10/6/2016 DrugBank:Rosiglitazone

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Identification

Name Rosiglitazone

AccessionNumber DB00412(APRD00403)

Type SmallMolecule

Groups Approved,Investigational

Description Rosiglitazoneisanantidiabeticdruginthethiazolidinedioneclassofdrugs.ItismarketedbythepharmaceuticalcompanyGlaxoSmithKlineasastandalon
(Avandia)andincombinationwithmetformin(Avandamet)orwithglimepiride(Avandaryl).Likeotherthiazolidinediones,themechanismofactionofrosiglita
byactivationoftheintracellularreceptorclassoftheperoxisomeproliferatoractivatedreceptors(PPARs),specificallyPPAR.Rosiglitazoneisaselectiveliga
PPAR,andhasnoPPARbindingaction.Apartfromitseffectoninsulinresistance,itappearstohaveanantiinflammatoryeffect:nuclearfactorkappaB(
levelsfallandinhibitor(IB)levelsincreaseinpatientsonrosiglitazone.Recentresearchhassuggestedthatrosiglitazonemayalsobeofbenefittoasubset
patientswithAlzheimer'sdiseasenotexpressingtheApoE4allele.Thisisthesubjectofaclinicaltrialcurrentlyunderway.

Structure

CH

(http://moldb.wishartlab.com/molecules/DB00412/image.svg)
3

NH
N N S
O
O

MOL(/structures/structures/small_molecule_drugs/DB00412.mol) SDF(/structures/structures/small_molecule_drugs/DB00412.sdf)

3DSDF(/structures/structures/small_molecule_drugs/DB00412.sdf?dim=3d) PDB(/structures/structures/small_molecule_drugs/DB00412.pdb)

SMILES(/structures/structures/small_molecule_drugs/DB00412.smiles) InChI(/structures/structures/small_molecule_drugs/DB00412.inchi)

View3DStructure(/structures/structures/small_molecule_drugs/DB00412)

Synonyms ()5[p[2(methyl2pyridylamino)ethoxy]benzyl]2,4thiazolidinedione

(RS)5{4[2(Methyl2pyridylamino)ethoxy]benzyl}2,4thiazolidinedion

Rosiglitazon

Rosiglitazona

Rosiglitazone

Rosiglitazonum

ExternalIdentifiers BRL49653C

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10/6/2016 DrugBank:Rosiglitazone

Approved
Show 10 entries
Prescription
Search
Products
Name Dosage Strength Route Labeller MarketingStart MarketingEnd

Avandia tablet,filmcoated 2mg/1 oral PhysiciansTotalCare,Inc. 20050513 Notapplicable

Avandia tablet,filmcoated 2mg/1 oral GlaxoSmithKlineLlc 20110525 Notapplicable

Avandia tablet 4mg oral GlaxosmithklineInc 20000321 Notapplicable

Avandia tablet,filmcoated 4mg/1 oral CardinalHealth 19990529 Notapplicable

Avandia tablet,filmcoated 8mg/1 oral GlaxoSmithKlineLlc 20110525 20160403

Avandia tablet 8mg oral GlaxosmithklineInc 20000321 Notapplicable

Avandia tablet,filmcoated 4mg/1 oral PhysiciansTotalCare,Inc. 20060207 Notapplicable

Avandia tablet,filmcoated 8mg/1 oral CardinalHealth 19990528 Notapplicable

Avandia tablet,filmcoated 8mg/1 oral PhysiciansTotalCare,Inc. 20010509 Notapplicable

Avandia tablet 2mg oral GlaxosmithklineInc 20000321 Notapplicable

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ApprovedGeneric
Show 10 entries
Prescription
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Products
Name Dosage Strength Route Labeller MarketingStart MarketingEnd

Apo tablet 2.0mg oral ApotexInc Notapplicable Notapplicable

rosiglitazone

Apo tablet 4.0mg oral ApotexInc Notapplicable Notapplicable

rosiglitazone

Apo tablet 8.0mg oral ApotexInc Notapplicable Notapplicable

rosiglitazone

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ApprovedOverthe NotAvailable
CounterProducts

Unapproved/Other
Show 10 entries
Products
Search

Name Dosage Strength Route Labeller MarketingStart MarketingEnd

Avandia Filmcoatedtablet 4mg Oraluse SmithKlineBeechamPlc 20000711 Notapplicable

Avandia Filmcoatedtablet 2mg Oraluse SmithKlineBeechamPlc 20000711 Notapplicable

Avandia Filmcoatedtablet 4mg Oraluse SmithKlineBeechamPlc 20000711 Notapplicable

Avandia Filmcoatedtablet 2mg Oraluse SmithKlineBeechamPlc 20000711 Notapplicable

Avandia Filmcoatedtablet 4mg Oraluse SmithKlineBeechamPlc 20000711 Notapplicable

Avandia Filmcoatedtablet 8mg Oraluse SmithKlineBeechamPlc 20000711 Notapplicable

Avandia Filmcoatedtablet 8mg Oraluse SmithKlineBeechamPlc 20000711 Notapplicable

Avandia Filmcoatedtablet 2mg Oraluse SmithKlineBeechamPlc 20000711 Notapplicable

Avandia Filmcoatedtablet 4mg Oraluse SmithKlineBeechamPlc 20000711 Notapplicable

Avandia Filmcoatedtablet 4mg Oraluse SmithKlineBeechamPlc 20000711 Notapplicable

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10/6/2016 DrugBank:Rosiglitazone

International Name/CAS Structure Properties

Show 10 entries
Brands
Search

Name Company

Blutab Werrick

DHRosidia Hasan

Diaben Elea

Diaglinex Farmindustria

Gaudil Craveri
Identification Taxonomy Pharmacology
Gliximina ADMET Pharmacoeconomics
Denver Properties Spectra References Interactions Targets(2) Enzymes(7) Carriers(1)

Transporters(1) 0Comments
Naidi Hisun

Rogelin Torrent

Roglit GedeonRichter

Romerol DrugInternational

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Brandmixtures
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Search

Name Labeller Ingredients

Avaglim SmithKlineBeechamLtd Glimepiride(/drugs/DB00222) / Rosiglitazone

Avandamet GlaxoSmithKlineLlc Metformin(/drugs/DB00331) / Rosiglitazone

Avandaryl GlaxoSmithKlineLlc Glimepiride(/drugs/DB00222) / Rosiglitazone

PMSrosiglitazonemetformin PharmascienceInc Metformin(/drugs/DB00331) / Rosiglitazone

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Salts Name/CAS Structure Properties

RosiglitazoneMaleate InChIKey: DBSALT000153(/salts/DBSALT0

(/salts/DBSALT000153) SUFUKZSWUHZXAV
155141290 BTJKTKAUNAN
MonoisotopicMass:
473.125670795
AverageMass:
473.499
(http://moldb.wishartlab.com/molecules/DBSALT000153/image.png)

