Identification

Name
Lepirudin
Accession Number
DB00001  (BTD00024, BIOD00024)
Type
Biotech
Groups
Approved
Biologic Classification
Protein Based Therapies
Other protein based therapies
Description

Lepirudin is identical to natural hirudin except for substitution of leucine for isoleucine at the N-terminal end of the molecule and the absence of a sulfate group on the tyrosine at position 63. It is produced via yeast cells. Bayer ceased the production of lepirudin (Refludan) effective May 31, 2012.

Protein structure
Db00001
Protein chemical formula
C287H440N80O110S6
Protein average weight
6963.425 Da
Sequences
>DB00001 sequence
LVYTDCTESGQNLCLCEGSNVCGQGNKCILGSDGEKNQCVTGEGTPKPQSHNDGDFEEIP
EEYLQ
Download FASTA Format
Synonyms
  • Hirudin variant-1
  • Lepirudin recombinant
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
RefludanPowder, for solution50 mgIntravenousBayer2000-01-312013-07-26Canada
Unapproved/Other Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
RefludanInjection, solution, concentrate50 mgIntravenousCelgene Europe Limited1997-03-13Not applicableEu
RefludanInjection, solution, concentrate20 mgIntravenousCelgene Europe Limited1997-03-13Not applicableEu
RefludanInjection, solution, concentrate50 mgIntravenousCelgene Europe Limited1997-03-13Not applicableEu
RefludanInjection, solution, concentrate20 mgIntravenousCelgene Europe Limited1997-03-13Not applicableEu
Categories
UNII
Y43GF64R34
CAS number
138068-37-8

Pharmacology

Indication

For the treatment of heparin-induced thrombocytopenia

Structured Indications
Not Available
Pharmacodynamics

Lepirudin is used to break up clots and to reduce thrombocytopenia. It binds to thrombin and prevents thrombus or clot formation. It is a highly potent, selective, and essentially irreversible inhibitor of thrombin and clot-bond thrombin. Lepirudin requires no cofactor for its anticoagulant action. Lepirudin is a recombinant form of hirudin, an endogenous anticoagulant found in medicinal leeches.

Mechanism of action

Lepirudin 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.

TargetActionsOrganism
AProthrombin
inhibitor
Human
Absorption

Bioavailability 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 binding
Not 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 elimination

Lepirudin 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 life

Approximately 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)]
Toxicity

In case of overdose (eg, suggested by excessively high aPTT values) the risk of bleeding is increased.

