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Identification
NameXimelagatran
Accession NumberDB04898
TypeSmall Molecule
GroupsApproved, Investigational, Withdrawn
DescriptionXimelagatran (Exanta® or Exarta®, H 376/95) is an anticoagulant that has been investigated extensively as a replacement for warfarin that would overcome the problematic dietary, drug interaction, and monitoring issues associated with warfarin therapy. In 2006, its manufacturer AstraZeneca announced that it would not attempt to market ximelagatran after reports of hepatotoxicity (liver damage) during trials, and to discontinue its distribution in countries where the drug had been approved.
Structure
Thumb
Synonyms
Ethyl 2-[[(1R)-1-cyclohexyl-2- [(2S)-2-[[4-(n'-hydroxycarbamimidoyl) phenyl]methylcarbamoyl]azetidin-1-yl]- 2-oxo-ethyl]amino]acetate
Exanta
Exarta
H 376-95
H 376/95
H 37695
Ximelagatranum
External Identifiers Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
ExantaNot Available
ExartaNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNII49HFB70472
CAS number192939-46-1
WeightAverage: 473.5652
Monoisotopic: 473.263819255
Chemical FormulaC24H35N5O5
InChI KeyZXIBCJHYVWYIKI-PZJWPPBQSA-N
InChI
InChI=1S/C24H35N5O5/c1-2-34-20(30)15-26-21(17-6-4-3-5-7-17)24(32)29-13-12-19(29)23(31)27-14-16-8-10-18(11-9-16)22(25)28-33/h8-11,17,19,21,26,33H,2-7,12-15H2,1H3,(H2,25,28)(H,27,31)/t19-,21+/m0/s1
IUPAC Name
ethyl 2-{[(1R)-1-cyclohexyl-2-[(2S)-2-[({4-[(Z)-N'-hydroxycarbamimidoyl]phenyl}methyl)carbamoyl]azetidin-1-yl]-2-oxoethyl]amino}acetate
SMILES
CCOC(=O)CN[C@@H](C(=O)N1CC[[email protected]]1C(=O)NCC1=CC=C(C=C1)C(\N)=N\O)C1CCCCC1
Pharmacology
IndicationFor the treatment of acute deep vein thrombosis.
Structured Indications Not Available
PharmacodynamicsNot Available
Mechanism of actionXimelagatran was the first member of the drug class of direct thrombin inhibitors that can be taken orally. It acts solely by inhibiting the actions of thrombin. Ximelagatran is a prodrug, being converted in vivo to the active agent melagatran.
TargetKindPharmacological actionActionsOrganismUniProt ID
ProthrombinProteinyes
inhibitor
HumanP00734 details
Related Articles
AbsorptionRapidly absorbed by the small intestine with an oral bioavailability of 20%.
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

Hepatic. Ximelagatran is a prodrug, being converted in vivo to the active agent melagatran. This conversion takes place in the liver and many other tissues through dealkylation and dehydroxylation (replacing the ethyl and hydroxyl groups with hydrogen).

Route of eliminationNot Available
Half life3-5 hours
ClearanceNot Available
ToxicityHepatotoxicity (liver damage) was reported during trials.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Ximelagatran Action PathwayDrug actionSMP00279
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
AbacavirThe serum concentration of Abacavir can be decreased when it is combined with Ximelagatran.Approved, Investigational
AbciximabAbciximab may increase the anticoagulant activities of Ximelagatran.Approved
AbirateroneThe metabolism of Ximelagatran can be decreased when combined with Abiraterone.Approved
AceclofenacAceclofenac may increase the anticoagulant activities of Ximelagatran.Approved
AcenocoumarolAcenocoumarol may increase the anticoagulant activities of Ximelagatran.Approved
AcetovanilloneAcetovanillone may increase the anticoagulant activities of Ximelagatran.Investigational
Acetylsalicylic acidAcetylsalicylic acid may increase the anticoagulant activities of Ximelagatran.Approved, Vet Approved
AdapaleneAdapalene may increase the anticoagulant activities of Ximelagatran.Approved
AlfuzosinThe serum concentration of Alfuzosin can be increased when it is combined with Ximelagatran.Approved, Investigational
AllylestrenolThe therapeutic efficacy of Ximelagatran can be decreased when used in combination with Allylestrenol.Approved
AlprazolamThe serum concentration of Alprazolam can be increased when it is combined with Ximelagatran.Approved, Illicit, Investigational
AlprostadilAlprostadil may increase the anticoagulant activities of Ximelagatran.Approved, Investigational
AlteplaseAlteplase may increase the anticoagulant activities of Ximelagatran.Approved
AltrenogestThe therapeutic efficacy of Ximelagatran can be decreased when used in combination with Altrenogest.Vet Approved
ALX-0081ALX-0081 may increase the anticoagulant activities of Ximelagatran.Investigational
Ambroxol acefyllinateThe serum concentration of Ambroxol acefyllinate can be decreased when it is combined with Ximelagatran.Experimental
AmineptineThe serum concentration of Amineptine can be increased when it is combined with Ximelagatran.Illicit, Withdrawn
AminophyllineThe serum concentration of Aminophylline can be decreased when it is combined with Ximelagatran.Approved
Aminosalicylic AcidAminosalicylic Acid may increase the anticoagulant activities of Ximelagatran.Approved
AmiodaroneThe metabolism of Ximelagatran can be decreased when combined with Amiodarone.Approved, Investigational
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Ximelagatran.Approved
AnagrelideAnagrelide may increase the anticoagulant activities of Ximelagatran.Approved
AncrodXimelagatran may increase the anticoagulant activities of Ancrod.Investigational
AnisodamineAnisodamine may increase the anticoagulant activities of Ximelagatran.Investigational
AnistreplaseAnistreplase may increase the anticoagulant activities of Ximelagatran.Approved
AntipyrineAntipyrine may increase the anticoagulant activities of Ximelagatran.Approved
Antithrombin III humanXimelagatran may increase the anticoagulant activities of Antithrombin III human.Approved
ApixabanApixaban may increase the anticoagulant activities of Ximelagatran.Approved
ApremilastApremilast may increase the anticoagulant activities of Ximelagatran.Approved, Investigational