Categories AlimentaryTractandMetabolism(/categories/DBCAT002118)
BloodGlucoseLoweringAgents(/categories/DBCAT002698)
BloodGlucoseLoweringDrugs,Excl.Insulins(/categories/DBCAT002199)
ChemicalActionsandUses(/categories/DBCAT000006)
CytochromeP450CYP1A2Inhibitors(/categories/DBCAT000402)
CytochromeP450CYP2A6Inhibitors(/categories/DBCAT002614)
CytochromeP450CYP2C19Inhibitors(/categories/DBCAT000403)
CytochromeP450CYP2C8Inhibitors(/categories/DBCAT000868)
CytochromeP450CYP2C8Inhibitors(moderate)(/categories/DBCAT002644)
CytochromeP450CYP2C8Substrates(/categories/DBCAT002642)
CytochromeP450CYP2C9Inhibitors(/categories/DBCAT000489)
CytochromeP450CYP2C9Substrates(/categories/DBCAT002634)
CytochromeP450CYP2D6Inhibitors(/categories/DBCAT000911)
DrugsUsedinDiabetes(/categories/DBCAT002117)
FibrinolyticAgents(/categories/DBCAT000013)
HypoglycemicAgents(/categories/DBCAT000137)
PharmacologicActions(/categories/DBCAT000005)
PhysiologicalEffectsofDrugs(/categories/DBCAT000039)
PPARgamma(/categories/DBCAT000837)
Thiazolidinediones(/categories/DBCAT002198)
VasodilatorAgents(/categories/DBCAT000516)

UNII 05V02F2KDG(http://fdasis.nlm.nih.gov/srs/srsdirect.jsp?regno=05V02F2KDG)

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10/6/2016 DrugBank:Rosiglitazone

CASnumber 122320734

Weight Average:357.427
Monoisotopic:357.114712179

ChemicalFormula C18H19N3O3S

InChIKey InChIKey=YASAKCUCGLMORWUHFFFAOYNAN

InChI InChI=1/C18H19N3O3S/c121(1642391916)101124147513(6814)121517(22)2018(23)2515/h29,15H,1012H2,1H3,(H,20,22,23)

IUPACName 5[(4{2[methyl(pyridin2yl)amino]ethoxy}phenyl)methyl]1,3thiazolidine2,4dione

SMILES CN(CCOC1=CC=C(CC2SC(=O)NC2=O)C=C1)C1=CC=CC=N1
Identification
Taxonomy Taxonomy Pharmacology ADMET Pharmacoeconomics Properties Spectra References Interactions Targets(2) Enzymes(7) Carriers(1)

Transporters(1)
Description 0Comments
Thiscompoundbelongstotheclassoforganiccompoundsknownasphenolethers.Thesearearomaticcompoundscontaininganethergroupsubstitutedw
benzenering.

Kingdom Organiccompounds(http://classyfire.wishartlab.com/tax_nodes/C0000000)

SuperClass Benzenoids(http://classyfire.wishartlab.com/tax_nodes/C0002448)

Class Benzeneandsubstitutedderivatives(http://classyfire.wishartlab.com/tax_nodes/C0002279)

SubClass Phenolethers(http://classyfire.wishartlab.com/tax_nodes/C0002341)

DirectParent Phenolethers(http://classyfire.wishartlab.com/tax_nodes/C0002341)

AlternativeParents Dialkylarylamines(http://classyfire.wishartlab.com/tax_nodes/C0003901)
Thiazolidinediones(http://classyfire.wishartlab.com/tax_nodes/C0000228)
Aminopyridinesandderivatives(http://classyfire.wishartlab.com/tax_nodes/C0000283)
Alkylarylethers(http://classyfire.wishartlab.com/tax_nodes/C0000128)
Imidolactams(http://classyfire.wishartlab.com/tax_nodes/C0003886)
Heteroaromaticcompounds(http://classyfire.wishartlab.com/tax_nodes/C0004144)
Thioethers(http://classyfire.wishartlab.com/tax_nodes/C0001202)
Carboxylicacidamides(http://classyfire.wishartlab.com/tax_nodes/C0000475)
Azacycliccompounds(http://classyfire.wishartlab.com/tax_nodes/C0004139)
Hydrocarbonderivatives(http://classyfire.wishartlab.com/tax_nodes/C0004150)
Carbonylcompounds(http://classyfire.wishartlab.com/tax_nodes/C0001831)

Substituents Dialkylarylamine
Phenolether
Thiazolidinedione
Aminopyridine
Alkylarylether
Imidolactam
Pyridine
Heteroaromaticcompound
Thiazolidine
Tertiaryamine
Carboxamidegroup
Azacycle
Organoheterocycliccompound
Thioether
Ether
Carboxylicacidderivative
Hydrocarbonderivative
Organooxygencompound
Organonitrogencompound
Carbonylgroup
Amine
Aromaticheteromonocycliccompound

Molecular Aromaticheteromonocycliccompounds
Framework

External NotAvailable
Descriptors

Pharmacology

Indication Rosiglitazoneisindicatedasanadjuncttodietandexercisetoimproveglycemiccontrolinadultswithtype2diabetesmellitus.

Pharmacodynamics Whenrosiglitazoneisusedasmonotherapy,itisassociatedwithincreasesintotalcholesterol,LDL,andHDL.Itisalsoassociatedwithdecreasesinfreefat
IncreasesinLDLoccurredprimarilyduringthefirst1to2monthsoftherapywithAVANDIAandLDLlevelsremainedelevatedabovebaselinethroughoutthe
Incontrast,HDLcontinuedtoriseovertime.Asaresult,theLDL/HDLratiopeakedafter2monthsoftherapyandthenappearedtodecreaseovertime.

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10/6/2016 DrugBank:Rosiglitazone

Mechanismof Rosiglitazoneactsasahighlyselectiveandpotentagonistatperoxisomeproliferatoractivatedreceptors(PPAR)intargettissuesforinsulinactionsuchasa
action tissue,skeletalmuscle,andliver.ActivationofPPARgammareceptorsregulatesthetranscriptionofinsulinresponsivegenesinvolvedinthecontrolofgluco
production,transport,andutilization.Inthisway,rosiglitazoneenhancestissuesensitivitytoinsulin.

