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Identification
NameLepirudin
Accession NumberDB00001  (BTD00024, BIOD00024)
TypeBiotech
GroupsApproved
DescriptionLepirudin is identical to natural hirudin except for substitution of leucine for isoleucine at the N-terminal end of the molecule and the absence of a sulfate group on the tyrosine at position 63. It is produced via yeast cells. Bayer ceased the production of lepirudin (Refludan) effective May 31, 2012.
Protein structureDb00001
Related Articles
Protein chemical formulaC287H440N80O110S6
Protein average weight6963.425 Da
Sequences
>DB00001 sequence
LVYTDCTESGQNLCLCEGSNVCGQGNKCILGSDGEKNQCVTGEGTPKPQSHNDGDFEEIP
EEYLQ
Download FASTA Format
Synonyms
Hirudin variant-1
Lepirudin recombinant
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
RefludanPowder, for solution50 mgIntravenousBayer Inc2000-01-312013-07-26Canada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
RefludanInjection, solution, concentrate50 mgIntravenousCelgene Europe Ltd.1997-03-13Not applicableEu
RefludanInjection, solution, concentrate50 mgIntravenousCelgene Europe Ltd.1997-03-13Not applicableEu
RefludanInjection, solution, concentrate20 mgIntravenousCelgene Europe Ltd.1997-03-13Not applicableEu
RefludanInjection, solution, concentrate20 mgIntravenousCelgene Europe Ltd.1997-03-13Not applicableEu
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIY43GF64R34
CAS number138068-37-8
Pharmacology
IndicationFor the treatment of heparin-induced thrombocytopenia
Structured Indications Not Available
PharmacodynamicsLepirudin is used to break up clots and to reduce thrombocytopenia. It binds to thrombin and prevents thrombus or clot formation. It is a highly potent, selective, and essentially irreversible inhibitor of thrombin and clot-bond thrombin. Lepirudin requires no cofactor for its anticoagulant action. Lepirudin is a recombinant form of hirudin, an endogenous anticoagulant found in medicinal leeches.
Mechanism of actionLepirudin forms a stable non-covalent complex with alpha-thrombin, thereby abolishing its ability to cleave fibrinogen and initiate the clotting cascade. The inhibition of thrombin prevents the blood clotting cascade.
TargetKindPharmacological actionActionsOrganismUniProt ID
ProthrombinProteinyes
inhibitor
HumanP00734 details
Related Articles
AbsorptionBioavailability is 100% following injection.
Volume of distribution
  • 12.2 L [Healthy young subjects (n = 18, age 18-60 years)]
  • 18.7 L [Healthy elderly subjects (n = 10, age 65-80 years)]
  • 18 L [Renally impaired patients (n = 16, creatinine clearance below 80 mL/min)]
  • 32.1 L [HIT patients (n = 73)]
Protein bindingNot Available
Metabolism

Lepirudin is thought to be metabolized by release of amino acids via catabolic hydrolysis of the parent drug. However, con-clusive data are not available. About 48% of the administration dose is excreted in the urine which consists of unchanged drug (35%) and other fragments of the parent drug.

Route of eliminationLepirudin is thought to be metabolized by release of amino acids via catabolic hydrolysis of the parent drug. About 48% of the administration dose is excreted in the urine which consists of unchanged drug (35%) and other fragments of the parent drug.
Half lifeApproximately 1.3 hours
Clearance
  • 164 ml/min [Healthy 18-60 yrs]
  • 139 ml/min [Healthy 65-80 yrs]
  • 61 ml/min [renal impaired]
  • 114 ml/min [HIT (Heparin-induced thrombocytopenia)]
ToxicityIn case of overdose (eg, suggested by excessively high aPTT values) the risk of bleeding is increased.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Lepirudin Action PathwayDrug actionSMP00278
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 Lepirudin.Approved, Investigational
AbciximabLepirudin may increase the anticoagulant activities of Abciximab.Approved
AceclofenacAceclofenac may increase the anticoagulant activities of Lepirudin.Approved
AcenocoumarolLepirudin may increase the anticoagulant activities of Acenocoumarol.Approved
AcetovanilloneAcetovanillone may increase the anticoagulant activities of Lepirudin.Investigational
Acetylsalicylic acidAcetylsalicylic acid may increase the anticoagulant activities of Lepirudin.Approved, Vet Approved
AdapaleneAdapalene may increase the anticoagulant activities of Lepirudin.Approved
AlfuzosinThe serum concentration of Alfuzosin can be increased when it is combined with Lepirudin.Approved, Investigational
AllylestrenolThe therapeutic efficacy of Lepirudin can be decreased when used in combination with Allylestrenol.Approved
AlprazolamThe serum concentration of Alprazolam can be increased when it is combined with Lepirudin.Approved, Illicit, Investigational
AlprostadilAlprostadil may increase the anticoagulant activities of Lepirudin.Approved, Investigational
AlteplaseAlteplase may increase the anticoagulant activities of Lepirudin.Approved