AprepitantThe metabolism of Ximelagatran can be increased when combined with Aprepitant.Approved, Investigational
AprotininThe therapeutic efficacy of Ximelagatran can be decreased when used in combination with Aprotinin.Approved, Withdrawn
ArdeparinArdeparin may increase the anticoagulant activities of Ximelagatran.Approved, Withdrawn
ArgatrobanArgatroban may increase the anticoagulant activities of Ximelagatran.Approved, Investigational
AstaxanthinAstaxanthin may increase the anticoagulant activities of Ximelagatran.Investigational
AtorvastatinThe serum concentration of Atorvastatin can be increased when it is combined with Ximelagatran.Approved
AzapropazoneAzapropazone may increase the anticoagulant activities of Ximelagatran.Withdrawn
AzelastineAzelastine may increase the anticoagulant activities of Ximelagatran.Approved
BalsalazideBalsalazide may increase the anticoagulant activities of Ximelagatran.Approved, Investigational
BatroxobinBatroxobin may increase the anticoagulant activities of Ximelagatran.Experimental
BazedoxifeneBazedoxifene may decrease the anticoagulant activities of Ximelagatran.Approved, Investigational
BecaplerminBecaplermin may increase the anticoagulant activities of Ximelagatran.Approved, Investigational
BemiparinBemiparin may increase the anticoagulant activities of Ximelagatran.Approved
BenoxaprofenBenoxaprofen may increase the anticoagulant activities of Ximelagatran.Withdrawn
BeraprostBeraprost may increase the anticoagulant activities of Ximelagatran.Investigational
Betulinic AcidBetulinic Acid may increase the anticoagulant activities of Ximelagatran.Investigational
BivalirudinBivalirudin may increase the anticoagulant activities of Ximelagatran.Approved, Investigational
BoceprevirThe serum concentration of Ximelagatran can be decreased when it is combined with Boceprevir.Approved
BromfenacBromfenac may increase the anticoagulant activities of Ximelagatran.Approved
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Ximelagatran.Approved, Investigational
BucillamineBucillamine may increase the anticoagulant activities of Ximelagatran.Investigational
ButylphthalideButylphthalide may increase the anticoagulant activities of Ximelagatran.Investigational
CabergolineThe serum concentration of Cabergoline can be increased when it is combined with Ximelagatran.Approved
CangrelorCangrelor may increase the anticoagulant activities of Ximelagatran.Approved
CapecitabineThe metabolism of Ximelagatran can be decreased when combined with Capecitabine.Approved, Investigational
CarbamazepineThe metabolism of Ximelagatran can be increased when combined with Carbamazepine.Approved, Investigational
CarprofenCarprofen may increase the anticoagulant activities of Ximelagatran.Approved, Vet Approved, Withdrawn
CastanospermineCastanospermine may increase the anticoagulant activities of Ximelagatran.Experimental
CelecoxibCelecoxib may increase the anticoagulant activities of Ximelagatran.Approved, Investigational
CeritinibThe serum concentration of Ximelagatran can be increased when it is combined with Ceritinib.Approved
CertoparinXimelagatran may increase the anticoagulant activities of Certoparin.Approved
ChloroquineChloroquine may increase the anticoagulant activities of Ximelagatran.Approved, Vet Approved
ChlorotrianiseneThe serum concentration of Chlorotrianisene can be decreased when it is combined with Ximelagatran.Withdrawn
CholecalciferolThe metabolism of Ximelagatran can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CilostazolCilostazol may increase the anticoagulant activities of Ximelagatran.Approved
CisaprideThe serum concentration of Cisapride can be increased when it is combined with Ximelagatran.Approved, Investigational, Withdrawn
Citric AcidCitric Acid may increase the anticoagulant activities of Ximelagatran.Nutraceutical, Vet Approved
ClarithromycinThe therapeutic efficacy of Clarithromycin can be decreased when used in combination with Ximelagatran.Approved
ClomipramineThe serum concentration of Clomipramine can be increased when it is combined with Ximelagatran.Approved, Vet Approved
ClonixinClonixin may increase the anticoagulant activities of Ximelagatran.Approved
ClopidogrelClopidogrel may increase the anticoagulant activities of Ximelagatran.Approved, Nutraceutical
ClotrimazoleThe metabolism of Ximelagatran can be decreased when combined with Clotrimazole.Approved, Vet Approved
CollagenaseThe risk or severity of adverse effects can be increased when Ximelagatran is combined with Collagenase.Approved
Conjugated Equine EstrogensThe serum concentration of Conjugated Equine Estrogens can be decreased when it is combined with Ximelagatran.Approved
CurcuminCurcumin may increase the anticoagulant activities of Ximelagatran.Investigational
CyclobenzaprineThe serum concentration of Cyclobenzaprine can be increased when it is combined with Ximelagatran.Approved
CyclophosphamideThe risk or severity of adverse effects can be increased when Ximelagatran is combined with Cyclophosphamide.Approved, Investigational
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Ximelagatran.Approved, Investigational, Vet Approved
CyclosporineThe metabolism of Ximelagatran can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
D-LimoneneD-Limonene may increase the anticoagulant activities of Ximelagatran.Investigational
Dabigatran etexilateDabigatran etexilate may increase the anticoagulant activities of Ximelagatran.Approved
DabrafenibThe serum concentration of Ximelagatran can be decreased when it is combined with Dabrafenib.Approved
DalteparinXimelagatran may increase the anticoagulant activities of Dalteparin.Approved
DanaparoidXimelagatran may increase the anticoagulant activities of Danaparoid.Approved, Withdrawn
DasatinibDasatinib may increase the anticoagulant activities of Ximelagatran.Approved, Investigational