RelatedArticles GlitazonesforTreatmentofLipodystrophy? PPARGammaandMetabolism:InsightsFromtheStudyofHumanGeneticVa

GraemeJ.Moyle,MD,MBBS,Medscape,2001 MarkGurnell,Medscape,2003

LossofPPARFunctionAssociatedWithInsulinResistance AnARBtoHelpTreatType2Diabetes?
AnnM.Contijoch,PhD,Medscape,2000 JennyA.VanAmburgh,PharmD,CDE,Medscape,2010

HowDoesPioglitazoneCompareWithRosiglitazone?
WilliamC.Gong,PharmD,Medscape,2011

Identification Taxonomy Pharmacology ADMET Pharmacoeconomics Properties Spectra References Interactions Targets(2) Enzymes(7) Carriers(1)

Transporters(1) 0Comments Poweredby

Absorption Theabsolutebioavailabilityofrosiglitazoneis99%.Peakplasmaconcentrationsareobservedabout1hourafterdosing.Administrationofrosiglitazonewith
resultedinnochangeinoverallexposure(AUC),buttherewasanapproximately28%decreaseinCmaxandadelayinT max(1.75hours).Thesechangesar
likelytobeclinicallysignificanttherefore,rosiglitazonemaybeadministeredwithorwithoutfood.Maximumplasmaconcentration(Cmax)andtheareaunde
curve(AUC)ofrosiglitazoneincreaseinadoseproportionalmanneroverthetherapeuticdoserange.

Volumeof 17.6L[oralvolumeofdistributionVss/F]
distribution 13.5L[populationmean,pediatricpatients]

Proteinbinding 99.8%boundtoplasmaproteins,primarilyalbumin.

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Metabolism Hepatic.RosiglitazoneisextensivelymetabolizedinthelivertoinactivemetabolitesviaNdemethylation,hydroxylation,andconjugationwithsulfateandgluc
Substrate Enzymes Product
acid.InvitrodatahaveshownthatCytochrome(CYP)P450isoenzyme2C8(CYP2C8)andtoaminorextentCYP2C9areinvolvedinthehepaticmetabolism
rosiglitazone.

Substrate Enzymes Product

Rosiglitazone NDesmethylrosiglitazone Details

CytochromeP4502C8 (/metabolites/DBMET00295)
(/biodb/bio_entities/BE0002887)
CytochromeP4502C9
(/biodb/bio_entities/BE0002793)

Identification Taxonomy Rosiglitazone

Pharmacology ADMET Pharmacoeconomics
Properties Spectra References paraHydroxyrosiglitazone
Interactions Targets(2) Enzymes(7) Carriers(1) Details
CytochromeP4502C8 (/metabolites/DBMET00296)
Transporters(1) 0Comments (/biodb/bio_entities/BE0002887)
CytochromeP4502C9
(/biodb/bio_entities/BE0002793)

Rosiglitazone orthoHydroxyrosiglitazone Details

CytochromeP4502C8 (/metabolites/DBMET00470)
(/biodb/bio_entities/BE0002887)
CytochromeP4502C9
(/biodb/bio_entities/BE0002793)

Rosiglitazone NDespyridinylrosiglitazone Details

NotAvailable (/metabolites/DBMET00942)

NDesmethylrosiglitazone NDesmethylorthohydroxyrosiglitazone Details

(/metabolites/DBMET00295) NotAvailable (/metabolites/DBMET00936)

orthoHydroxyrosiglitazone NDesmethylorthohydroxyrosiglitazone Details

(/metabolites/DBMET00470) NotAvailable (/metabolites/DBMET00936)

NDesmethylrosiglitazone NDesmethylparahydroxyrosiglitazone Details

(/metabolites/DBMET00295) NotAvailable (/metabolites/DBMET00938)

paraHydroxyrosiglitazone NDesmethylparahydroxyrosiglitazone Details

(/metabolites/DBMET00296) NotAvailable (/metabolites/DBMET00938)

NDesmethylorthohydroxyrosiglitazone NDesmethylorthoOsulfaterosiglitazone Details

(/metabolites/DBMET00936) NotAvailable (/metabolites/DBMET00937)

orthoHydroxyrosiglitazone orthoOGlucuroniderosiglitazone Details

(/metabolites/DBMET00470) NotAvailable (/metabolites/DBMET00968)

orthoHydroxyrosiglitazone orthoOSulfaterosiglitazone Details

(/metabolites/DBMET00470) NotAvailable (/metabolites/DBMET00969)

NDesmethylrosiglitazone NDesmethylglucuroniderosiglitazone Details

(/metabolites/DBMET00295) NotAvailable (/metabolites/DBMET01111)

paraHydroxyrosiglitazone paraOGlucuroniderosiglitazone Details

(/metabolites/DBMET00296) NotAvailable (/metabolites/DBMET00981)

paraHydroxyrosiglitazone paraOSulfaterosiglitazone Details

(/metabolites/DBMET00296) NotAvailable (/metabolites/DBMET01112)

NDesmethylparahydroxyrosiglitazone NDesmethylparaOsulfaterosiglitazone Details

(/metabolites/DBMET00938) NotAvailable (/metabolites/DBMET01113)

Rosiglitazone Phenoxyaceticacidderivativeofrosiglitazone Details

NotAvailable (/metabolites/DBMET01365)

Routeof Followingoralorintravenousadministrationof[14C]rosiglitazonemaleate,approximately64%and23%ofthedosewaseliminatedintheurineandinthefe
elimination respectively.

Halflife 34hours(singleoraldose,independentofdose)

Clearance Oralclearance(CL)=3.030.87L/hr[1mgFasting]
OralCL=2.890.71L/hr[2mgFasting]
OralCL=2.850.69L/hr[8mgFasting]
OralCL=2.970.81L/hr[8mgFed]
3.15L/hr[Populationmean,Pediatricpatients]

Toxicity Sideeffectsincludefluidretention,congestiveheartfailure(CHF),liverdisease

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Affectedorganisms Pathway
Property
Humansandothermammals Category SMPDBIDValue Probability

Pathways Pathway Category SMPDBID

RosiglitazoneMetabolismPathway Drugmetabolism SMP00653(http://smpdb.ca/view/SMP00653?highlight[compounds][]=DB00412&highlight[proteins][]=DB00412)

SNPMediated NotAvailable
Effects

SNPMediated NotAvailable
AdverseDrug
Reactions
Identification
ADMET Taxonomy Pharmacology ADMET Pharmacoeconomics Properties Spectra References Interactions Targets(2) Enzymes(7) Carriers(1)

Transporters(1) 0Comments
PredictedADMET Property Value Probability
features
HumanIntestinalAbsorption + 0.9861