AltrenogestThe therapeutic efficacy of Lepirudin can be decreased when used in combination with Altrenogest.Vet Approved
ALX-0081ALX-0081 may increase the anticoagulant activities of Lepirudin.Investigational
Ambroxol acefyllinateThe serum concentration of Ambroxol acefyllinate can be decreased when it is combined with Lepirudin.Experimental
AmineptineThe serum concentration of Amineptine can be increased when it is combined with Lepirudin.Illicit, Withdrawn
AminophyllineThe serum concentration of Aminophylline can be decreased when it is combined with Lepirudin.Approved
Aminosalicylic AcidAminosalicylic Acid may increase the anticoagulant activities of Lepirudin.Approved
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Lepirudin.Approved
AnagrelideAnagrelide may increase the anticoagulant activities of Lepirudin.Approved
AncrodLepirudin may increase the anticoagulant activities of Ancrod.Investigational
AnisodamineAnisodamine may increase the anticoagulant activities of Lepirudin.Investigational
AnistreplaseAnistreplase may increase the anticoagulant activities of Lepirudin.Approved
AntipyrineAntipyrine may increase the anticoagulant activities of Lepirudin.Approved
Antithrombin III humanLepirudin may increase the anticoagulant activities of Antithrombin III human.Approved
ApixabanApixaban may increase the anticoagulant activities of Lepirudin.Approved
ApremilastApremilast may increase the anticoagulant activities of Lepirudin.Approved, Investigational
AprotininThe therapeutic efficacy of Lepirudin can be decreased when used in combination with Aprotinin.Approved, Withdrawn
ArdeparinLepirudin may increase the anticoagulant activities of Ardeparin.Approved, Withdrawn
ArgatrobanLepirudin may increase the anticoagulant activities of Argatroban.Approved, Investigational
AstaxanthinAstaxanthin may increase the anticoagulant activities of Lepirudin.Investigational
AtorvastatinThe serum concentration of Atorvastatin can be increased when it is combined with Lepirudin.Approved
AzapropazoneAzapropazone may increase the anticoagulant activities of Lepirudin.Withdrawn
AzelastineAzelastine may increase the anticoagulant activities of Lepirudin.Approved
BalsalazideBalsalazide may increase the anticoagulant activities of Lepirudin.Approved, Investigational
BatroxobinBatroxobin may increase the anticoagulant activities of Lepirudin.Experimental
BazedoxifeneBazedoxifene may decrease the anticoagulant activities of Lepirudin.Approved, Investigational
BecaplerminLepirudin may increase the anticoagulant activities of Becaplermin.Approved, Investigational
BemiparinBemiparin may increase the anticoagulant activities of Lepirudin.Approved
BenoxaprofenBenoxaprofen may increase the anticoagulant activities of Lepirudin.Withdrawn
BeraprostBeraprost may increase the anticoagulant activities of Lepirudin.Investigational
Betulinic AcidBetulinic Acid may increase the anticoagulant activities of Lepirudin.Investigational
BivalirudinLepirudin may increase the anticoagulant activities of Bivalirudin.Approved, Investigational
BoceprevirThe serum concentration of Lepirudin can be decreased when it is combined with Boceprevir.Approved
BromfenacBromfenac may increase the anticoagulant activities of Lepirudin.Approved
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Lepirudin.Approved, Investigational
BucillamineBucillamine may increase the anticoagulant activities of Lepirudin.Investigational
ButylphthalideButylphthalide may increase the anticoagulant activities of Lepirudin.Investigational
CabergolineThe serum concentration of Cabergoline can be increased when it is combined with Lepirudin.Approved
CangrelorCangrelor may increase the anticoagulant activities of Lepirudin.Approved
CarbamazepineThe metabolism of Lepirudin can be increased when combined with Carbamazepine.Approved, Investigational
CarprofenCarprofen may increase the anticoagulant activities of Lepirudin.Approved, Vet Approved, Withdrawn
CastanospermineCastanospermine may increase the anticoagulant activities of Lepirudin.Experimental
CelecoxibCelecoxib may increase the anticoagulant activities of Lepirudin.Approved, Investigational
CertoparinLepirudin may increase the anticoagulant activities of Certoparin.Approved
ChloroquineChloroquine may increase the anticoagulant activities of Lepirudin.Approved, Vet Approved
ChlorotrianiseneThe serum concentration of Chlorotrianisene can be decreased when it is combined with Lepirudin.Withdrawn
CilostazolCilostazol may increase the anticoagulant activities of Lepirudin.Approved
CisaprideThe serum concentration of Cisapride can be increased when it is combined with Lepirudin.Approved, Investigational, Withdrawn
Citric AcidLepirudin may increase the anticoagulant activities of Citric Acid.Nutraceutical, Vet Approved
ClarithromycinThe therapeutic efficacy of Clarithromycin can be decreased when used in combination with Lepirudin.Approved
ClomipramineThe serum concentration of Clomipramine can be increased when it is combined with Lepirudin.Approved, Vet Approved
