Identification

Name
Argatroban
Accession Number
DB00278  (APRD00105)
Type
Small Molecule
Groups
Approved, Investigational
Description

Argatroban is a direct, selective thrombin inhibitor. The American College of Cardiologists (ACC) recommend using bivalirudin or argatroban in patients who have had, or at risk for, heparin induced thrombocytopenia (HIT) and are undergoing percutaneous coronary intervention. Argatroban is a non-heparin anticoagulant shown to both normalize platelet count in patients with HIT and prevent the formation of thrombi. Parental anticoagulants must be stopped and a baseline activated partial thromboplastin time must be obtained prior to administering argatroban.

Structure
Thumb
Synonyms
Not Available
Product Ingredients
IngredientUNIICASInChI Key
Argatroban monohydrateIY90U61Z3S141396-28-3AIEZTKLTLCMZIA-CZSXTPSTSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
ArgatrobanInjection1 mg/mLIntravenousEagle Pharmaceuticals, Inc.2011-09-06Not applicableUs
ArgatrobanInjection1 mg/mLIntravenousSandoz2011-09-06Not applicableUs
ArgatrobanInjection250 mg/2.5mLIntravenousWest Ward Pharmaceutical2012-01-05Not applicableUs
ArgatrobanSolution100 mgIntravenousNovartis2002-06-13Not applicableCanada
ArgatrobanInjection, solution1 mg/mLIntravenousTeva Parenteral Medicines, Inc.2015-04-27Not applicableUs
ArgatrobanInjection1 mg/mLIntravenousEagle Pharmaceuticals, Inc.2011-09-06Not applicableUs
ArgatrobanInjection1 mg/mLIntravenousSandoz2011-09-06Not applicableUs
ArgatrobanInjection, solution100 mg/mLIntravenousGlaxosmithkline Inc2000-11-28Not applicableUs
ArgatrobanSolution125 mg/125mLIntravenousSandoz2011-05-09Not applicableUs
ArgatrobanInjection50 mg/50mLIntravenousWest Ward Pharmaceutical2016-11-01Not applicableUs
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
ArgatrobanInjection250 mg/2.5mLIntravenousPar Pharmaceutical2015-06-01Not applicableUs
ArgatrobanSolution125 mg/125mLIntravenousGland Pharma Limited2017-05-26Not applicableUs
ArgatrobanInjection, solution100 mg/mLIntravenousHospira, Inc.2017-01-16Not applicableUs
Categories
UNII
0DW7MIH1VX
CAS number
74863-84-6
Weight
Average: 508.634
Monoisotopic: 508.246788982
Chemical Formula
C23H36N6O5S
InChI Key
KXNPVXPOPUZYGB-XYVMCAHJSA-N
InChI
InChI=1S/C23H36N6O5S/c1-14-8-10-29(18(12-14)22(31)32)21(30)17(6-4-9-26-23(24)25)28-35(33,34)19-7-3-5-16-11-15(2)13-27-20(16)19/h3,5,7,14-15,17-18,27-28H,4,6,8-13H2,1-2H3,(H,31,32)(H4,24,25,26)/t14-,15-,17+,18-/m1/s1
IUPAC Name
(2R,4R)-1-[(2S)-5-[(diaminomethylidene)amino]-2-[(3R)-3-methyl-1,2,3,4-tetrahydroquinoline-8-sulfonamido]pentanoyl]-4-methylpiperidine-2-carboxylic acid
SMILES
C[[email protected]@H]1CCN([[email protected]](C1)C(O)=O)C(=O)[[email protected]](CCCN=C(N)N)NS(=O)(=O)C1=CC=CC2=C1NC[[email protected]](C)C2

Pharmacology

Indication

Argatroban is indicated for prevention and treatment of thrombosis caused by heparin induced thrombocytopenia (HIT). It is also indicated for use in patients with, or at risk for, HIT who are undergoing percutaneous coronary intervention.

Structured Indications
Pharmacodynamics

Argatroban is a synthetic direct thrombin inhibitor derived from L-arginine indicated as an anticoagulant for prophylaxis or treatment of thrombosis in patients with heparin-induced thrombocytopenia. Argatroban is a direct thrombin inhibitor that reversibly binds to the thrombin active site. Argatroban does not require the co-factor antithrombin III for antithrombotic activity. Argatroban exerts its anticoagulant effects by inhibiting thrombin-catalyzed or -induced reactions, including fibrin formation; activation of coagulation factors V, VIII, and XIII; protein C; and platelet aggregation. Argatroban is highly selective for thrombin with an inhibitory constant (Ki) of 0.04 µM. At therapeutic concentrations, Argatroban has little or no effect on related serine proteases (trypsin, factor Xa, plasmin, and kallikrein). Argatroban is capable of inhibiting the action of both free and clot-associated thrombin.