BloodBrainBarrier + 0.8994

Caco2permeable 0.5451

Pglycoproteinsubstrate Substrate 0.6535

PglycoproteininhibitorI Noninhibitor 0.5274

PglycoproteininhibitorII Noninhibitor 0.6289

Renalorganiccationtransporter Noninhibitor 0.5203

CYP4502C9substrate Nonsubstrate 0.7418

CYP4502D6substrate Nonsubstrate 0.9116

CYP4503A4substrate Substrate 0.5744

CYP4501A2substrate Inhibitor 0.5391

CYP4502C9inhibitor Inhibitor 0.5783

CYP4502D6inhibitor Noninhibitor 0.846

CYP4502C19inhibitor Inhibitor 0.5884

CYP4503A4inhibitor Noninhibitor 0.8309

CYP450inhibitorypromiscuity HighCYPInhibitoryPromiscuity 0.7213

Amestest NonAMEStoxic 0.687

Carcinogenicity Noncarcinogens 0.9465

Biodegradation Notreadybiodegradable 0.8635

Ratacutetoxicity 2.4515LD50,mol/kg Notapplicable

hERGinhibition(predictorI) Weakinhibitor 0.8055

hERGinhibition(predictorII) Noninhibitor 0.7768

ADMETdataispredictedusingadmetSAR(http://lmmd.ecust.edu.cn:8000),afreetoolforevaluatingchemicalADMETproperties.
(23092397(http://www.ncbi.nlm.nih.gov/pubmed/23092397))

Pharmacoeconomics

Manufacturers Sbpharmcopuertoricoinc
Glaxosmithkline

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10/6/2016 DrugBank:Rosiglitazone

Packagers ASMedicationSolutionsLLC(http://orders.asmeds.com)
AtlanticBiologicalsCorporation(http://www.atlanticbiologicals.com)
CardinalHealth(http://www.cardinal.com)
DiversifiedHealthcareServicesInc.(http://www.dhscorp.com)
GlaxoSmithKlineInc.(http://www.gsk.com)
KaiserFoundationHospital
LakeErieMedicalandSurgicalSupply
MurfreesboroPharmaceuticalNursingSupply(http://www.unitdosesupply.com)
PDRxPharmaceuticalsInc.(http://www.pdrx.com)
PharmacyServiceCenter
PhysiciansTotalCareInc.(http://www.physicianstotalcare.com)
PrepackageSpecialists
Identification Taxonomy Pharmacology ADMET Pharmacoeconomics
ResourceOptimizationandInnovationLLC Properties Spectra References Interactions Targets(2) Enzymes(7) Carriers(1)

Transporters(1) 0Comments SearleandCo.

SouthwoodPharmaceuticals(http://www.southwoodhealthcare.com)
TyaPharmaceuticals
VangardLabsInc.
WestWardPharmaceuticals(http://www.westward.com)

Dosageforms
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Form Route Strength

Filmcoatedtablet Oraluse

Filmcoatedtablet Oraluse 2mg

Filmcoatedtablet Oraluse 4mg

Filmcoatedtablet Oraluse 8mg

Tablet oral 2.0mg

Tablet oral 4.0mg

Tablet oral 8.0mg

Tablet oral

Tablet oral 2mg

Tablet oral 4mg

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Prices
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Unitdescription Cost Unit

Avandia2mgtablet 3.22USD tablet

Avandia4mgtablet 4.72USD tablet

Avandia8mgtablet 8.69USD tablet

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DrugBankdoesnotsellnorbuydrugs.Pricinginformationissuppliedforinformationalpurposesonly.

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10/6/2016 DrugBank:Rosiglitazone

Patents Property
SpectrumType Description
Value Source Value Source
SplashKey(http://splash.fiehnlab.ucdavis.edu/)
Show 10 entries
Search

PatentNumber PediatricExtension Approved Expires(estimated)

CA1328452(https://patents.google.com/patent/CA1328452) No 19940412 20110412

CA2143849(https://patents.google.com/patent/CA2143849) No 20000425 20130901

US5002953(https://patents.google.com/patent/US5002953) No 19940917 20110917

US5965584(https://patents.google.com/patent/US5965584) No 19960619 20160619

US6166042(https://patents.google.com/patent/US6166042) No 19960619 20160619

Identification Taxonomy Pharmacology ADMET Pharmacoeconomics Properties Spectra References Interactions Targets(2) Enzymes(7) Carriers(1)
US6288095 (https://patents.google.com/patent/US6288095) Yes 19970811 20170811
Transporters(1) 0Comments
US7358366 (https://patents.google.com/patent/US7358366) Yes 20001019 20201019

US8236345(https://patents.google.com/patent/US8236345) No 20021007 20221007

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Properties

State Solid

Experimental Property Value Source

Properties
meltingpoint 122123C NotAvailable

logP 2.4 NotAvailable

Predicted Property Value Source

Properties
WaterSolubility 0.038mg/mL ALOGPS(http://www.vcclab.org/lab/alogps/)

logP 2.95 ALOGPS(http://www.vcclab.org/lab/alogps/)

logP 2.45 ChemAxon(http://www.chemaxon.com/products/calculatorplugins/propertypredictors/#logp_logd)

logS 4 ALOGPS(http://www.vcclab.org/lab/alogps/)

pKa(StrongestAcidic) 6.84 ChemAxon(http://www.chemaxon.com/products/calculatorplugins/propertypredictors/#pka)

pKa(StrongestBasic) 6.23 ChemAxon(http://www.chemaxon.com/products/calculatorplugins/propertypredictors/#pka)

PhysiologicalCharge 1 ChemAxon(http://www.chemaxon.com/products/calculatorplugins/propertypredictors/#pka)

HydrogenAcceptorCount 5 ChemAxon(http://www.chemaxon.com/products/calculatorplugins/propertycalculations/#h_bond)

HydrogenDonorCount 1 ChemAxon(http://www.chemaxon.com/products/calculatorplugins/propertycalculations/#h_bond)

PolarSurfaceArea 71.532 ChemAxon(http://www.chemaxon.com/products/calculatorplugins/propertycalculations/#topolgical_surface)

RotatableBondCount 7 ChemAxon(http://www.chemaxon.com/products/calculatorplugins/propertycalculations/#topology_analysis)
3 1
Refractivity 97.79m mol ChemAxon(http://www.chemaxon.com/products/calculatorplugins/propertycalculations/#refractivity)

Polarizability 37.83 ChemAxon(http://www.chemaxon.com/products/calculatorplugins/molecularmodelling/#polarization)

NumberofRings 3 ChemAxon(http://www.chemaxon.com/products/calculatorplugins/propertycalculations/#topology_analysis)

Bioavailability 1 ChemAxon(http://www.chemaxon.com/products/calculatorplugins/molecularmodelling/#polarization)

RuleofFive Yes ChemAxon(http://www.chemaxon.com/products/calculatorplugins/molecularmodelling/#polarization)

GhoseFilter Yes ChemAxon(http://www.chemaxon.com/products/calculatorplugins/molecularmodelling/#polarization)

Veber'sRule Yes ChemAxon(http://www.chemaxon.com/products/calculatorplugins/molecularmodelling/#polarization)

MDDRlikeRule Yes ChemAxon(http://www.chemaxon.com/products/calculatorplugins/molecularmodelling/#polarization)