ClonixinClonixin may increase the anticoagulant activities of Lepirudin.Approved
ClopidogrelClopidogrel may increase the anticoagulant activities of Lepirudin.Approved, Nutraceutical
CollagenaseThe risk or severity of adverse effects can be increased when Lepirudin is combined with Collagenase.Approved
Conjugated Equine EstrogensThe serum concentration of Conjugated Equine Estrogens can be decreased when it is combined with Lepirudin.Approved
CurcuminCurcumin may increase the anticoagulant activities of Lepirudin.Investigational
CyclobenzaprineThe serum concentration of Cyclobenzaprine can be increased when it is combined with Lepirudin.Approved
CyclophosphamideThe risk or severity of adverse effects can be increased when Lepirudin is combined with Cyclophosphamide.Approved, Investigational
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Lepirudin.Approved, Investigational, Vet Approved
D-LimoneneD-Limonene may increase the anticoagulant activities of Lepirudin.Investigational
Dabigatran etexilateDabigatran etexilate may increase the anticoagulant activities of Lepirudin.Approved
DalteparinLepirudin may increase the anticoagulant activities of Dalteparin.Approved
DanaparoidLepirudin may increase the anticoagulant activities of Danaparoid.Approved, Withdrawn
DasatinibDasatinib may increase the anticoagulant activities of Lepirudin.Approved, Investigational
DeferasiroxThe risk or severity of adverse effects can be increased when Lepirudin is combined with Deferasirox.Approved, Investigational
DefibrotideDefibrotide may increase the anticoagulant activities of Lepirudin.Approved, Investigational
DelavirdineThe serum concentration of Delavirdine can be decreased when it is combined with Lepirudin.Approved
Deoxycholic AcidThe risk or severity of adverse effects can be increased when Lepirudin is combined with Deoxycholic Acid.Approved
dersalazinedersalazine may increase the anticoagulant activities of Lepirudin.Investigational
DesipramineThe serum concentration of Desipramine can be increased when it is combined with Lepirudin.Approved
DesirudinLepirudin may increase the anticoagulant activities of Desirudin.Approved
DesmoteplaseDesmoteplase may increase the anticoagulant activities of Lepirudin.Investigational
DesogestrelThe therapeutic efficacy of Lepirudin can be decreased when used in combination with Desogestrel.Approved
DextranLepirudin may increase the anticoagulant activities of Dextran.Approved, Vet Approved
Dextran 40Lepirudin may increase the anticoagulant activities of Dextran 40.Approved
Dextran 70Lepirudin may increase the anticoagulant activities of Dextran 70.Approved
Dextran 75Lepirudin may increase the anticoagulant activities of Dextran 75.Approved
DiclofenacDiclofenac may increase the anticoagulant activities of Lepirudin.Approved, Vet Approved
DicoumarolLepirudin may increase the anticoagulant activities of Dicoumarol.Approved
DienestrolThe serum concentration of Dienestrol can be decreased when it is combined with Lepirudin.Approved
DienogestThe therapeutic efficacy of Lepirudin can be decreased when used in combination with Dienogest.Approved
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be decreased when it is combined with Lepirudin.Approved
DiflunisalDiflunisal may increase the anticoagulant activities of Lepirudin.Approved
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Lepirudin.Approved
DihydroergotamineThe serum concentration of Dihydroergotamine can be increased when it is combined with Lepirudin.Approved
DiltiazemThe metabolism of Diltiazem can be decreased when combined with Lepirudin.Approved
DipyridamoleDipyridamole may increase the anticoagulant activities of Lepirudin.Approved
DitazoleDitazole may increase the anticoagulant activities of Lepirudin.Approved, Withdrawn
DosulepinThe serum concentration of Dosulepin can be increased when it is combined with Lepirudin.Approved
DoxepinThe serum concentration of Doxepin can be increased when it is combined with Lepirudin.Approved
DrospirenoneThe therapeutic efficacy of Lepirudin can be decreased when used in combination with Drospirenone.Approved
Drotrecogin alfaDrotrecogin alfa may increase the anticoagulant activities of Lepirudin.Approved, Investigational, Withdrawn
DroxicamDroxicam may increase the anticoagulant activities of Lepirudin.Approved
DuvelisibDuvelisib may increase the anticoagulant activities of Lepirudin.Investigational
DydrogesteroneThe therapeutic efficacy of Lepirudin can be decreased when used in combination with Dydrogesterone.Approved, Withdrawn
DyphyllineThe serum concentration of Dyphylline can be decreased when it is combined with Lepirudin.Approved
E6201E6201 may increase the anticoagulant activities of Lepirudin.Investigational
EbselenEbselen may increase the anticoagulant activities of Lepirudin.Investigational
Edetic AcidLepirudin may increase the anticoagulant activities of Edetic Acid.Approved, Vet Approved