Mechanism of action

Argatroban exerts its anticoagulant effects by inhibiting thrombin-catalyzed or -induced reactions, including fibrin formation; activation of coagulation factors V, VIII, and XIII; protein C; and platelet aggregation.

TargetActionsOrganism
AProthrombin
inhibitor
Human
Absorption

Bioavailability is 100% (intravenous).

Volume of distribution
  • 174 mL/kg
  • 12.18 L [70-kg adult]
Protein binding

54%

Metabolism

Liver via hydroxylation and aromatization of the 3-methyltetrahydroquinoline ring. Age and gender do not substantially affect the pharmacodynamic or pharmacokinetic profile of argatroban.

Route of elimination

Argatroban is excreted primarily in the feces (65%), presumably through biliary secretion; 22% is eliminated via urine.

Half life

39 and 51 minutes

Clearance
  • 5.1 L/kg/hr [infusion doses up to 40 mcg/kg/min]
Toxicity

Excessive bleeding

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Argatroban 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 Argatroban.Approved, Investigational
AbciximabAbciximab may increase the anticoagulant activities of Argatroban.Approved
AceclofenacAceclofenac may increase the anticoagulant activities of Argatroban.Approved, Investigational
AcemetacinAcemetacin may increase the anticoagulant activities of Argatroban.Approved
AcenocoumarolArgatroban may increase the anticoagulant activities of Acenocoumarol.Approved
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Argatroban is combined with Acetylsalicylic acid.Approved, Vet Approved
AdapaleneAdapalene may increase the anticoagulant activities of Argatroban.Approved
AlclofenacAlclofenac may increase the anticoagulant activities of Argatroban.Approved, Withdrawn
AlfuzosinThe serum concentration of Alfuzosin can be increased when it is combined with Argatroban.Approved, Investigational
AllylestrenolThe therapeutic efficacy of Argatroban can be decreased when used in combination with Allylestrenol.Approved
AlminoprofenAlminoprofen may increase the anticoagulant activities of Argatroban.Experimental
AloxiprinThe risk or severity of adverse effects can be increased when Argatroban is combined with Aloxiprin.Experimental
AlprazolamThe serum concentration of Alprazolam can be increased when it is combined with Argatroban.Approved, Illicit, Investigational
AlprostadilAlprostadil may increase the anticoagulant activities of Argatroban.Approved, Investigational
AlteplaseAlteplase may increase the anticoagulant activities of Argatroban.Approved
AltrenogestThe therapeutic efficacy of Argatroban can be decreased when used in combination with Altrenogest.Vet Approved
ALX-0081ALX-0081 may increase the anticoagulant activities of Argatroban.Investigational
Ambroxol acefyllinateThe serum concentration of Ambroxol acefyllinate can be decreased when it is combined with Argatroban.Experimental, Investigational
AmineptineThe serum concentration of Amineptine can be increased when it is combined with Argatroban.Illicit, Withdrawn
AminophyllineThe serum concentration of Aminophylline can be decreased when it is combined with Argatroban.Approved
Aminosalicylic AcidThe risk or severity of adverse effects can be increased when Argatroban is combined with Aminosalicylic Acid.Approved
AmiodaroneThe metabolism of Argatroban can be decreased when combined with Amiodarone.Approved, Investigational
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Argatroban.Approved
AnagrelideAnagrelide may increase the anticoagulant activities of Argatroban.Approved
AncrodArgatroban may increase the anticoagulant activities of Ancrod.Investigational
AndrographolideAndrographolide may increase the anticoagulant activities of Argatroban.Investigational
AnisodamineAnisodamine may increase the anticoagulant activities of Argatroban.Investigational
AnistreplaseAnistreplase may increase the anticoagulant activities of Argatroban.Approved
AntipyrineAntipyrine may increase the anticoagulant activities of Argatroban.Approved
Antithrombin III humanArgatroban may increase the anticoagulant activities of Antithrombin III human.Approved
ApixabanThe risk or severity of adverse effects can be increased when Argatroban is combined with Apixaban.Approved
ApocyninApocynin may increase the anticoagulant activities of Argatroban.Investigational
ApremilastApremilast may increase the anticoagulant activities of Argatroban.Approved, Investigational
AprepitantThe serum concentration of Argatroban can be increased when it is combined with Aprepitant.Approved, Investigational
AprotininThe therapeutic efficacy of Argatroban can be decreased when used in combination with Aprotinin.Approved, Withdrawn
ArdeparinArgatroban may increase the anticoagulant activities of Ardeparin.Approved, Investigational, Withdrawn
AstaxanthinAstaxanthin may increase the anticoagulant activities of Argatroban.Investigational
AtazanavirThe metabolism of Argatroban can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Argatroban can be decreased when combined with Atomoxetine.Approved
AtorvastatinThe serum concentration of Atorvastatin can be increased when it is combined with Argatroban.Approved