Spectra

MassSpec(NIST) NotAvailable

Spectra SpectrumType Description SplashKey(http://splash.fiehnlab.ucdavis.edu/)

PredictedLCMS/MS PredictedLCMS/MSSpectrum10V,Positive(/spectra/ms_ms/69159) NotAvailable

PredictedLCMS/MS PredictedLCMS/MSSpectrum20V,Positive(/spectra/ms_ms/69160) NotAvailable

PredictedLCMS/MS PredictedLCMS/MSSpectrum40V,Positive(/spectra/ms_ms/69161) NotAvailable

PredictedLCMS/MS PredictedLCMS/MSSpectrum10V,Negative(/spectra/ms_ms/127374) NotAvailable

PredictedLCMS/MS PredictedLCMS/MSSpectrum20V,Negative(/spectra/ms_ms/127375) NotAvailable

PredictedLCMS/MS PredictedLCMS/MSSpectrum40V,Negative(/spectra/ms_ms/127376) NotAvailable

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10/6/2016 DrugBank:Rosiglitazone

References Resource Link

Synthesis ManneReddy,Amorphousformofrosiglitazonemaleateandprocessforpreparationthereof.U.S.PatentUS20040242658,issuedDecember02,2004.
Reference
US20040242658(https://www.google.com/?tbm=pts#q=20040242658&tbm=pts)

GeneralReferences 1.MohantyP,AljadaA,GhanimH,HofmeyerD,TripathyD,SyedT,AlHaddadW,DhindsaS,DandonaP:Evidenceforapotentantiinflammatoryeffectofrosiglitazone.JClinEnd
Metab.2004Jun89(6):272835.[PubMed:15181049(http://www.ncbi.nlm.nih.gov/pubmed/15181049)]
2.KahnSE,HaffnerSM,HeiseMA,HermanWH,HolmanRR,JonesNP,KravitzBG,LachinJM,O'NeillMC,ZinmanB,VibertiG:Glycemicdurabilityofrosiglitazone,metformin,or
glyburidemonotherapy.NEnglJMed.2006Dec7355(23):242743.Epub2006Dec4.[PubMed:17145742(http://www.ncbi.nlm.nih.gov/pubmed/17145742)]

ExternalLinks Resource Link

KEGGDrug D00596(http://www.genome.jp/dbgetbin/www_bget?drug:D00596)

Identification Taxonomy PubChemCompound

Pharmacology ADMET 77999(http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=77999)
Pharmacoeconomics Properties Spectra References Interactions Targets(2) Enzymes(7) Carriers(1)

Transporters(1) PubChemSubstance
0Comments 46504556(http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504556)

BindingDB 28681(http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=28681)

ChEBI 50122(http://www.ebi.ac.uk/chebi/searchId.do?chebiId=50122)

ChEMBL CHEMBL121(http://www.ebi.ac.uk/chembldb/index.php/compound/inspect/CHEMBL121)

TherapeuticTargetsDatabase DAP000271(http://bidd.nus.edu.sg/group/cjttd/ZFTTDDRUG.asp?ID=DAP000271)

PharmGKB PA451283(http://www.pharmgkb.org/drug/PA451283)

IUPHAR 1056(http://www.iuphardb.org/DATABASE/LigandDisplayForward?ligandId=1056)

GuidetoPharmacology 1056(http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=1056)

HET BRL(http://www.ebi.ac.uk/pdbesrv/pdbechem/chemicalCompound/show/BRL)

DrugProductDatabase 11925(http://webprod5.hcsc.gc.ca/dpdbdpp/info.do?code=11925&lang=eng)

RxList http://www.rxlist.com/cgi/generic2/rosigl.htm(http://www.rxlist.com/cgi/generic2/rosigl.htm)

Drugs.com http://www.drugs.com/cdi/rosiglitazone.html(http://www.drugs.com/cdi/rosiglitazone.html)

PDRhealth http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/cx1532.shtml(http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/cx1532

Wikipedia Rosiglitazone(http://en.wikipedia.org/wiki/Rosiglitazone)

ATCCodes A10BD03
A10BDCombinationsoforalbloodglucoseloweringdrugs(/atc/A10BD)
A10BBLOODGLUCOSELOWERINGDRUGS,EXCL.INSULINS(/atc/A10B)
A10DRUGSUSEDINDIABETES(/atc/A10)
AALIMENTARYTRACTANDMETABOLISM(/atc/A)

A10BG02
A10BGThiazolidinediones(/atc/A10BG)
A10BBLOODGLUCOSELOWERINGDRUGS,EXCL.INSULINS(/atc/A10B)
A10DRUGSUSEDINDIABETES(/atc/A10)
AALIMENTARYTRACTANDMETABOLISM(/atc/A)

A10BD04
A10BDCombinationsoforalbloodglucoseloweringdrugs(/atc/A10BD)
A10BBLOODGLUCOSELOWERINGDRUGS,EXCL.INSULINS(/atc/A10B)
A10DRUGSUSEDINDIABETES(/atc/A10)
AALIMENTARYTRACTANDMETABOLISM(/atc/A)

AHFSCodes 68:20.28

PDBEntries NotAvailable

FDAlabel Download(https://s3uswest2.amazonaws.com/drugbank/fda_labels/DB00412.pdf?1265922808)(86.2KB)

MSDS Download(https://s3uswest2.amazonaws.com/drugbank/msds/DB00412.pdf?1265922746)(30KB)

Interactions

http://www.drugbank.ca/drugs/DB00412 10/17
10/6/2016 DrugBank:Rosiglitazone

DrugInteractions
Show 10 entries
Search

Drug
7,8DICHLORO1,2,3,4 7,8DICHLORO1,2,3,4TETRAHYDROISOQUINOLINEmayincreasethehypoglycemicactivitiesofRosiglitazone.
TETRAHYDROISOQUINOLINE
(/drugs/DB08550)

Abciximab(/drugs/DB00054) RosiglitazonemayincreasetheanticoagulantactivitiesofAbciximab.

Abiraterone(/drugs/DB05812) TheserumconcentrationofRosiglitazonecanbeincreasedwhenitiscombinedwithAbiraterone.

Acenocoumarol(/drugs/DB01418) RosiglitazonemayincreasetheanticoagulantactivitiesofAcenocoumarol.
Identification Taxonomy Pharmacology ADMET Pharmacoeconomics Properties Spectra References Interactions Targets(2) Enzymes(7) Carriers(1)
Acetaminophen(/drugs/DB00316) ThemetabolismofAcetaminophencanbedecreasedwhencombinedwithRosiglitazone.
Transporters(1) 0Comments
Acetohexamide(/drugs/DB00414) RosiglitazonemayincreasethehypoglycemicactivitiesofAcetohexamide.