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Lepirudin Action PathwayDrug action
Pharmacogenomic Effects/ADRs
Not 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, Investigational
AcemetacinAcemetacin may increase the anticoagulant activities of Lepirudin.Approved
AcenocoumarolLepirudin may increase the anticoagulant activities of Acenocoumarol.Approved
Acetylsalicylic acidAcetylsalicylic acid may increase the anticoagulant activities of Lepirudin.Approved, Vet Approved
AdapaleneAdapalene may increase the anticoagulant activities of Lepirudin.Approved
AlclofenacAlclofenac may increase the anticoagulant activities of Lepirudin.Approved, Withdrawn
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
AlminoprofenAlminoprofen may increase the anticoagulant activities of Lepirudin.Experimental
AloxiprinAloxiprin may increase the anticoagulant activities of Lepirudin.Experimental
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, Investigational
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
AmoxapineThe serum concentration of Amoxapine 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
AndrographolideAndrographolide may increase the anticoagulant activities of Lepirudin.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
ApocyninApocynin may increase the anticoagulant activities of Lepirudin.Investigational
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, Investigational, 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
BecaplerminLepirudin may increase the anticoagulant activities of Becaplermin.Approved, Investigational
BemiparinBemiparin may increase the anticoagulant activities of Lepirudin.Approved, Investigational
BendazacBendazac may increase the anticoagulant activities of Lepirudin.Experimental
BenorilateBenorilate may increase the anticoagulant activities of Lepirudin.Experimental
BenoxaprofenBenoxaprofen may increase the anticoagulant activities of Lepirudin.Withdrawn
BenzydamineBenzydamine may increase the anticoagulant activities of Lepirudin.Approved
BeraprostBeraprost may increase the anticoagulant activities of Lepirudin.Investigational
BevoniumBevonium may increase the anticoagulant activities of Lepirudin.Experimental
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, Withdrawn
BrinaseBrinase may increase the anticoagulant activities of Lepirudin.Experimental
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
BufexamacBufexamac may increase the anticoagulant activities of Lepirudin.Experimental
BuflomedilBuflomedil may increase the anticoagulant activities of Lepirudin.Experimental
BumadizoneBumadizone may increase the anticoagulant activities of Lepirudin.Experimental
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
Carbaspirin calciumCarbaspirin calcium may increase the anticoagulant activities of Lepirudin.Experimental, 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, Investigational
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.Investigational, Withdrawn
Choline magnesium trisalicylateCholine magnesium trisalicylate may increase the anticoagulant activities of Lepirudin.Approved
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.Approved, 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
CloricromenCloricromen may increase the anticoagulant activities of Lepirudin.Experimental
ClorindioneClorindione may increase the anticoagulant activities of Lepirudin.Experimental
Collagenase clostridium histolyticumThe risk or severity of adverse effects can be increased when Lepirudin is combined with Collagenase clostridium histolyticum.Approved, Investigational
Conjugated estrogensThe serum concentration of Conjugated 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 etexilateLepirudin may increase the anticoagulant activities of Dabigatran etexilate.Approved
DaidzeinDaidzein may decrease the anticoagulant activities of Lepirudin.Experimental
DalteparinLepirudin may increase the anticoagulant activities of Dalteparin.Approved
DanaparoidLepirudin may increase the anticoagulant activities of Danaparoid.Approved, Withdrawn
DarexabanLepirudin may increase the anticoagulant activities of Darexaban.Investigational
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
DemegestoneThe therapeutic efficacy of Lepirudin can be decreased when used in combination with Demegestone.Experimental
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
DibenzepinThe serum concentration of Dibenzepin can be increased when it is combined with Lepirudin.Experimental
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, Investigational
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, Investigational
DifenpiramideDifenpiramide may increase the anticoagulant activities of Lepirudin.Experimental
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
DiphenadioneDiphenadione may increase the anticoagulant activities of Lepirudin.Experimental
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
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, Investigational, Withdrawn
DyphyllineThe serum concentration of Dyphylline can be decreased when it is combined with Lepirudin.Approved
E-6201E-6201 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
EpimestrolEpimestrol may decrease the anticoagulant activities of Lepirudin.Experimental
EpinastineEpinastine may increase the anticoagulant activities of Lepirudin.Approved, Investigational
EpirizoleEpirizole may increase the anticoagulant activities of Lepirudin.Approved
EplivanserinEplivanserin may increase the anticoagulant activities of Lepirudin.Investigational
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
EquolEquol may decrease the anticoagulant activities of Lepirudin.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, Investigational, 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
EthenzamideEthenzamide may increase the anticoagulant activities of Lepirudin.Experimental
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
EthynodiolThe therapeutic efficacy of Lepirudin can be decreased when used in combination with Ethynodiol.Experimental
EtodolacEtodolac may increase the anticoagulant activities of Lepirudin.Approved, Investigational, Vet Approved
EtofenamateEtofenamate may increase the anticoagulant activities of Lepirudin.Approved, Investigational
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, Investigational
exisulindexisulind may increase the anticoagulant activities of Lepirudin.Investigational
FelbinacFelbinac may increase the anticoagulant activities of Lepirudin.Experimental
FenbufenFenbufen may increase the anticoagulant activities of Lepirudin.Approved
FenoprofenFenoprofen may increase the anticoagulant activities of Lepirudin.Approved
FentiazacFentiazac may increase the anticoagulant activities of Lepirudin.Experimental
FeprazoneFeprazone may increase the anticoagulant activities of Lepirudin.Experimental
Ferulic acidFerulic acid may increase the anticoagulant activities of Lepirudin.Experimental
FibrinolysinFibrinolysin may increase the anticoagulant activities of Lepirudin.Investigational
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
FlunoxaprofenFlunoxaprofen may increase the anticoagulant activities of Lepirudin.Experimental
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, Investigational
GestonoroneThe therapeutic efficacy of Lepirudin can be decreased when used in combination with Gestonorone.Experimental
GestrinoneThe therapeutic efficacy of Lepirudin can be decreased when used in combination with Gestrinone.Approved
GuacetisalGuacetisal may increase the anticoagulant activities of Lepirudin.Experimental
HeminHemin may increase the anticoagulant activities of Lepirudin.Approved
Hemoglobin crosfumarilHemoglobin crosfumaril may increase the anticoagulant activities of Lepirudin.Experimental
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
Hydroxyprogesterone caproateThe therapeutic efficacy of Lepirudin can be decreased when used in combination with Hydroxyprogesterone caproate.Approved
HydroxytyrosolHydroxytyrosol may increase the anticoagulant activities of Lepirudin.Investigational
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, Investigational, Withdrawn
IfetrobanIfetroban may increase the anticoagulant activities of Lepirudin.Investigational