DeferasiroxThe risk or severity of adverse effects can be increased when Ximelagatran is combined with Deferasirox.Approved, Investigational
DefibrotideDefibrotide may increase the anticoagulant activities of Ximelagatran.Approved, Investigational
DelavirdineThe serum concentration of Delavirdine can be decreased when it is combined with Ximelagatran.Approved
Deoxycholic AcidThe risk or severity of adverse effects can be increased when Ximelagatran is combined with Deoxycholic Acid.Approved
dersalazinedersalazine may increase the anticoagulant activities of Ximelagatran.Investigational
DesipramineThe serum concentration of Desipramine can be increased when it is combined with Ximelagatran.Approved
DesirudinXimelagatran may increase the anticoagulant activities of Desirudin.Approved
DesmoteplaseDesmoteplase may increase the anticoagulant activities of Ximelagatran.Investigational
DesogestrelThe therapeutic efficacy of Ximelagatran can be decreased when used in combination with Desogestrel.Approved
DextranXimelagatran may increase the anticoagulant activities of Dextran.Approved, Vet Approved
Dextran 40Ximelagatran may increase the anticoagulant activities of Dextran 40.Approved
Dextran 70Ximelagatran may increase the anticoagulant activities of Dextran 70.Approved
Dextran 75Ximelagatran may increase the anticoagulant activities of Dextran 75.Approved
DiclofenacDiclofenac may increase the anticoagulant activities of Ximelagatran.Approved, Vet Approved
DicoumarolDicoumarol may increase the anticoagulant activities of Ximelagatran.Approved
DienestrolThe serum concentration of Dienestrol can be decreased when it is combined with Ximelagatran.Approved
DienogestThe therapeutic efficacy of Ximelagatran can be decreased when used in combination with Dienogest.Approved
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be decreased when it is combined with Ximelagatran.Approved
DiflunisalDiflunisal may increase the anticoagulant activities of Ximelagatran.Approved
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Ximelagatran.Approved
DihydroergotamineThe serum concentration of Dihydroergotamine can be increased when it is combined with Ximelagatran.Approved
DiltiazemThe metabolism of Diltiazem can be decreased when combined with Ximelagatran.Approved
DipyridamoleDipyridamole may increase the anticoagulant activities of Ximelagatran.Approved
DitazoleDitazole may increase the anticoagulant activities of Ximelagatran.Approved, Withdrawn
DosulepinThe serum concentration of Dosulepin can be increased when it is combined with Ximelagatran.Approved
DoxepinThe serum concentration of Doxepin can be increased when it is combined with Ximelagatran.Approved
DrospirenoneThe therapeutic efficacy of Ximelagatran can be decreased when used in combination with Drospirenone.Approved
Drotrecogin alfaDrotrecogin alfa may increase the anticoagulant activities of Ximelagatran.Approved, Investigational, Withdrawn
DroxicamDroxicam may increase the anticoagulant activities of Ximelagatran.Approved
DuvelisibDuvelisib may increase the anticoagulant activities of Ximelagatran.Investigational
DydrogesteroneThe therapeutic efficacy of Ximelagatran can be decreased when used in combination with Dydrogesterone.Approved, Withdrawn
DyphyllineThe serum concentration of Dyphylline can be decreased when it is combined with Ximelagatran.Approved
E6201E6201 may increase the anticoagulant activities of Ximelagatran.Investigational
EbselenEbselen may increase the anticoagulant activities of Ximelagatran.Investigational
Edetic AcidEdetic Acid may increase the anticoagulant activities of Ximelagatran.Approved, Vet Approved
EdoxabanEdoxaban may increase the anticoagulant activities of Ximelagatran.Approved
EfavirenzThe metabolism of Ximelagatran can be decreased when combined with Efavirenz.Approved, Investigational
EnfuvirtideThe serum concentration of Enfuvirtide can be increased when it is combined with Ximelagatran.Approved, Investigational
EnoxaparinEnoxaparin may increase the anticoagulant activities of Ximelagatran.Approved
EpinastineEpinastine may increase the anticoagulant activities of Ximelagatran.Approved, Investigational
EpirizoleEpirizole may increase the anticoagulant activities of Ximelagatran.Approved
eplivanserineeplivanserine may increase the anticoagulant activities of Ximelagatran.Investigational
EpoprostenolEpoprostenol may increase the anticoagulant activities of Ximelagatran.Approved
EptifibatideEptifibatide may increase the anticoagulant activities of Ximelagatran.Approved, Investigational
Ergoloid mesylateThe serum concentration of Ergoloid mesylate can be increased when it is combined with Ximelagatran.Approved
ErgonovineThe serum concentration of Ergonovine can be increased when it is combined with Ximelagatran.Approved
ErgotamineThe serum concentration of Ergotamine can be increased when it is combined with Ximelagatran.Approved
EsmirtazapineThe serum concentration of Esmirtazapine can be increased when it is combined with Ximelagatran.Investigational
EstradiolThe serum concentration of Estradiol can be decreased when it is combined with Ximelagatran.Approved, Investigational, Vet Approved
EstramustineThe serum concentration of Estramustine can be decreased when it is combined with Ximelagatran.Approved
EstriolEstriol may decrease the anticoagulant activities of Ximelagatran.Approved, Vet Approved
Estrogens, esterifiedThe serum concentration of Estrogens, esterified can be decreased when it is combined with Ximelagatran.Approved
EstroneEstrone may decrease the anticoagulant activities of Ximelagatran.Approved
Estrone sulfateThe serum concentration of Estrone sulfate can be decreased when it is combined with Ximelagatran.Approved
EtanerceptEtanercept may increase the anticoagulant activities of Ximelagatran.Approved, Investigational