EdoxabanEdoxaban may increase the anticoagulant activities of Lepirudin.Approved
EnfuvirtideThe serum concentration of Enfuvirtide can be increased when it is combined with Lepirudin.Approved, Investigational
EnoxaparinLepirudin may increase the anticoagulant activities of Enoxaparin.Approved
EpinastineEpinastine may increase the anticoagulant activities of Lepirudin.Approved, Investigational
EpirizoleEpirizole may increase the anticoagulant activities of Lepirudin.Approved
eplivanserineeplivanserine may increase the anticoagulant activities of Lepirudin.Investigational
EpoprostenolEpoprostenol may increase the anticoagulant activities of Lepirudin.Approved
EptifibatideEptifibatide may increase the anticoagulant activities of Lepirudin.Approved, Investigational
Ergoloid mesylateThe serum concentration of Ergoloid mesylate can be increased when it is combined with Lepirudin.Approved
ErgonovineThe serum concentration of Ergonovine can be increased when it is combined with Lepirudin.Approved
ErgotamineThe serum concentration of Ergotamine can be increased when it is combined with Lepirudin.Approved
EsmirtazapineThe serum concentration of Esmirtazapine can be increased when it is combined with Lepirudin.Investigational
EstradiolThe serum concentration of Estradiol can be decreased when it is combined with Lepirudin.Approved, Investigational, Vet Approved
EstramustineThe serum concentration of Estramustine can be decreased when it is combined with Lepirudin.Approved
EstriolEstriol may decrease the anticoagulant activities of Lepirudin.Approved, Vet Approved
Estrogens, esterifiedThe serum concentration of Estrogens, esterified can be decreased when it is combined with Lepirudin.Approved
EstroneEstrone may decrease the anticoagulant activities of Lepirudin.Approved
Estrone sulfateThe serum concentration of Estrone sulfate can be decreased when it is combined with Lepirudin.Approved
EtanerceptEtanercept may increase the anticoagulant activities of Lepirudin.Approved, Investigational
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be decreased when it is combined with Lepirudin.Approved
Ethyl biscoumacetateLepirudin may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
Ethynodiol diacetateThe therapeutic efficacy of Lepirudin can be decreased when used in combination with Ethynodiol diacetate.Approved
EtodolacEtodolac may increase the anticoagulant activities of Lepirudin.Approved, Investigational, Vet Approved
EtofenamateEtofenamate may increase the anticoagulant activities of Lepirudin.Approved
EtonogestrelThe therapeutic efficacy of Lepirudin can be decreased when used in combination with Etonogestrel.Approved, Investigational
EtoricoxibEtoricoxib may increase the anticoagulant activities of Lepirudin.Approved, Investigational
EtravirineThe serum concentration of Etravirine can be decreased when it is combined with Lepirudin.Approved
Evening primrose oilEvening primrose oil may increase the anticoagulant activities of Lepirudin.Approved
exisulindexisulind may increase the anticoagulant activities of Lepirudin.Investigational
FenbufenFenbufen may increase the anticoagulant activities of Lepirudin.Approved
FenoprofenFenoprofen may increase the anticoagulant activities of Lepirudin.Approved
FibrinolysinFibrinolysin may increase the anticoagulant activities of Lepirudin.Approved
FloctafenineFloctafenine may increase the anticoagulant activities of Lepirudin.Approved, Withdrawn
FluindioneLepirudin may increase the anticoagulant activities of Fluindione.Investigational
FlunixinFlunixin may increase the anticoagulant activities of Lepirudin.Vet Approved
FlurbiprofenFlurbiprofen may increase the anticoagulant activities of Lepirudin.Approved, Investigational
FondaparinuxLepirudin may increase the anticoagulant activities of Fondaparinux.Investigational
Fondaparinux sodiumLepirudin may increase the anticoagulant activities of Fondaparinux sodium.Approved, Investigational
GabexateLepirudin may increase the anticoagulant activities of Gabexate.Investigational
GarlicThe serum concentration of Lepirudin can be decreased when it is combined with Garlic.Approved
GenisteinGenistein may decrease the anticoagulant activities of Lepirudin.Investigational
GestodeneThe therapeutic efficacy of Lepirudin can be decreased when used in combination with Gestodene.Approved
GestrinoneThe therapeutic efficacy of Lepirudin can be decreased when used in combination with Gestrinone.Approved
HeminHemin may increase the anticoagulant activities of Lepirudin.Approved
HeparinLepirudin may increase the anticoagulant activities of Heparin.Approved, Investigational
HexestrolThe serum concentration of Hexestrol can be decreased when it is combined with Lepirudin.Withdrawn
HigenamineHigenamine may increase the anticoagulant activities of Lepirudin.Investigational
HirulogLepirudin may increase the anticoagulant activities of Hirulog.Experimental
