoint-cluster (Bcr) gene and Abelson (Abl) tyrosine gene. This chromosomal abnormality results in the formation of what is commonly known as the Philadelphia chromosome or Philadelphia translocation. The Bcr-Abl gene expresses a particular kinase that promotes the progression of CML. A decrease in the growth and size of the CML tumour has been observed following administration of bosutinib. Bosutinib did not inhibit the T315I and V299L mutant cells.
n3:patent
n7:7919625 n7:7767678 n7:7417148 n7:RE42376 n7:6002008
n3:routeOfElimination
When given a single oral dose, 91.3% of the dose was recovered in feces and 3% of the dose recovered in urine.
n3:synonym
4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methyl-1-piperazinyl)propoxy)-3-quinolinecarbonitrile Bosutinib Monohydrate Bosutinib SKI-606 Bosulif® SKI 606
n3:toxicity
Most common adverse reactions (incidence greater than 20%) are diarrhea, nausea, thrombocytopenia, vomiting, abdominal pain, rash, anemia, pyrexia, and fatigue. Because bosutinib is not an inhibitor of c-KIT or PDGF receptor, it has less hematologic toxicities.
n3:volumeOfDistribution
Apparent volume of distribution = 6080 ± 1230 L.
n17:hasAHFSCode
n18:10-00
n3:foodInteraction
When given with a high fat meal, the Cmax and AUC of bosutinib increased 1.8- and 1.7-fold, respectively.
n3:proteinBinding
94% bound to human plasma proteins in vitro. 96% bound to human plasma proteins in healthy subjects ex vivo. Extent of protein binding is not concentration-dependent.
foaf:page
n9:bosutinib.html n20:bosulif-drug.htm
n3:IUPAC-Name
n4:271B4D6B-363D-11E5-9242-09173F13E4C5
n3:InChI
n4:271B4D71-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n4:271B4D70-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n4:271B4D6D-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n4:271B4D6E-363D-11E5-9242-09173F13E4C5
n3:SMILES
n4:271B4D6F-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n4:271B4D69-363D-11E5-9242-09173F13E4C5
n3:logP
n4:271B4D67-363D-11E5-9242-09173F13E4C5 n4:271B4D6A-363D-11E5-9242-09173F13E4C5
n3:logS
n4:271B4D68-363D-11E5-9242-09173F13E4C5
n17:hasATCCode
n21:L01XE14
n3:H-Bond-Acceptor-Count
n4:271B4D77-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n4:271B4D78-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n4:271B4D72-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n4:271B4D73-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n4:271B4D75-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n4:271B4D74-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n4:271B4D76-363D-11E5-9242-09173F13E4C5
n3:absorption
Food increase the exposure of bosutinib. Tmax, single dose, cancer patients, fed-state = 4-6 hours; After 15 daily doses of bosutinib 500 mg with food in CML patients, the pharmacokinetic parameters are as follows: Cmax = 200 ng/mL; AUC = 3650 ng∙h/mL
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
380843-75-4
n3:clearance
Mean clearance (CL/F), single oral dose, fed-state = 189 L/h
n3:Bioavailability
n4:271B4D7D-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n4:271B4D7F-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n4:271B4D80-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n4:271B4D7C-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n4:271B4D7B-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n4:271B4D7E-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n4:271B4D6C-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n4:271B4D79-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n4:271B4D7A-363D-11E5-9242-09173F13E4C5