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be decreased when it is combined with Ximelagatran.Approved
Ethyl biscoumacetateXimelagatran may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
Ethynodiol diacetateThe therapeutic efficacy of Ximelagatran can be decreased when used in combination with Ethynodiol diacetate.Approved
EtodolacEtodolac may increase the anticoagulant activities of Ximelagatran.Approved, Investigational, Vet Approved
EtofenamateEtofenamate may increase the anticoagulant activities of Ximelagatran.Approved
EtonogestrelThe therapeutic efficacy of Ximelagatran can be decreased when used in combination with Etonogestrel.Approved, Investigational
EtoricoxibEtoricoxib may increase the anticoagulant activities of Ximelagatran.Approved, Investigational
EtravirineThe serum concentration of Etravirine can be decreased when it is combined with Ximelagatran.Approved
Evening primrose oilEvening primrose oil may increase the anticoagulant activities of Ximelagatran.Approved
exisulindexisulind may increase the anticoagulant activities of Ximelagatran.Investigational
FenbufenFenbufen may increase the anticoagulant activities of Ximelagatran.Approved
FenoprofenFenoprofen may increase the anticoagulant activities of Ximelagatran.Approved
FibrinolysinFibrinolysin may increase the anticoagulant activities of Ximelagatran.Approved
FloctafenineFloctafenine may increase the anticoagulant activities of Ximelagatran.Approved, Withdrawn
FloxuridineThe metabolism of Ximelagatran can be decreased when combined with Floxuridine.Approved
FluconazoleThe metabolism of Ximelagatran can be decreased when combined with Fluconazole.Approved
FluindioneXimelagatran may increase the anticoagulant activities of Fluindione.Investigational
FlunixinFlunixin may increase the anticoagulant activities of Ximelagatran.Vet Approved
FluorouracilThe metabolism of Ximelagatran can be decreased when combined with Fluorouracil.Approved
FlurbiprofenFlurbiprofen may increase the anticoagulant activities of Ximelagatran.Approved, Investigational
FluvastatinThe metabolism of Ximelagatran can be decreased when combined with Fluvastatin.Approved
FluvoxamineThe metabolism of Ximelagatran can be decreased when combined with Fluvoxamine.Approved, Investigational
FondaparinuxXimelagatran may increase the anticoagulant activities of Fondaparinux.Investigational
Fondaparinux sodiumFondaparinux sodium may increase the anticoagulant activities of Ximelagatran.Approved, Investigational
FosphenytoinThe metabolism of Ximelagatran can be increased when combined with Fosphenytoin.Approved
GabexateXimelagatran may increase the anticoagulant activities of Gabexate.Investigational
GarlicThe serum concentration of Ximelagatran can be decreased when it is combined with Garlic.Approved
GemfibrozilThe metabolism of Ximelagatran can be decreased when combined with Gemfibrozil.Approved
GenisteinGenistein may decrease the anticoagulant activities of Ximelagatran.Investigational
GestodeneThe therapeutic efficacy of Ximelagatran can be decreased when used in combination with Gestodene.Approved
GestrinoneThe therapeutic efficacy of Ximelagatran can be decreased when used in combination with Gestrinone.Approved
HeminHemin may increase the anticoagulant activities of Ximelagatran.Approved
HeparinHeparin may increase the anticoagulant activities of Ximelagatran.Approved, Investigational
HexestrolThe serum concentration of Hexestrol can be decreased when it is combined with Ximelagatran.Withdrawn
HigenamineHigenamine may increase the anticoagulant activities of Ximelagatran.Investigational
HirulogHirulog may increase the anticoagulant activities of Ximelagatran.Experimental
HMPL-004HMPL-004 may increase the anticoagulant activities of Ximelagatran.Investigational
Hydroxyprogesterone caproateThe therapeutic efficacy of Ximelagatran can be decreased when used in combination with Hydroxyprogesterone caproate.Approved
Ibritumomab tiuxetanThe risk or severity of adverse effects can be increased when Ximelagatran is combined with Ibritumomab tiuxetan.Approved
IbrutinibThe risk or severity of adverse effects can be increased when Ibrutinib is combined with Ximelagatran.Approved
IbudilastIbudilast may increase the anticoagulant activities of Ximelagatran.Approved, Investigational
IbuprofenIbuprofen may increase the anticoagulant activities of Ximelagatran.Approved
IbuproxamIbuproxam may increase the anticoagulant activities of Ximelagatran.Withdrawn
IcatibantIcatibant may increase the anticoagulant activities of Ximelagatran.Approved
Icosapent ethylIcosapent ethyl may increase the anticoagulant activities of Ximelagatran.Approved, Nutraceutical
idraparinuxXimelagatran may increase the anticoagulant activities of idraparinux.Investigational
IfenprodilIfenprodil may increase the anticoagulant activities of Ximelagatran.Approved, Withdrawn
IloprostIloprost may increase the anticoagulant activities of Ximelagatran.Approved, Investigational
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Ximelagatran.Approved
IndinavirThe metabolism of Ximelagatran can be decreased when combined with Indinavir.Approved
IndobufenIndobufen may increase the anticoagulant activities of Ximelagatran.Investigational
IndomethacinIndomethacin may increase the anticoagulant activities of Ximelagatran.Approved, Investigational
IndoprofenIndoprofen may increase the anticoagulant activities of Ximelagatran.Withdrawn
IrbesartanThe metabolism of Ximelagatran can be decreased when combined with Irbesartan.Approved, Investigational
IsoxicamIsoxicam may increase the anticoagulant activities of Ximelagatran.Withdrawn
Kct 0809Kct 0809 may increase the anticoagulant activities of Ximelagatran.Investigational
KebuzoneKebuzone may increase the anticoagulant activities of Ximelagatran.Experimental
KetanserinKetanserin may increase the anticoagulant activities of Ximelagatran.Investigational