HMPL-004HMPL-004 may increase the anticoagulant activities of Lepirudin.Investigational
Hydroxyprogesterone caproateThe therapeutic efficacy of Lepirudin can be decreased when used in combination with Hydroxyprogesterone caproate.Approved
Ibritumomab tiuxetanThe risk or severity of adverse effects can be increased when Lepirudin is combined with Ibritumomab tiuxetan.Approved
IbrutinibThe risk or severity of adverse effects can be increased when Ibrutinib is combined with Lepirudin.Approved
IbudilastIbudilast may increase the anticoagulant activities of Lepirudin.Approved, Investigational
IbuprofenIbuprofen may increase the anticoagulant activities of Lepirudin.Approved
IbuproxamIbuproxam may increase the anticoagulant activities of Lepirudin.Withdrawn
IcatibantIcatibant may increase the anticoagulant activities of Lepirudin.Approved
Icosapent ethylIcosapent ethyl may increase the anticoagulant activities of Lepirudin.Approved, Nutraceutical
idraparinuxLepirudin may increase the anticoagulant activities of idraparinux.Investigational
IfenprodilIfenprodil may increase the anticoagulant activities of Lepirudin.Approved, Withdrawn
IloprostIloprost may increase the anticoagulant activities of Lepirudin.Approved, Investigational
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Lepirudin.Approved
IndobufenIndobufen may increase the anticoagulant activities of Lepirudin.Investigational
IndomethacinIndomethacin may increase the anticoagulant activities of Lepirudin.Approved, Investigational
IndoprofenIndoprofen may increase the anticoagulant activities of Lepirudin.Withdrawn
IsoxicamIsoxicam may increase the anticoagulant activities of Lepirudin.Withdrawn
Kct 0809Kct 0809 may increase the anticoagulant activities of Lepirudin.Investigational
KebuzoneKebuzone may increase the anticoagulant activities of Lepirudin.Experimental
KetanserinKetanserin may increase the anticoagulant activities of Lepirudin.Investigational
KetoprofenKetoprofen may increase the anticoagulant activities of Lepirudin.Approved, Vet Approved
KetorolacKetorolac may increase the anticoagulant activities of Lepirudin.Approved
LeflunomideLeflunomide may increase the anticoagulant activities of Lepirudin.Approved, Investigational
LevonorgestrelThe therapeutic efficacy of Lepirudin 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 Lepirudin.Approved
LisofyllineLisofylline may increase the anticoagulant activities of Lepirudin.Investigational
LornoxicamLornoxicam may increase the anticoagulant activities of Lepirudin.Approved
LovastatinThe serum concentration of Lovastatin can be increased when it is combined with Lepirudin.Approved, Investigational
LoxoprofenLoxoprofen may increase the anticoagulant activities of Lepirudin.Approved
LumiracoxibLumiracoxib may increase the anticoagulant activities of Lepirudin.Approved, Investigational
LynestrenolThe therapeutic efficacy of Lepirudin can be decreased when used in combination with Lynestrenol.Investigational
Magnesium salicylateMagnesium salicylate may increase the anticoagulant activities of Lepirudin.Approved
MasoprocolMasoprocol may increase the anticoagulant activities of Lepirudin.Approved
Meclofenamic acidMeclofenamic acid may increase the anticoagulant activities of Lepirudin.Approved, Vet Approved
MedrogestoneThe therapeutic efficacy of Lepirudin can be decreased when used in combination with Medrogestone.Approved
Medroxyprogesterone acetateThe therapeutic efficacy of Lepirudin can be decreased when used in combination with Medroxyprogesterone acetate.Approved, Investigational
Mefenamic acidMefenamic acid may increase the anticoagulant activities of Lepirudin.Approved
Megestrol acetateThe therapeutic efficacy of Lepirudin can be decreased when used in combination with Megestrol acetate.Approved, Vet Approved
MeloxicamMeloxicam may increase the anticoagulant activities of Lepirudin.Approved, Vet Approved
MesalazineMesalazine may increase the anticoagulant activities of Lepirudin.Approved
MestranolThe serum concentration of Mestranol can be decreased when it is combined with Lepirudin.Approved
MetamizoleMetamizole may increase the anticoagulant activities of Lepirudin.Withdrawn
MethallenestrilThe serum concentration of Methallenestril can be decreased when it is combined with Lepirudin.Experimental
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Lepirudin.Approved, Illicit
MilrinoneMilrinone may increase the anticoagulant activities of Lepirudin.Approved
MirtazapineThe serum concentration of Mirtazapine can be increased when it is combined with Lepirudin.Approved
MizoribineMizoribine may increase the anticoagulant activities of Lepirudin.Investigational
Mycophenolate mofetilMycophenolate mofetil may increase the anticoagulant activities of Lepirudin.Approved, Investigational
Mycophenolic acidMycophenolic acid may increase the anticoagulant activities of Lepirudin.Approved
NabumetoneNabumetone may increase the anticoagulant activities of Lepirudin.Approved