IloprostIloprost may increase the anticoagulant activities of Lepirudin.Approved, Investigational
Imidazole salicylateImidazole salicylate may increase the anticoagulant activities of Lepirudin.Experimental
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
IprindoleThe serum concentration of Iprindole can be increased when it is combined with Lepirudin.Experimental
IsoxicamIsoxicam may increase the anticoagulant activities of Lepirudin.Withdrawn
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
LetaxabanLepirudin may increase the anticoagulant activities of Letaxaban.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, Investigational
LinsidomineLinsidomine may increase the anticoagulant activities of Lepirudin.Experimental
LisofyllineLisofylline may increase the anticoagulant activities of Lepirudin.Investigational
LofepramineThe serum concentration of Lofepramine can be increased when it is combined with Lepirudin.Experimental
LonazolacLonazolac may increase the anticoagulant activities of Lepirudin.Experimental
LornoxicamLornoxicam may increase the anticoagulant activities of Lepirudin.Approved, Investigational
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, Investigational
LumiracoxibLumiracoxib may increase the anticoagulant activities of Lepirudin.Approved, Investigational
Magnesium salicylateMagnesium salicylate may increase the anticoagulant activities of Lepirudin.Approved
MasoprocolMasoprocol may increase the anticoagulant activities of Lepirudin.Approved, Investigational
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
MelagatranLepirudin may increase the anticoagulant activities of Melagatran.Experimental
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.Investigational, Withdrawn
MethallenestrilThe serum concentration of Methallenestril can be decreased when it is combined with Lepirudin.Experimental
Methyl salicylateMethyl salicylate may increase the anticoagulant activities of Lepirudin.Approved, Vet Approved
MethylergometrineThe serum concentration of Methylergometrine can be increased when it is combined with Lepirudin.Approved
MethylestrenoloneThe therapeutic efficacy of Lepirudin can be decreased when used in combination with Methylestrenolone.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
MofebutazoneMofebutazone may increase the anticoagulant activities of Lepirudin.Experimental
MoxestrolMoxestrol may decrease the anticoagulant activities of Lepirudin.Experimental
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.Approved, 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
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
NifenazoneNifenazone may increase the anticoagulant activities of Lepirudin.Experimental
Niflumic AcidNiflumic Acid may increase the anticoagulant activities of Lepirudin.Approved
NimesulideNimesulide may increase the anticoagulant activities of Lepirudin.Approved, Investigational, 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
NorgestrienoneThe therapeutic efficacy of Lepirudin can be decreased when used in combination with Norgestrienone.Experimental
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, Nutraceutical
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.Approved, Withdrawn
OzagrelOzagrel may increase the anticoagulant activities of Lepirudin.Investigational
ParecoxibParecoxib may increase the anticoagulant activities of Lepirudin.Approved
ParnaparinParnaparin may increase the anticoagulant activities of Lepirudin.Approved, Investigational
ParthenolideParthenolide may increase the anticoagulant activities of Lepirudin.Investigational
Pentaerythritol TetranitrateLepirudin may increase the anticoagulant activities of Pentaerythritol Tetranitrate.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, Investigational
PhenprocoumonLepirudin may increase the anticoagulant activities of Phenprocoumon.Approved, Investigational
PhenylbutazonePhenylbutazone may increase the anticoagulant activities of Lepirudin.Approved, Vet Approved
PicotamidePicotamide may increase the anticoagulant activities of Lepirudin.Experimental
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.Approved, Investigational
PiroxicamPiroxicam may increase the anticoagulant activities of Lepirudin.Approved, Investigational
PirprofenPirprofen may increase the anticoagulant activities of Lepirudin.Experimental
Polyestradiol phosphatePolyestradiol phosphate may decrease the anticoagulant activities of Lepirudin.Approved
PranoprofenPranoprofen may increase the anticoagulant activities of Lepirudin.Experimental, Investigational
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
ProglumetacinProglumetacin may increase the anticoagulant activities of Lepirudin.Experimental
PromegestoneThe therapeutic efficacy of Lepirudin can be decreased when used in combination with Promegestone.Experimental
PromestrienePromestriene may decrease the anticoagulant activities of Lepirudin.Investigational
PropacetamolPropacetamol may increase the anticoagulant activities of Lepirudin.Approved, Investigational
PropyphenazonePropyphenazone may increase the anticoagulant activities of Lepirudin.Experimental
ProquazoneProquazone may increase the anticoagulant activities of Lepirudin.Experimental
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.Approved, Experimental, Investigational
ReteplaseReteplase may increase the anticoagulant activities of Lepirudin.Approved
ReviparinLepirudin may increase the anticoagulant activities of Reviparin.Approved, Investigational
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
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
SarpogrelateSarpogrelate may increase the anticoagulant activities of Lepirudin.Investigational
SaruplaseSaruplase may increase the anticoagulant activities of Lepirudin.Experimental
SecoisolariciresinolSecoisolariciresinol may decrease the anticoagulant activities of Lepirudin.Investigational
SelexipagSelexipag may increase the anticoagulant activities of Lepirudin.Approved
SemapimodSemapimod may increase the anticoagulant activities of Lepirudin.Investigational
SeratrodastSeratrodast may increase the anticoagulant activities of Lepirudin.Approved
SerrapeptaseSerrapeptase may increase the anticoagulant activities of Lepirudin.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.Investigational, Nutraceutical
StreptokinaseStreptokinase may increase the anticoagulant activities of Lepirudin.Approved, Investigational
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
SuxibuzoneSuxibuzone may increase the anticoagulant activities of Lepirudin.Experimental
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
TarenflurbilTarenflurbil may increase the anticoagulant activities of Lepirudin.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
TenidapTenidap may increase the anticoagulant activities of Lepirudin.Experimental
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, Investigational
Tiaprofenic acidTiaprofenic acid may increase the anticoagulant activities of Lepirudin.Approved
TiboloneTibolone may increase the anticoagulant activities of Lepirudin.Approved, Investigational
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
TioclomarolTioclomarol may increase the anticoagulant activities of Lepirudin.Experimental
TipranavirTipranavir may increase the anticoagulant activities of Lepirudin.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, Investigational
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
TribenosideTribenoside may increase the anticoagulant activities of Lepirudin.Experimental
TriflusalTriflusal may increase the anticoagulant activities of Lepirudin.Approved, Investigational
TrimipramineThe serum concentration of Trimipramine can be increased when it is combined with Lepirudin.Approved
TriptolideTriptolide may increase the anticoagulant activities of Lepirudin.Investigational
Trolamine salicylateTrolamine salicylate may increase the anticoagulant activities of Lepirudin.Approved
TroxerutinLepirudin may increase the anticoagulant activities of Troxerutin.Investigational
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
ZaltoprofenZaltoprofen may increase the anticoagulant activities of Lepirudin.Approved, Investigational
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 Interactions
Not Available