KetoconazoleThe metabolism of Ximelagatran can be decreased when combined with Ketoconazole.Approved, Investigational
KetoprofenKetoprofen may increase the anticoagulant activities of Ximelagatran.Approved, Vet Approved
KetorolacKetorolac may increase the anticoagulant activities of Ximelagatran.Approved
LeflunomideThe metabolism of Ximelagatran can be decreased when combined with Leflunomide.Approved, Investigational
LepirudinLepirudin may increase the anticoagulant activities of Ximelagatran.Approved
LevonorgestrelThe therapeutic efficacy of Ximelagatran can be decreased when used in combination with Levonorgestrel.Approved, Investigational
LimaprostThe risk or severity of adverse effects can be increased when Limaprost is combined with Ximelagatran.Approved
LisofyllineLisofylline may increase the anticoagulant activities of Ximelagatran.Investigational
LornoxicamLornoxicam may increase the anticoagulant activities of Ximelagatran.Approved
LosartanThe metabolism of Ximelagatran can be decreased when combined with Losartan.Approved
LovastatinThe serum concentration of Lovastatin can be increased when it is combined with Ximelagatran.Approved, Investigational
LoxoprofenLoxoprofen may increase the anticoagulant activities of Ximelagatran.Approved
LumacaftorThe serum concentration of Ximelagatran can be decreased when it is combined with Lumacaftor.Approved
LumiracoxibLumiracoxib may increase the anticoagulant activities of Ximelagatran.Approved, Investigational
LynestrenolThe therapeutic efficacy of Ximelagatran can be decreased when used in combination with Lynestrenol.Investigational
Magnesium salicylateMagnesium salicylate may increase the anticoagulant activities of Ximelagatran.Approved
MasoprocolMasoprocol may increase the anticoagulant activities of Ximelagatran.Approved
Meclofenamic acidMeclofenamic acid may increase the anticoagulant activities of Ximelagatran.Approved, Vet Approved
MedrogestoneThe therapeutic efficacy of Ximelagatran can be decreased when used in combination with Medrogestone.Approved
Medroxyprogesterone acetateThe therapeutic efficacy of Ximelagatran can be decreased when used in combination with Medroxyprogesterone acetate.Approved, Investigational
Mefenamic acidMefenamic acid may increase the anticoagulant activities of Ximelagatran.Approved
Megestrol acetateThe therapeutic efficacy of Ximelagatran can be decreased when used in combination with Megestrol acetate.Approved, Vet Approved
MeloxicamMeloxicam may increase the anticoagulant activities of Ximelagatran.Approved, Vet Approved
MesalazineMesalazine may increase the anticoagulant activities of Ximelagatran.Approved
MestranolThe serum concentration of Mestranol can be decreased when it is combined with Ximelagatran.Approved
MetamizoleMetamizole may increase the anticoagulant activities of Ximelagatran.Withdrawn
MethallenestrilThe serum concentration of Methallenestril can be decreased when it is combined with Ximelagatran.Experimental
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Ximelagatran.Approved, Illicit
MifepristoneThe serum concentration of Ximelagatran can be increased when it is combined with Mifepristone.Approved, Investigational
MilrinoneMilrinone may increase the anticoagulant activities of Ximelagatran.Approved
MirtazapineThe serum concentration of Mirtazapine can be increased when it is combined with Ximelagatran.Approved
MizoribineMizoribine may increase the anticoagulant activities of Ximelagatran.Investigational
Mycophenolate mofetilMycophenolate mofetil may increase the anticoagulant activities of Ximelagatran.Approved, Investigational
Mycophenolic acidMycophenolic acid may increase the anticoagulant activities of Ximelagatran.Approved
NabumetoneNabumetone may increase the anticoagulant activities of Ximelagatran.Approved
NadroparinXimelagatran may increase the anticoagulant activities of Nadroparin.Approved
NafamostatNafamostat may increase the anticoagulant activities of Ximelagatran.Investigational
NaftifineNaftifine may increase the anticoagulant activities of Ximelagatran.Approved
NaftopidilNaftopidil may increase the anticoagulant activities of Ximelagatran.Investigational
NaproxenNaproxen may increase the anticoagulant activities of Ximelagatran.Approved, Vet Approved
NCX 4016NCX 4016 may increase the anticoagulant activities of Ximelagatran.Investigational
NefazodoneThe serum concentration of Nefazodone can be increased when it is combined with Ximelagatran.Approved, Withdrawn
NepafenacNepafenac may increase the anticoagulant activities of Ximelagatran.Approved
NicardipineThe metabolism of Ximelagatran can be decreased when combined with Nicardipine.Approved
Niflumic AcidNiflumic Acid may increase the anticoagulant activities of Ximelagatran.Approved
NimesulideNimesulide may increase the anticoagulant activities of Ximelagatran.Approved, Withdrawn
NintedanibThe risk or severity of adverse effects can be increased when Ximelagatran is combined with Nintedanib.Approved
NitroaspirinNitroaspirin may increase the anticoagulant activities of Ximelagatran.Investigational
NomegestrolThe therapeutic efficacy of Ximelagatran can be decreased when used in combination with Nomegestrol.Approved
NorethisteroneThe therapeutic efficacy of Ximelagatran can be decreased when used in combination with Norethisterone.Approved
NortriptylineThe serum concentration of Nortriptyline can be increased when it is combined with Ximelagatran.Approved
ObinutuzumabThe risk or severity of adverse effects can be increased when Ximelagatran is combined with Obinutuzumab.Approved
OlopatadineOlopatadine may increase the anticoagulant activities of Ximelagatran.Approved
OlsalazineOlsalazine may increase the anticoagulant activities of Ximelagatran.Approved
Omacetaxine mepesuccinateThe risk or severity of adverse effects can be increased when Ximelagatran is combined with Omacetaxine mepesuccinate.Approved