Acetylsalicylicacid TheriskorseverityofadverseeffectscanbeincreasedwhenAcetylsalicylicacidiscombinedwithRosiglitazone.
(/drugs/DB00945)

Acetylsalicylicacid ThemetabolismofAcetylsalicylicacidcanbedecreasedwhencombinedwithRosiglitazone.
(/drugs/DB00945)

Almotriptan(/drugs/DB00918) ThemetabolismofAlmotriptancanbedecreasedwhencombinedwithRosiglitazone.

Alprostadil(/drugs/DB00770) AlprostadilmayincreasetheanticoagulantactivitiesofRosiglitazone.

Showing1to10of415entries
Previous 1 2 3 4 5

FoodInteractions NotAvailable

Targets

1.Peroxisomeproliferatoractivatedreceptorgamma(/biodb/polypeptides/P37231) Details(/biodb/polypeptides/P37231)

Kind
Protein
Organism
Human
Pharmacologicalaction
yes
Actions
agonist

GeneralFunction:
Zincionbinding
SpecificFunction:
Nuclearreceptorthatbindsperoxisomeproliferatorssuchashypolipidemicdrugsandfattyacids.Onceactivatedbyaligand,thenuclearreceptorbindsto
DNAspecificPPARresponseelements(PPRE)andmodulatesthetranscriptionofitstargetgenes,suchasacylCoAoxidase.Itthereforecontrolsthe
peroxisomalbetaoxidationpathwayoffattyacids.Keyregulatorofadipocytedifferentiation...
GeneName:
PPARG
UniprotID:
P37231(http://www.uniprot.org/uniprot/P37231)
MolecularWeight:
57619.58Da

References

1.SuJL,WinegarDA,WiselyGB,SigelCS,HullRydeEA:UseofaPPARgammaspecificmonoclonalantibodytodemonstratethiazolidinedionesinducePPARgamma
receptorexpressioninvitro.Hybridoma.1999Jun18(3):27380.[PubMed:10475242(http://www.ncbi.nlm.nih.gov/pubmed/10475242)]
2.RieussetJ,AuwerxJ,VidalH:Regulationofgeneexpressionbyactivationoftheperoxisomeproliferatoractivatedreceptorgammawithrosiglitazone(BRL49653)in
humanadipocytes.BiochemBiophysResCommun.1999Nov265(1):26571.[PubMed:10548525(http://www.ncbi.nlm.nih.gov/pubmed/10548525)]
3.KamedaN,OkuyaS,OkaY:[Rosiglitazone(BRL49653)].NihonRinsho.2000Feb58(2):4014.
[PubMed:10707565(http://www.ncbi.nlm.nih.gov/pubmed/10707565)]
4.JohnsonBA,WilsonEM,LiY,MollerDE,SmithRG,ZhouG:LigandinducedstabilizationofPPARgammamonitoredbyNMRspectroscopy:implicationsfornuclear
receptoractivation.JMolBiol.2000Apr28298(2):18794.[PubMed:10764590(http://www.ncbi.nlm.nih.gov/pubmed/10764590)]
5.CampHS,LiO,WiseSC,HongYH,FrankowskiCL,ShenX,VanbogelenR,LeffT:Differentialactivationofperoxisomeproliferatoractivatedreceptorgammaby
troglitazoneandrosiglitazone.Diabetes.2000Apr49(4):53947.[PubMed:10871190(http://www.ncbi.nlm.nih.gov/pubmed/10871190)]
6.ChenX,JiZL,ChenYZ:TTD:TherapeuticTargetDatabase.NucleicAcidsRes.2002Jan130(1):4125.
[PubMed:11752352(http://www.ncbi.nlm.nih.gov/pubmed/11752352)]

2.LongchainfattyacidCoAligase4(/biodb/polypeptides/O60488) Details(/biodb/polypeptides/O60488)

http://www.drugbank.ca/drugs/DB00412 11/17
10/6/2016 DrugBank:Rosiglitazone

Kind
Protein
Organism
Human
Pharmacologicalaction
unknown
Actions
inhibitor

GeneralFunction:
Verylongchainfattyacidcoaligaseactivity
SpecificFunction:
Identification Taxonomy Pharmacology ADMET Pharmacoeconomics Properties Spectra References Interactions Targets(2) Enzymes(7) Carriers(1)
Activationoflongchainfattyacidsforbothsynthesisofcellularlipids,anddegradationviabetaoxidation.Preferentiallyusesarachidonateand
eicosapentaenoateassubstrates.
Transporters(1) 0Comments
GeneName:
ACSL4
UniprotID:
O60488(http://www.uniprot.org/uniprot/O60488)
MolecularWeight:
79187.38Da

References

1.AskariB,KanterJE,SherridAM,GolejDL,BenderAT,LiuJ,HsuehWA,BeavoJA,ColemanRA,BornfeldtKE:RosiglitazoneinhibitsacylCoAsynthetaseactivityand
fattyacidpartitioningtodiacylglycerolandtriacylglycerolviaaperoxisomeproliferatoractivatedreceptorgammaindependentmechanisminhumanarterialsmooth
musclecellsandmacrophages.Diabetes.2007Apr56(4):114352.Epub2007Jan26.[PubMed:17259370(http://www.ncbi.nlm.nih.gov/pubmed/17259370)]

Enzymes

1.CytochromeP4502C8(/biodb/polypeptides/P10632) Details(/biodb/polypeptides/P10632)

Kind
Protein
Organism
Human
Pharmacologicalaction
unknown
Actions
substrate inhibitor

GeneralFunction:
Steroidhydroxylaseactivity
SpecificFunction:
CytochromesP450areagroupofhemethiolatemonooxygenases.Inlivermicrosomes,thisenzymeisinvolvedinanNADPHdependentelectrontransport
pathway.Itoxidizesavarietyofstructurallyunrelatedcompounds,includingsteroids,fattyacids,andxenobiotics.Intheepoxidationofarachidonicacidit
generatesonly14,15and11,12cisepoxyeicosatrienoicacids.Itistheprincipalenzyme...
GeneName:
CYP2C8
UniprotID:
P10632(http://www.uniprot.org/uniprot/P10632)
MolecularWeight:
55824.275Da

References

1.ZhouSF,ZhouZW,YangLP,CaiJP:Substrates,inducers,inhibitorsandstructureactivityrelationshipsofhumanCytochromeP4502C9andimplicationsindrug
development.CurrMedChem.200916(27):3480675.Epub2009Sep1.[PubMed:19515014(http://www.ncbi.nlm.nih.gov/pubmed/19515014)]
2.PreissnerS,KrollK,DunkelM,SengerC,GoldsobelG,KuzmanD,GuentherS,WinnenburgR,SchroederM,PreissnerR:SuperCYP:acomprehensivedatabaseon
CytochromeP450enzymesincludingatoolforanalysisofCYPdruginteractions.NucleicAcidsRes.2010Jan38(Databaseissue):D23743.doi:10.1093/nar/gkp970.
Epub2009Nov24.[PubMed:19934256(http://www.ncbi.nlm.nih.gov/pubmed/19934256)]