NadroparinLepirudin may increase the anticoagulant activities of Nadroparin.Approved
NafamostatNafamostat may increase the anticoagulant activities of Lepirudin.Investigational
NaftifineNaftifine may increase the anticoagulant activities of Lepirudin.Approved
NaftopidilNaftopidil may increase the anticoagulant activities of Lepirudin.Investigational
NaproxenNaproxen may increase the anticoagulant activities of Lepirudin.Approved, Vet Approved
NCX 4016NCX 4016 may increase the anticoagulant activities of Lepirudin.Investigational
NefazodoneThe serum concentration of Nefazodone can be increased when it is combined with Lepirudin.Approved, Withdrawn
NepafenacNepafenac may increase the anticoagulant activities of Lepirudin.Approved
Niflumic AcidNiflumic Acid may increase the anticoagulant activities of Lepirudin.Approved
NimesulideNimesulide may increase the anticoagulant activities of Lepirudin.Approved, Withdrawn
NintedanibThe risk or severity of adverse effects can be increased when Lepirudin is combined with Nintedanib.Approved
NitroaspirinNitroaspirin may increase the anticoagulant activities of Lepirudin.Investigational
NomegestrolThe therapeutic efficacy of Lepirudin can be decreased when used in combination with Nomegestrol.Approved
NorethisteroneThe therapeutic efficacy of Lepirudin can be decreased when used in combination with Norethisterone.Approved
NortriptylineThe serum concentration of Nortriptyline can be increased when it is combined with Lepirudin.Approved
ObinutuzumabThe risk or severity of adverse effects can be increased when Lepirudin is combined with Obinutuzumab.Approved
OlopatadineOlopatadine may increase the anticoagulant activities of Lepirudin.Approved
OlsalazineOlsalazine may increase the anticoagulant activities of Lepirudin.Approved
Omacetaxine mepesuccinateThe risk or severity of adverse effects can be increased when Lepirudin is combined with Omacetaxine mepesuccinate.Approved
Omega-3 fatty acidsOmega-3 fatty acids may increase the anticoagulant activities of Lepirudin.Approved
OpipramolThe serum concentration of Opipramol can be increased when it is combined with Lepirudin.Investigational
OrgoteinOrgotein may increase the anticoagulant activities of Lepirudin.Vet Approved
OtamixabanLepirudin may increase the anticoagulant activities of Otamixaban.Investigational
OxaprozinOxaprozin may increase the anticoagulant activities of Lepirudin.Approved
OxyphenbutazoneOxyphenbutazone may increase the anticoagulant activities of Lepirudin.Withdrawn
ParecoxibParecoxib may increase the anticoagulant activities of Lepirudin.Approved
ParnaparinParnaparin may increase the anticoagulant activities of Lepirudin.Approved
Pentosan PolysulfatePentosan Polysulfate may increase the anticoagulant activities of Lepirudin.Approved
PentoxifyllinePentoxifylline may increase the anticoagulant activities of Lepirudin.Approved, Investigational
PethidineThe risk or severity of adverse effects can be increased when Lepirudin is combined with Pethidine.Approved
PhenindioneLepirudin may increase the anticoagulant activities of Phenindione.Approved
PhenprocoumonLepirudin may increase the anticoagulant activities of Phenprocoumon.Approved
PhenylbutazonePhenylbutazone may increase the anticoagulant activities of Lepirudin.Approved, Vet Approved
PimecrolimusPimecrolimus may increase the anticoagulant activities of Lepirudin.Approved, Investigational
PimozideThe serum concentration of Pimozide can be increased when it is combined with Lepirudin.Approved
PirfenidonePirfenidone may increase the anticoagulant activities of Lepirudin.Investigational
PiroxicamPiroxicam may increase the anticoagulant activities of Lepirudin.Approved, Investigational
PlasminPlasmin may increase the anticoagulant activities of Lepirudin.Investigational
Polyestradiol phosphatePolyestradiol phosphate may decrease the anticoagulant activities of Lepirudin.Approved
PrasugrelPrasugrel may increase the anticoagulant activities of Lepirudin.Approved
ProgesteroneThe therapeutic efficacy of Lepirudin can be decreased when used in combination with Progesterone.Approved, Vet Approved
PromestrienePromestriene may decrease the anticoagulant activities of Lepirudin.Investigational
PropacetamolPropacetamol may increase the anticoagulant activities of Lepirudin.Approved
Protein CLepirudin may increase the anticoagulant activities of Protein C.Approved
Protein S humanLepirudin may increase the anticoagulant activities of Protein S human.Approved
ProtocatechualdehydeLepirudin may increase the anticoagulant activities of Protocatechualdehyde.Approved
ProtriptylineThe serum concentration of Protriptyline can be increased when it is combined with Lepirudin.Approved
PTC299PTC299 may increase the anticoagulant activities of Lepirudin.Investigational
QuinestrolQuinestrol may decrease the anticoagulant activities of Lepirudin.Approved
RamatrobanRamatroban may increase the anticoagulant activities of Lepirudin.Investigational