Omega-3 fatty acidsOmega-3 fatty acids may increase the anticoagulant activities of Ximelagatran.Approved
OmeprazoleThe metabolism of Ximelagatran can be decreased when combined with Omeprazole.Approved, Investigational, Vet Approved
OpipramolThe serum concentration of Opipramol can be increased when it is combined with Ximelagatran.Investigational
OrgoteinOrgotein may increase the anticoagulant activities of Ximelagatran.Vet Approved
OtamixabanXimelagatran may increase the anticoagulant activities of Otamixaban.Investigational
OxaprozinOxaprozin may increase the anticoagulant activities of Ximelagatran.Approved
OxyphenbutazoneOxyphenbutazone may increase the anticoagulant activities of Ximelagatran.Withdrawn
ParecoxibParecoxib may increase the anticoagulant activities of Ximelagatran.Approved
ParnaparinParnaparin may increase the anticoagulant activities of Ximelagatran.Approved
Pentosan PolysulfatePentosan Polysulfate may increase the anticoagulant activities of Ximelagatran.Approved
PentoxifyllinePentoxifylline may increase the anticoagulant activities of Ximelagatran.Approved, Investigational
PethidineThe risk or severity of adverse effects can be increased when Ximelagatran is combined with Pethidine.Approved
PhenindionePhenindione may increase the anticoagulant activities of Ximelagatran.Approved
PhenobarbitalThe metabolism of Ximelagatran can be increased when combined with Phenobarbital.Approved
PhenprocoumonPhenprocoumon may increase the anticoagulant activities of Ximelagatran.Approved
PhenylbutazonePhenylbutazone may increase the anticoagulant activities of Ximelagatran.Approved, Vet Approved
PhenytoinThe metabolism of Ximelagatran can be increased when combined with Phenytoin.Approved, Vet Approved
PimecrolimusPimecrolimus may increase the anticoagulant activities of Ximelagatran.Approved, Investigational
PimozideThe serum concentration of Pimozide can be increased when it is combined with Ximelagatran.Approved
PirfenidonePirfenidone may increase the anticoagulant activities of Ximelagatran.Investigational
PiroxicamPiroxicam may increase the anticoagulant activities of Ximelagatran.Approved, Investigational
PlasminPlasmin may increase the anticoagulant activities of Ximelagatran.Investigational
Polyestradiol phosphatePolyestradiol phosphate may decrease the anticoagulant activities of Ximelagatran.Approved
PrasugrelPrasugrel may increase the anticoagulant activities of Ximelagatran.Approved
PrimidoneThe metabolism of Ximelagatran can be increased when combined with Primidone.Approved, Vet Approved
ProgesteroneThe therapeutic efficacy of Ximelagatran can be decreased when used in combination with Progesterone.Approved, Vet Approved
PromestrienePromestriene may decrease the anticoagulant activities of Ximelagatran.Investigational
PropacetamolPropacetamol may increase the anticoagulant activities of Ximelagatran.Approved
Protein CXimelagatran may increase the anticoagulant activities of Protein C.Approved
Protein S humanXimelagatran may increase the anticoagulant activities of Protein S human.Approved
ProtocatechualdehydeXimelagatran may increase the anticoagulant activities of Protocatechualdehyde.Approved
ProtriptylineThe serum concentration of Protriptyline can be increased when it is combined with Ximelagatran.Approved
PTC299PTC299 may increase the anticoagulant activities of Ximelagatran.Investigational
PyrimethamineThe metabolism of Ximelagatran can be decreased when combined with Pyrimethamine.Approved, Vet Approved
QuinestrolQuinestrol may decrease the anticoagulant activities of Ximelagatran.Approved
QuinineThe metabolism of Ximelagatran can be decreased when combined with Quinine.Approved
RamatrobanRamatroban may increase the anticoagulant activities of Ximelagatran.Investigational
ResveratrolResveratrol may increase the anticoagulant activities of Ximelagatran.Experimental, Investigational
ReteplaseReteplase may increase the anticoagulant activities of Ximelagatran.Approved
ReviparinXimelagatran may increase the anticoagulant activities of Reviparin.Approved
RidogrelRidogrel may increase the anticoagulant activities of Ximelagatran.Approved
RifampicinThe metabolism of Ximelagatran can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Ximelagatran can be increased when combined with Rifapentine.Approved
RiociguatThe serum concentration of Riociguat can be increased when it is combined with Ximelagatran.Approved
RivaroxabanXimelagatran may increase the anticoagulant activities of Rivaroxaban.Approved
RofecoxibRofecoxib may increase the anticoagulant activities of Ximelagatran.Investigational, Withdrawn
RosiglitazoneRosiglitazone may increase the anticoagulant activities of Ximelagatran.Approved, Investigational
RosuvastatinThe serum concentration of Rosuvastatin can be increased when it is combined with Ximelagatran.Approved
S EquolS Equol may decrease the anticoagulant activities of Ximelagatran.Investigational
SalicylamideSalicylamide may increase the anticoagulant activities of Ximelagatran.Approved
Salicylic acidSalicylic acid may increase the anticoagulant activities of Ximelagatran.Approved, Vet Approved
SalsalateSalsalate may increase the anticoagulant activities of Ximelagatran.Approved
SCH-530348SCH-530348 may increase the anticoagulant activities of Ximelagatran.Investigational
SecobarbitalThe metabolism of Ximelagatran can be increased when combined with Secobarbital.Approved, Vet Approved
SecoisolariciresinolSecoisolariciresinol may decrease the anticoagulant activities of Ximelagatran.Investigational
SelexipagSelexipag may increase the anticoagulant activities of Ximelagatran.Approved
SeratrodastSeratrodast may increase the anticoagulant activities of Ximelagatran.Approved, Investigational
SevofluraneSevoflurane may increase the anticoagulant activities of Ximelagatran.Approved, Vet Approved