AzapropazoneAzapropazone may increase the anticoagulant activities of Argatroban.Withdrawn
AzelastineAzelastine may increase the anticoagulant activities of Argatroban.Approved
BalsalazideBalsalazide may increase the anticoagulant activities of Argatroban.Approved, Investigational
BatroxobinBatroxobin may increase the anticoagulant activities of Argatroban.Experimental
BecaplerminBecaplermin may increase the anticoagulant activities of Argatroban.Approved, Investigational
BemiparinBemiparin may increase the anticoagulant activities of Argatroban.Approved, Investigational
BendazacBendazac may increase the anticoagulant activities of Argatroban.Experimental
BenorilateBenorilate may increase the anticoagulant activities of Argatroban.Experimental
BenoxaprofenBenoxaprofen may increase the anticoagulant activities of Argatroban.Withdrawn
BeraprostBeraprost may increase the anticoagulant activities of Argatroban.Investigational
BevoniumBevonium may increase the anticoagulant activities of Argatroban.Experimental
BivalirudinBivalirudin may increase the anticoagulant activities of Argatroban.Approved, Investigational
BoceprevirThe serum concentration of Argatroban can be decreased when it is combined with Boceprevir.Approved, Withdrawn
BortezomibThe metabolism of Argatroban can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Argatroban can be decreased when it is combined with Bosentan.Approved, Investigational
BrinaseBrinase may increase the anticoagulant activities of Argatroban.Experimental
BromfenacBromfenac may increase the anticoagulant activities of Argatroban.Approved
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Argatroban.Approved, Investigational
BucillamineBucillamine may increase the anticoagulant activities of Argatroban.Investigational
BufexamacBufexamac may increase the anticoagulant activities of Argatroban.Experimental
BuflomedilBuflomedil may increase the anticoagulant activities of Argatroban.Experimental
BumadizoneBumadizone may increase the anticoagulant activities of Argatroban.Experimental
ButylphthalideButylphthalide may increase the anticoagulant activities of Argatroban.Investigational
CabergolineThe serum concentration of Cabergoline can be increased when it is combined with Argatroban.Approved
CangrelorCangrelor may increase the anticoagulant activities of Argatroban.Approved
CarbamazepineThe metabolism of Argatroban can be increased when combined with Carbamazepine.Approved, Investigational
Carbaspirin calciumThe risk or severity of adverse effects can be increased when Argatroban is combined with Carbaspirin calcium.Experimental, Investigational
CarprofenCarprofen may increase the anticoagulant activities of Argatroban.Approved, Vet Approved, Withdrawn
CastanospermineCastanospermine may increase the anticoagulant activities of Argatroban.Experimental
CelecoxibCelecoxib may increase the anticoagulant activities of Argatroban.Approved, Investigational
CeritinibThe serum concentration of Argatroban can be increased when it is combined with Ceritinib.Approved
CertoparinArgatroban may increase the anticoagulant activities of Certoparin.Approved, Investigational
ChloroquineChloroquine may increase the anticoagulant activities of Argatroban.Approved, Vet Approved
ChlorotrianiseneThe serum concentration of Chlorotrianisene can be decreased when it is combined with Argatroban.Investigational, Withdrawn
Choline magnesium trisalicylateCholine magnesium trisalicylate may increase the anticoagulant activities of Argatroban.Approved
CilostazolCilostazol may increase the anticoagulant activities of Argatroban.Approved
CisaprideThe serum concentration of Cisapride can be increased when it is combined with Argatroban.Approved, Investigational, Withdrawn
Citric AcidArgatroban 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 Argatroban.Approved
ClemastineThe metabolism of Argatroban can be decreased when combined with Clemastine.Approved
ClomipramineThe serum concentration of Clomipramine can be increased when it is combined with Argatroban.Approved, Vet Approved
ClonixinClonixin may increase the anticoagulant activities of Argatroban.Approved
ClopidogrelClopidogrel may increase the anticoagulant activities of Argatroban.Approved, Nutraceutical
CloricromenCloricromen may increase the anticoagulant activities of Argatroban.Experimental
ClorindioneClorindione may increase the anticoagulant activities of Argatroban.Experimental
ClotrimazoleThe metabolism of Argatroban can be decreased when combined with Clotrimazole.Approved, Vet Approved
CobicistatThe metabolism of Argatroban can be decreased when combined with Cobicistat.Approved
Collagenase clostridium histolyticumThe risk or severity of adverse effects can be increased when Argatroban is combined with Collagenase clostridium histolyticum.Approved, Investigational
ConivaptanThe serum concentration of Argatroban can be increased when it is combined with Conivaptan.Approved, Investigational
Conjugated estrogensThe serum concentration of Conjugated estrogens can be decreased when it is combined with Argatroban.Approved
CrizotinibThe metabolism of Argatroban can be decreased when combined with Crizotinib.Approved