ResveratrolResveratrol may increase the anticoagulant activities of Lepirudin.Experimental, Investigational
ReteplaseReteplase may increase the anticoagulant activities of Lepirudin.Approved
ReviparinLepirudin may increase the anticoagulant activities of Reviparin.Approved
RidogrelRidogrel may increase the anticoagulant activities of Lepirudin.Approved
RiociguatThe serum concentration of Riociguat can be increased when it is combined with Lepirudin.Approved
RivaroxabanLepirudin may increase the anticoagulant activities of Rivaroxaban.Approved
RofecoxibRofecoxib may increase the anticoagulant activities of Lepirudin.Investigational, Withdrawn
RosiglitazoneRosiglitazone may increase the anticoagulant activities of Lepirudin.Approved, Investigational
RosuvastatinThe serum concentration of Rosuvastatin can be increased when it is combined with Lepirudin.Approved
S EquolS Equol may decrease the anticoagulant activities of Lepirudin.Investigational
SalicylamideSalicylamide may increase the anticoagulant activities of Lepirudin.Approved
Salicylic acidSalicylic acid may increase the anticoagulant activities of Lepirudin.Approved, Vet Approved
SalsalateSalsalate may increase the anticoagulant activities of Lepirudin.Approved
SCH-530348SCH-530348 may increase the anticoagulant activities of Lepirudin.Investigational
SecoisolariciresinolSecoisolariciresinol may decrease the anticoagulant activities of Lepirudin.Investigational
SelexipagSelexipag may increase the anticoagulant activities of Lepirudin.Approved
SeratrodastSeratrodast may increase the anticoagulant activities of Lepirudin.Approved, Investigational
SevofluraneSevoflurane may increase the anticoagulant activities of Lepirudin.Approved, Vet Approved
SildenafilThe serum concentration of Sildenafil can be increased when it is combined with Lepirudin.Approved, Investigational
SimeprevirThe serum concentration of Simeprevir can be increased when it is combined with Lepirudin.Approved
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Lepirudin.Approved
SRT501SRT501 may increase the anticoagulant activities of Lepirudin.Investigational
St. John's WortThe metabolism of Lepirudin can be increased when combined with St. John's Wort.Nutraceutical
StreptokinaseStreptokinase may increase the anticoagulant activities of Lepirudin.Approved
SugammadexSugammadex may increase the anticoagulant activities of Lepirudin.Approved
SulfasalazineSulfasalazine may increase the anticoagulant activities of Lepirudin.Approved
SulindacSulindac may increase the anticoagulant activities of Lepirudin.Approved
SulodexideLepirudin may increase the anticoagulant activities of Sulodexide.Approved, Investigational
SuprofenSuprofen may increase the anticoagulant activities of Lepirudin.Approved, Withdrawn
Synthetic Conjugated Estrogens, AThe serum concentration of Synthetic Conjugated Estrogens, A can be decreased when it is combined with Lepirudin.Approved
Synthetic Conjugated Estrogens, BSynthetic Conjugated Estrogens, B may decrease the anticoagulant activities of Lepirudin.Approved
TacrolimusThe metabolism of Tacrolimus can be decreased when combined with Lepirudin.Approved, Investigational
TemsirolimusThe risk or severity of adverse effects can be increased when Lepirudin is combined with Temsirolimus.Approved
TenecteplaseTenecteplase may increase the anticoagulant activities of Lepirudin.Approved
TenoxicamTenoxicam may increase the anticoagulant activities of Lepirudin.Approved
TepoxalinTepoxalin may increase the anticoagulant activities of Lepirudin.Vet Approved
TeriflunomideTeriflunomide may increase the anticoagulant activities of Lepirudin.Approved
TesmilifeneTesmilifene may increase the anticoagulant activities of Lepirudin.Investigational
TheophyllineThe serum concentration of Theophylline can be decreased when it is combined with Lepirudin.Approved
TianeptineThe serum concentration of Tianeptine can be increased when it is combined with Lepirudin.Approved
Tiaprofenic acidTiaprofenic acid may increase the anticoagulant activities of Lepirudin.Approved
TiboloneTibolone may increase the anticoagulant activities of Lepirudin.Approved
TicagrelorTicagrelor may increase the anticoagulant activities of Lepirudin.Approved
TiclopidineTiclopidine may increase the anticoagulant activities of Lepirudin.Approved
TinoridineTinoridine may increase the anticoagulant activities of Lepirudin.Investigational
TinzaparinTinzaparin may increase the anticoagulant activities of Lepirudin.Approved
TipranavirThe serum concentration of Lepirudin can be decreased when it is combined with Tipranavir.Approved, Investigational
TirofibanTirofiban may increase the anticoagulant activities of Lepirudin.Approved
Tolfenamic AcidTolfenamic Acid may increase the anticoagulant activities of Lepirudin.Approved
TolmetinTolmetin may increase the anticoagulant activities of Lepirudin.Approved