SildenafilThe serum concentration of Sildenafil can be increased when it is combined with Ximelagatran.Approved, Investigational
SimeprevirThe serum concentration of Simeprevir can be increased when it is combined with Ximelagatran.Approved
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Ximelagatran.Approved
SorafenibThe metabolism of Ximelagatran can be decreased when combined with Sorafenib.Approved, Investigational
SRT501SRT501 may increase the anticoagulant activities of Ximelagatran.Investigational
St. John's WortThe metabolism of Ximelagatran can be increased when combined with St. John's Wort.Nutraceutical
StreptokinaseStreptokinase may increase the anticoagulant activities of Ximelagatran.Approved
SugammadexSugammadex may increase the anticoagulant activities of Ximelagatran.Approved
SulfadiazineThe metabolism of Ximelagatran can be decreased when combined with Sulfadiazine.Approved, Vet Approved
SulfamethoxazoleThe metabolism of Ximelagatran can be decreased when combined with Sulfamethoxazole.Approved
SulfasalazineSulfasalazine may increase the anticoagulant activities of Ximelagatran.Approved
SulfisoxazoleThe metabolism of Ximelagatran can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SulindacSulindac may increase the anticoagulant activities of Ximelagatran.Approved
SulodexideXimelagatran may increase the anticoagulant activities of Sulodexide.Approved, Investigational
SuprofenSuprofen may increase the anticoagulant activities of Ximelagatran.Approved, Withdrawn
Synthetic Conjugated Estrogens, AThe serum concentration of Synthetic Conjugated Estrogens, A can be decreased when it is combined with Ximelagatran.Approved
Synthetic Conjugated Estrogens, BSynthetic Conjugated Estrogens, B may decrease the anticoagulant activities of Ximelagatran.Approved
TacrolimusThe metabolism of Tacrolimus can be decreased when combined with Ximelagatran.Approved, Investigational
TemsirolimusThe risk or severity of adverse effects can be increased when Ximelagatran is combined with Temsirolimus.Approved
TenecteplaseTenecteplase may increase the anticoagulant activities of Ximelagatran.Approved
TenoxicamTenoxicam may increase the anticoagulant activities of Ximelagatran.Approved
TepoxalinTepoxalin may increase the anticoagulant activities of Ximelagatran.Vet Approved
TeriflunomideTeriflunomide may increase the anticoagulant activities of Ximelagatran.Approved
TesmilifeneTesmilifene may increase the anticoagulant activities of Ximelagatran.Investigational
TheophyllineThe serum concentration of Theophylline can be decreased when it is combined with Ximelagatran.Approved
TianeptineThe serum concentration of Tianeptine can be increased when it is combined with Ximelagatran.Approved
Tiaprofenic acidTiaprofenic acid may increase the anticoagulant activities of Ximelagatran.Approved
TiboloneTibolone may increase the anticoagulant activities of Ximelagatran.Approved
TicagrelorThe metabolism of Ximelagatran can be decreased when combined with Ticagrelor.Approved
TiclopidineThe metabolism of Ximelagatran can be decreased when combined with Ticlopidine.Approved
TinoridineTinoridine may increase the anticoagulant activities of Ximelagatran.Investigational
TinzaparinTinzaparin may increase the anticoagulant activities of Ximelagatran.Approved
TipranavirThe serum concentration of Ximelagatran can be decreased when it is combined with Tipranavir.Approved, Investigational
TirofibanTirofiban may increase the anticoagulant activities of Ximelagatran.Approved
TolbutamideThe metabolism of Ximelagatran can be decreased when combined with Tolbutamide.Approved
Tolfenamic AcidTolfenamic Acid may increase the anticoagulant activities of Ximelagatran.Approved
TolmetinTolmetin may increase the anticoagulant activities of Ximelagatran.Approved
TositumomabThe risk or severity of adverse effects can be increased when Ximelagatran is combined with Tositumomab.Approved
TranilastTranilast may increase the anticoagulant activities of Ximelagatran.Approved, Investigational
TrapidilTrapidil may increase the anticoagulant activities of Ximelagatran.Approved
TreprostinilTreprostinil may increase the anticoagulant activities of Ximelagatran.Approved, Investigational
TriazolamThe serum concentration of Triazolam can be increased when it is combined with Ximelagatran.Approved
TriflusalTriflusal may increase the anticoagulant activities of Ximelagatran.Approved
TrimethoprimThe metabolism of Ximelagatran can be decreased when combined with Trimethoprim.Approved, Vet Approved
TrimipramineThe serum concentration of Trimipramine can be increased when it is combined with Ximelagatran.Approved
Trisalicylate-cholineTrisalicylate-choline may increase the anticoagulant activities of Ximelagatran.Approved
UrokinaseUrokinase may increase the anticoagulant activities of Ximelagatran.Approved, Investigational, Withdrawn
ValdecoxibValdecoxib may increase the anticoagulant activities of Ximelagatran.Investigational, Withdrawn
Valproic AcidThe serum concentration of Valproic Acid can be decreased when it is combined with Ximelagatran.Approved, Investigational
ValsartanThe metabolism of Ximelagatran can be decreased when combined with Valsartan.Approved, Investigational
VerapamilThe metabolism of Verapamil can be decreased when combined with Ximelagatran.Approved
Vitamin EVitamin E may increase the anticoagulant activities of Ximelagatran.Approved, Nutraceutical, Vet Approved
VorapaxarThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Ximelagatran.Approved
VoriconazoleThe metabolism of Ximelagatran can be decreased when combined with Voriconazole.Approved, Investigational
WarfarinWarfarin may increase the anticoagulant activities of Ximelagatran.Approved
Ym150Ximelagatran may increase the anticoagulant activities of Ym150.Investigational
ZafirlukastThe metabolism of Ximelagatran can be decreased when combined with Zafirlukast.Approved, Investigational