References

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
UniProt
P01050
KEGG Drug
D06880
PubChem Substance
46507011
ChEMBL
CHEMBL1201666
Therapeutic Targets Database
DAP000541
PharmGKB
PA450195
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Lepirudin
ATC Codes
B01AE02 — Lepirudin
FDA label
Download (128 KB)
MSDS
Download (567 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1, 2TerminatedTreatmentLung Cancers1
2CompletedTreatmentThrombosis1
4TerminatedTreatmentCardiac surgery, heparin-induced thrombocytopenia and thrombosis syndrome1
4WithdrawnTreatmentCardiac surgery, heparin-induced thrombocytopenia and thrombosis syndrome1
Not AvailableCompletedNot AvailableAcute HIT II (Heparin-induced Thrombocytopenia Type II)1

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)
US5180668No1993-01-192010-01-19Us

Properties

State
Liquid
Experimental Properties
PropertyValueSource
melting point (°C)65 °COtto, A. & Seckler, R. Eur. J. Biochem. 202:67-73 (1991)
hydrophobicity-0.777Not Available
isoelectric point4.04Not Available

Taxonomy

Description
Not Available
Kingdom
Organic Compounds
Super Class
Organic Acids
Class
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Peptides
Alternative Parents
Not Available
Substituents
Not Available
Molecular Framework
Not Available
External Descriptors
Not 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 homeostas...
Gene Name
F2
Uniprot ID
P00734
Uniprot Name
Prothrombin
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]

Drug created on June 13, 2005 07:24 / Updated on November 06, 2017 06:43