TositumomabThe risk or severity of adverse effects can be increased when Lepirudin is combined with Tositumomab.Approved
TranilastTranilast may increase the anticoagulant activities of Lepirudin.Approved, Investigational
TrapidilTrapidil may increase the anticoagulant activities of Lepirudin.Approved
TreprostinilTreprostinil may increase the anticoagulant activities of Lepirudin.Approved, Investigational
TriazolamThe serum concentration of Triazolam can be increased when it is combined with Lepirudin.Approved
TriflusalTriflusal may increase the anticoagulant activities of Lepirudin.Approved
TrimipramineThe serum concentration of Trimipramine can be increased when it is combined with Lepirudin.Approved
Trisalicylate-cholineTrisalicylate-choline may increase the anticoagulant activities of Lepirudin.Approved
UrokinaseUrokinase may increase the anticoagulant activities of Lepirudin.Approved, Investigational, Withdrawn
ValdecoxibValdecoxib may increase the anticoagulant activities of Lepirudin.Investigational, Withdrawn
Valproic AcidThe serum concentration of Valproic Acid can be decreased when it is combined with Lepirudin.Approved, Investigational
VerapamilThe metabolism of Verapamil can be decreased when combined with Lepirudin.Approved
Vitamin EVitamin E may increase the anticoagulant activities of Lepirudin.Approved, Nutraceutical, Vet Approved
VorapaxarThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Lepirudin.Approved
WarfarinLepirudin may increase the anticoagulant activities of Warfarin.Approved
XimelagatranLepirudin may increase the anticoagulant activities of Ximelagatran.Approved, Investigational, Withdrawn
Ym150Lepirudin may increase the anticoagulant activities of Ym150.Investigational
ZaltoprofenZaltoprofen may increase the anticoagulant activities of Lepirudin.Approved
ZeranolZeranol may decrease the anticoagulant activities of Lepirudin.Vet Approved
ZidovudineThe serum concentration of Zidovudine can be decreased when it is combined with Lepirudin.Approved
ZileutonZileuton may increase the anticoagulant activities of Lepirudin.Approved, Investigational, Withdrawn
ZomepiracZomepirac may increase the anticoagulant activities of Lepirudin.Withdrawn
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General References
  1. Smythe MA, Stephens JL, Koerber JM, Mattson JC: A comparison of lepirudin and argatroban outcomes. Clin Appl Thromb Hemost. 2005 Oct;11(4):371-4. [PubMed:16244762 ]
  2. Tardy B, Lecompte T, Boelhen F, Tardy-Poncet B, Elalamy I, Morange P, Gruel Y, Wolf M, Francois D, Racadot E, Camarasa P, Blouch MT, Nguyen F, Doubine S, Dutrillaux F, Alhenc-Gelas M, Martin-Toutain I, Bauters A, Ffrench P, de Maistre E, Grunebaum L, Mouton C, Huisse MG, Gouault-Heilmann M, Lucke V: Predictive factors for thrombosis and major bleeding in an observational study in 181 patients with heparin-induced thrombocytopenia treated with lepirudin. Blood. 2006 Sep 1;108(5):1492-6. Epub 2006 May 11. [PubMed:16690967 ]
  3. Lubenow N, Eichler P, Lietz T, Greinacher A: Lepirudin in patients with heparin-induced thrombocytopenia - results of the third prospective study (HAT-3) and a combined analysis of HAT-1, HAT-2, and HAT-3. J Thromb Haemost. 2005 Nov;3(11):2428-36. [PubMed:16241940 ]
  4. Google books [Link]
External Links
ATC CodesB01AE02
AHFS Codes
  • 20:12.04.12
PDB Entries
FDA labelDownload (128 KB)
MSDSDownload (567 KB)
Pharmacoeconomics
Manufacturers
  • Bayer healthcare pharmaceuticals inc
Packagers
Dosage forms
FormRouteStrength
Injection, solution, concentrateIntravenous20 mg
Injection, solution, concentrateIntravenous50 mg
Powder, for solutionIntravenous50 mg
Prices
Unit descriptionCostUnit
Refludan 50 mg vial273.19USD vial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA1339104 No1997-07-292014-07-29Canada
US5180668 No1993-01-192010-01-19Us
Properties
StateLiquid
Experimental Properties
PropertyValueSource
melting point65 °COtto, A. & Seckler, R. Eur. J. Biochem. 202:67-73 (1991)
hydrophobicity-0.777Not Available
isoelectric point4.04Not Available
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available

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. Turpie AG: Anticoagulants in acute coronary syndromes. Am J Cardiol. 1999 Sep 2;84(5A):2M-6M. [PubMed:10505536 ]
  2. Warkentin TE: Venous thromboembolism in heparin-induced thrombocytopenia. Curr Opin Pulm Med. 2000 Jul;6(4):343-51. [PubMed:10912644 ]
  3. Eriksson BI: New therapeutic options in deep vein thrombosis prophylaxis. Semin Hematol. 2000 Jul;37(3 Suppl 5):7-9. [PubMed:11055889 ]
  4. Fabrizio MC: Use of ecarin clotting time (ECT) with lepirudin therapy in heparin-induced thrombocytopenia and cardiopulmonary bypass. J Extra Corpor Technol. 2001 May;33(2):117-25. [PubMed:11467439 ]
  5. Szaba FM, Smiley ST: Roles for thrombin and fibrin(ogen) in cytokine/chemokine production and macrophage adhesion in vivo. Blood. 2002 Feb 1;99(3):1053-9. [PubMed:11807012 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23