ZaltoprofenZaltoprofen may increase the anticoagulant activities of Ximelagatran.Approved
ZeranolZeranol may decrease the anticoagulant activities of Ximelagatran.Vet Approved
ZidovudineThe serum concentration of Zidovudine can be decreased when it is combined with Ximelagatran.Approved
ZileutonZileuton may increase the anticoagulant activities of Ximelagatran.Approved, Investigational, Withdrawn
ZomepiracZomepirac may increase the anticoagulant activities of Ximelagatran.Withdrawn
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General References
  1. Eriksson H, Wahlander K, Gustafsson D, Welin LT, Frison L, Schulman S: A randomized, controlled, dose-guiding study of the oral direct thrombin inhibitor ximelagatran compared with standard therapy for the treatment of acute deep vein thrombosis: THRIVE I. J Thromb Haemost. 2003 Jan;1(1):41-7. [PubMed:12871538 ]
  2. Weitz JI: New anticoagulants for treatment of venous thromboembolism. Circulation. 2004 Aug 31;110(9 Suppl 1):I19-26. [PubMed:15339877 ]
  3. Francis CW, Berkowitz SD, Comp PC, Lieberman JR, Ginsberg JS, Paiement G, Peters GR, Roth AW, McElhattan J, Colwell CW Jr: Comparison of ximelagatran with warfarin for the prevention of venous thromboembolism after total knee replacement. N Engl J Med. 2003 Oct 30;349(18):1703-12. [PubMed:14585938 ]
  4. Bergqvist D, Solhaug JH, Holmdahl L, Eriksson UG, Andersson M, Boberg B, Ogren M: Pharmacokinetics, preliminary efficacy and safety of subcutaneous melagatran and oral ximelagatran : a multicentre study of thromboprophylaxis in elective abdominal surgery. Clin Drug Investig. 2004;24(3):127-36. [PubMed:17516699 ]
  5. Koscielny J, Kiesewetter H, Jorg I, Harenberg J: Ximelagatran for treatment and prophylaxis of recurrent events in deep vein thrombosis. Clin Appl Thromb Hemost. 2007 Jul;13(3):299-307. [PubMed:17636192 ]
External Links
ATC CodesB01AE05
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.6065
Blood Brain Barrier-0.7499
Caco-2 permeable-0.7534
P-glycoprotein substrateSubstrate0.84
P-glycoprotein inhibitor INon-inhibitor0.755
P-glycoprotein inhibitor IINon-inhibitor0.947
Renal organic cation transporterNon-inhibitor0.7588
CYP450 2C9 substrateNon-substrate0.8632
CYP450 2D6 substrateNon-substrate0.8163
CYP450 3A4 substrateNon-substrate0.597
CYP450 1A2 substrateNon-inhibitor0.8409
CYP450 2C9 inhibitorNon-inhibitor0.7261
CYP450 2D6 inhibitorNon-inhibitor0.844
CYP450 2C19 inhibitorNon-inhibitor0.669
CYP450 3A4 inhibitorNon-inhibitor0.6775
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9157
Ames testNon AMES toxic0.6238
CarcinogenicityNon-carcinogens0.7863
BiodegradationNot ready biodegradable0.8515
Rat acute toxicity2.4109 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9654
hERG inhibition (predictor II)Inhibitor0.6003
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental PropertiesNot Available
Predicted Properties
PropertyValueSource
Water Solubility0.0845 mg/mLALOGPS
logP1.35ALOGPS
logP0.87ChemAxon
logS-3.8ALOGPS
pKa (Strongest Acidic)9.64ChemAxon
pKa (Strongest Basic)5.48ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count7ChemAxon
Hydrogen Donor Count4ChemAxon
Polar Surface Area146.35 Å2ChemAxon
Rotatable Bond Count11ChemAxon
Refractivity126.57 m3·mol-1ChemAxon
Polarizability52.15 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as alpha amino acid esters. These are ester derivatives of alpha amino acids.
KingdomOrganic compounds
Super ClassOrganic acids and derivatives
ClassCarboxylic acids and derivatives
Sub ClassAmino acids, peptides, and analogues
Direct ParentAlpha amino acid esters
Alternative Parents
Substituents
  • Alpha-amino acid ester
  • Alpha-amino acid amide
  • Phenylmethylamine
  • Benzylamine
  • Benzenoid
  • Monocyclic benzene moiety
  • Amidoxime
  • Tertiary carboxylic acid amide
  • Tertiary amine
  • Secondary carboxylic acid amide
  • Carboxylic acid ester
  • Carboxamide group
  • Azetidine
  • Amidoxime group
  • Azacycle
  • Organoheterocyclic compound
  • Secondary amine
  • Monocarboxylic acid or derivatives
  • Secondary aliphatic amine
  • Carboxylic acid amide
  • Amidine
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External Descriptors

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Thrombospondin receptor activity
Specific Function:
Thrombin, which cleaves bonds after Arg and Lys, converts fibrinogen to fibrin and activates factors V, VII, VIII, XIII, and, in complex with thrombomodulin, protein C. Functions in blood homeostasis, inflammation and wound healing.
Gene Name:
F2
Uniprot ID:
P00734
Molecular Weight:
70036.295 Da
References
  1. Testa L, Bhindi R, Agostoni P, Abbate A, Zoccai GG, van Gaal WJ: The direct thrombin inhibitor ximelagatran/melagatran: a systematic review on clinical applications and an evidence based assessment of risk benefit profile. Expert Opin Drug Saf. 2007 Jul;6(4):397-406. [PubMed:17688383 ]
  2. Ho SJ, Brighton TA: Ximelagatran: direct thrombin inhibitor. Vasc Health Risk Manag. 2006;2(1):49-58. [PubMed:17319469 ]
  3. Bergqvist D, Solhaug JH, Holmdahl L, Eriksson UG, Andersson M, Boberg B, Ogren M: Pharmacokinetics, preliminary efficacy and safety of subcutaneous melagatran and oral ximelagatran : a multicentre study of thromboprophylaxis in elective abdominal surgery. Clin Drug Investig. 2004;24(3):127-36. [PubMed:17516699 ]
  4. Ersdal E, Schutzer KM, Lonnerstedt C, Ohlsson L, Wall U, Eriksson UG: No influence of food on the pharmacokinetics, pharmacodynamics or tolerability of the 24mg and 36mg oral tablet formulations of ximelagatran. Clin Drug Investig. 2005;25(7):425-33. [PubMed:17532684 ]
  5. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Comments
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Drug created on October 21, 2007 16:23 / Updated on August 17, 2016 12:24