2.CytochromeP4502C9(/biodb/polypeptides/P11712) Details(/biodb/polypeptides/P11712)

Kind
Protein
Organism
Human
Pharmacologicalaction

http://www.drugbank.ca/drugs/DB00412 12/17
10/6/2016 DrugBank:Rosiglitazone
unknown
Actions
substrate inhibitor

GeneralFunction:
Steroidhydroxylaseactivity
SpecificFunction:
CytochromesP450areagroupofhemethiolatemonooxygenases.Inlivermicrosomes,thisenzymeisinvolvedinanNADPHdependentelectrontransport
pathway.Itoxidizesavarietyofstructurallyunrelatedcompounds,includingsteroids,fattyacids,andxenobiotics.Thisenzymecontributestothewide
pharmacokineticsvariabilityofthemetabolismofdrugssuchasSwarfarin,diclofenac,phenyto...
GeneName:
CYP2C9
UniprotID:
Identification Taxonomy Pharmacology ADMET Pharmacoeconomics Properties Spectra References Interactions Targets(2) Enzymes(7) Carriers(1)
P11712(http://www.uniprot.org/uniprot/P11712)
Transporters(1) 0Comments
MolecularWeight:
55627.365Da

References

1.PreissnerS,KrollK,DunkelM,SengerC,GoldsobelG,KuzmanD,GuentherS,WinnenburgR,SchroederM,PreissnerR:SuperCYP:acomprehensivedatabaseon
CytochromeP450enzymesincludingatoolforanalysisofCYPdruginteractions.NucleicAcidsRes.2010Jan38(Databaseissue):D23743.doi:10.1093/nar/gkp970.
Epub2009Nov24.[PubMed:19934256(http://www.ncbi.nlm.nih.gov/pubmed/19934256)]
2.DrugInteractions:CytochromeP450DrugInteractionTable[Link(http://medicine.iupui.edu/clinpharm/ddis/table.asp)]

3.ProstaglandinG/Hsynthase1(/biodb/polypeptides/P23219) Details(/biodb/polypeptides/P23219)

Kind
Protein
Organism
Human
Pharmacologicalaction
unknown
Actions
substrate

GeneralFunction:
Prostaglandinendoperoxidesynthaseactivity
SpecificFunction:
ConvertsarachidonatetoprostaglandinH2(PGH2),acommittedstepinprostanoidsynthesis.Involvedintheconstitutiveproductionofprostanoidsin
particularinthestomachandplatelets.Ingastricepithelialcells,itisakeystepinthegenerationofprostaglandins,suchasprostaglandinE2(PGE2),which
playsanimportantroleincytoprotection.Inplatelets,itisinvolvedinthegener...
GeneName:
PTGS1
UniprotID:
P23219(http://www.uniprot.org/uniprot/P23219)
MolecularWeight:
68685.82Da

References

1.ZhouSF,ZhouZW,YangLP,CaiJP:Substrates,inducers,inhibitorsandstructureactivityrelationshipsofhumanCytochromeP4502C9andimplicationsindrug
development.CurrMedChem.200916(27):3480675.Epub2009Sep1.[PubMed:19515014(http://www.ncbi.nlm.nih.gov/pubmed/19515014)]

4.CytochromeP4501A2(/biodb/polypeptides/P05177) Details(/biodb/polypeptides/P05177)

Kind
Protein
Organism
Human
Pharmacologicalaction
unknown
Actions
inhibitor

GeneralFunction:
Oxidoreductaseactivity,actingonpaireddonors,withincorporationorreductionofmolecularoxygen,reducedflavinorflavoproteinasonedonor,and
incorporationofoneatomofoxygen
SpecificFunction:

http://www.drugbank.ca/drugs/DB00412 13/17
10/6/2016 DrugBank:Rosiglitazone
CytochromesP450areagroupofhemethiolatemonooxygenases.Inlivermicrosomes,thisenzymeisinvolvedinanNADPHdependentelectrontransport
pathway.Itoxidizesavarietyofstructurallyunrelatedcompounds,includingsteroids,fattyacids,andxenobiotics.Mostactiveincatalyzing2hydroxylation.
CaffeineismetabolizedprimarilybycytochromeCYP1A2intheliverthroughaninitialN...
GeneName:
CYP1A2
UniprotID:
P05177(http://www.uniprot.org/uniprot/P05177)
MolecularWeight:
58293.76Da

References

1.PreissnerS,KrollK,DunkelM,SengerC,GoldsobelG,KuzmanD,GuentherS,WinnenburgR,SchroederM,PreissnerR:SuperCYP:acomprehensivedatabaseon
Identification Taxonomy Pharmacology ADMET Pharmacoeconomics Properties Spectra References Interactions Targets(2) Enzymes(7) Carriers(1)
CytochromeP450enzymesincludingatoolforanalysisofCYPdruginteractions.NucleicAcidsRes.2010Jan38(Databaseissue):D23743.doi:10.1093/nar/gkp970.
Transporters(1) Epub2009Nov24.[PubMed:19934256
0Comments (http://www.ncbi.nlm.nih.gov/pubmed/19934256)]

5.CytochromeP4502A6(/biodb/polypeptides/P11509) Details(/biodb/polypeptides/P11509)

Kind
Protein
Organism
Human
Pharmacologicalaction
unknown
Actions
inhibitor

GeneralFunction:
Steroidhydroxylaseactivity
SpecificFunction:
Exhibitsahighcoumarin7hydroxylaseactivity.Canactinthehydroxylationoftheanticancerdrugscyclophosphamideandifosphamide.Competentinthe
metabolicactivationofaflatoxinB1.ConstitutesthemajornicotineCoxidase.Actsasa1,4cineole2exomonooxygenase.PossesseslowphenacetinO
deethylationactivity.
GeneName:
CYP2A6
UniprotID:
P11509(http://www.uniprot.org/uniprot/P11509)
MolecularWeight:
56501.005Da

References

1.PreissnerS,KrollK,DunkelM,SengerC,GoldsobelG,KuzmanD,GuentherS,WinnenburgR,SchroederM,PreissnerR:SuperCYP:acomprehensivedatabaseon
CytochromeP450enzymesincludingatoolforanalysisofCYPdruginteractions.NucleicAcidsRes.2010Jan38(Databaseissue):D23743.doi:10.1093/nar/gkp970.
Epub2009Nov24.[PubMed:19934256(http://www.ncbi.nlm.nih.gov/pubmed/19934256)]

6.CytochromeP4502C19(/biodb/polypeptides/P33261) Details(/biodb/polypeptides/P33261)

Kind
Protein
Organism
Human
Pharmacologicalaction
unknown
Actions
inhibitor

GeneralFunction:
Steroidhydroxylaseactivity
SpecificFunction:
ResponsibleforthemetabolismofanumberoftherapeuticagentssuchastheanticonvulsantdrugSmephenytoin,omeprazole,proguanil,certain
barbiturates,diazepam,propranolol,citalopramandimipramine.
GeneName:
CYP2C19
UniprotID:
P33261(http://www.uniprot.org/uniprot/P33261)
MolecularWeight:
55930.545Da

References
http://www.drugbank.ca/drugs/DB00412 14/17
10/6/2016 DrugBank:Rosiglitazone
References

1.PreissnerS,KrollK,DunkelM,SengerC,GoldsobelG,KuzmanD,GuentherS,WinnenburgR,SchroederM,PreissnerR:SuperCYP:acomprehensivedatabaseon
CytochromeP450enzymesincludingatoolforanalysisofCYPdruginteractions.NucleicAcidsRes.2010Jan38(Databaseissue):D23743.doi:10.1093/nar/gkp970.
Epub2009Nov24.[PubMed:19934256(http://www.ncbi.nlm.nih.gov/pubmed/19934256)]

7.CytochromeP4502D6(/biodb/polypeptides/P10635) Details(/biodb/polypeptides/P10635)

Kind
Protein
Organism
Identification Taxonomy Pharmacology ADMET Pharmacoeconomics Properties Spectra References Interactions Targets(2) Enzymes(7) Carriers(1)
Human
Transporters(1) 0Comments
Pharmacologicalaction
unknown
Actions
inhibitor

GeneralFunction:
Steroidhydroxylaseactivity
SpecificFunction:
Responsibleforthemetabolismofmanydrugsandenvironmentalchemicalsthatitoxidizes.Itisinvolvedinthemetabolismofdrugssuchasantiarrhythmics,
adrenoceptorantagonists,andtricyclicantidepressants.
GeneName:
CYP2D6
UniprotID:
P10635(http://www.uniprot.org/uniprot/P10635)
MolecularWeight:
55768.94Da

References

1.PreissnerS,KrollK,DunkelM,SengerC,GoldsobelG,KuzmanD,GuentherS,WinnenburgR,SchroederM,PreissnerR:SuperCYP:acomprehensivedatabaseon
CytochromeP450enzymesincludingatoolforanalysisofCYPdruginteractions.NucleicAcidsRes.2010Jan38(Databaseissue):D23743.doi:10.1093/nar/gkp970.
Epub2009Nov24.[PubMed:19934256(http://www.ncbi.nlm.nih.gov/pubmed/19934256)]

Carriers

1.Serumalbumin(/biodb/polypeptides/P02768) Details(/biodb/polypeptides/P02768)

Kind
Protein
Organism
Human
Pharmacologicalaction
unknown
Actions
substrate

GeneralFunction:
Toxicsubstancebinding
SpecificFunction:
Serumalbumin,themainproteinofplasma,hasagoodbindingcapacityforwater,Ca(2+),Na(+),K(+),fattyacids,hormones,bilirubinanddrugs.Itsmain
functionistheregulationofthecolloidalosmoticpressureofblood.Majorzinctransporterinplasma,typicallybindsabout80%ofallplasmazinc.
GeneName:
ALB
UniprotID:
P02768(http://www.uniprot.org/uniprot/P02768)
MolecularWeight:
69365.94Da

Transporters

1.Solutecarrierorganicaniontransporterfamilymember1B1(/biodb/polypeptides/Q9Y6L6) Details(/biodb/polypeptides/Q9Y6L6)

Kind

http://www.drugbank.ca/drugs/DB00412 15/17
10/6/2016 DrugBank:Rosiglitazone
Protein
Organism
Human
Pharmacologicalaction
unknown
Actions
inhibitor

GeneralFunction:
Sodiumindependentorganicaniontransmembranetransporteractivity
SpecificFunction:
MediatestheNa(+)independentuptakeoforganicanionssuchaspravastatin,taurocholate,methotrexate,dehydroepiandrosteronesulfate,17beta
glucuronosylestradiol,estronesulfate,prostaglandinE2,thromboxaneB2,leukotrieneC3,leukotrieneE4,thyroxineandtriiodothyronine.Involvedinthe
Identification Taxonomy Pharmacology ADMET Pharmacoeconomics Properties Spectra References Interactions Targets(2) Enzymes(7) Carriers(1)
clearanceofbileacidsandorganicanionsfromtheliver.
Transporters(1) 0Comments
GeneName:
SLCO1B1
UniprotID:
Q9Y6L6(http://www.uniprot.org/uniprot/Q9Y6L6)
MolecularWeight:
76447.99Da

References

1.NozawaT,SugiuraS,NakajimaM,GotoA,YokoiT,NezuJ,TsujiA,TamaiI:Involvementoforganicaniontransportingpolypeptidesinthetransportoftroglitazone
sulfate:implicationsforunderstandingtroglitazonehepatotoxicity.DrugMetabDispos.2004Mar32(3):2914.
[PubMed:14977862(http://www.ncbi.nlm.nih.gov/pubmed/14977862)]

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DrugcreatedonJune13,200507:24/UpdatedonOctober05,201603:36

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ThisprojectissupportedbytheCanadianInstitutesofHealthResearch(http://www.cihrirsc.gc.ca)(award#111062),AlbertaInnovatesHealthSolutions(http://www.aihealthsolutions.ca),andby
TheMetabolomicsInnovationCentre(TMIC)(http://www.metabolomicscentre.ca/),anationallyfundedresearchandcorefacilitythatsupportsawiderangeofcuttingedgemetabolomicstudies.
TMICisfundedbyGenomeAlberta(http://www.genomealberta.ca),GenomeBritishColumbia(http://www.genomebc.ca/),andGenomeCanada(http://www.genomecanada.ca),anotforprofit
organizationthatisleadingCanada'snationalgenomicsstrategywith$900millioninfundingfromthefederalgovernment.Maintenance,support,andcommerciallicensingisprovidedbyOMx
PersonalHealthAnalytics,Inc.(http://omx.io)

(http://www.metabolomicscentre.ca)

(http://www.cihrirsc.gc.ca)
Identification Taxonomy Pharmacology ADMET (http://www.aihealthsolutions.ca)
Pharmacoeconomics Properties (http://genomealberta.ca)
Spectra References Interactions (http://genomebc.ca)
Targets(2) Enzymes(7) Carriers(1) (http://genomecanad

Transporters(1) 0Comments

http://www.drugbank.ca/drugs/DB00412 17/17