CurcuminCurcumin may increase the anticoagulant activities of Argatroban.Investigational
CyclobenzaprineThe serum concentration of Cyclobenzaprine can be increased when it is combined with Argatroban.Approved
CyclophosphamideThe risk or severity of adverse effects can be increased when Argatroban is combined with Cyclophosphamide.Approved, Investigational
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Argatroban.Approved, Investigational, Vet Approved
D-LimoneneD-Limonene may increase the anticoagulant activities of Argatroban.Investigational
DabrafenibThe serum concentration of Argatroban can be decreased when it is combined with Dabrafenib.Approved
DaidzeinDaidzein may decrease the anticoagulant activities of Argatroban.Experimental
DalteparinArgatroban may increase the anticoagulant activities of Dalteparin.Approved
DanaparoidArgatroban may increase the anticoagulant activities of Danaparoid.Approved, Withdrawn
DarexabanArgatroban may increase the anticoagulant activities of Darexaban.Investigational
DarunavirThe metabolism of Argatroban can be decreased when combined with Darunavir.Approved
DasatinibDasatinib may increase the anticoagulant activities of Argatroban.Approved, Investigational
DeferasiroxThe serum concentration of Argatroban can be decreased when it is combined with Deferasirox.Approved, Investigational
DefibrotideDefibrotide may increase the anticoagulant activities of Argatroban.Approved, Investigational
DelavirdineThe serum concentration of Delavirdine can be decreased when it is combined with Argatroban.Approved
DemegestoneThe therapeutic efficacy of Argatroban can be decreased when used in combination with Demegestone.Experimental
Deoxycholic AcidThe risk or severity of adverse effects can be increased when Argatroban is combined with Deoxycholic Acid.Approved
dersalazineThe risk or severity of adverse effects can be increased when Argatroban is combined with dersalazine.Investigational
DesipramineThe serum concentration of Desipramine can be increased when it is combined with Argatroban.Approved
DesirudinArgatroban may increase the anticoagulant activities of Desirudin.Approved
DesmoteplaseDesmoteplase may increase the anticoagulant activities of Argatroban.Investigational
DesogestrelThe therapeutic efficacy of Argatroban can be decreased when used in combination with Desogestrel.Approved
DextranArgatroban may increase the anticoagulant activities of Dextran.Approved, Vet Approved
Dextran 40Argatroban may increase the anticoagulant activities of Dextran 40.Approved
Dextran 70Argatroban may increase the anticoagulant activities of Dextran 70.Approved
Dextran 75Argatroban may increase the anticoagulant activities of Dextran 75.Approved
DibenzepinThe serum concentration of Dibenzepin can be increased when it is combined with Argatroban.Experimental
DiclofenacDiclofenac may increase the anticoagulant activities of Argatroban.Approved, Vet Approved
DicoumarolDicoumarol may increase the anticoagulant activities of Argatroban.Approved
DienestrolThe serum concentration of Dienestrol can be decreased when it is combined with Argatroban.Approved, Investigational
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be decreased when it is combined with Argatroban.Approved, Investigational
DifenpiramideDifenpiramide may increase the anticoagulant activities of Argatroban.Experimental
DiflunisalThe risk or severity of adverse effects can be increased when Argatroban is combined with Diflunisal.Approved
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Argatroban.Approved
DihydroergotamineThe metabolism of Argatroban can be decreased when combined with Dihydroergotamine.Approved
DiltiazemThe metabolism of Diltiazem can be decreased when combined with Argatroban.Approved
DiphenadioneDiphenadione may increase the anticoagulant activities of Argatroban.Experimental
DipyridamoleDipyridamole may increase the anticoagulant activities of Argatroban.Approved
DitazoleDitazole may increase the anticoagulant activities of Argatroban.Approved, Withdrawn
DosulepinThe serum concentration of Dosulepin can be increased when it is combined with Argatroban.Approved
DoxepinThe serum concentration of Doxepin can be increased when it is combined with Argatroban.Approved
DoxycyclineThe metabolism of Argatroban can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Argatroban can be decreased when combined with Dronedarone.Approved
Drotrecogin alfaDrotrecogin alfa may increase the anticoagulant activities of Argatroban.Approved, Investigational, Withdrawn
DroxicamDroxicam may increase the anticoagulant activities of Argatroban.Approved
DuvelisibDuvelisib may increase the anticoagulant activities of Argatroban.Investigational
DydrogesteroneThe therapeutic efficacy of Argatroban 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 Argatroban.Approved
E-6201E-6201 may increase the anticoagulant activities of Argatroban.Investigational
Edetic AcidArgatroban may increase the anticoagulant activities of Edetic Acid.Approved, Vet Approved
EdoxabanEdoxaban may increase the anticoagulant activities of Argatroban.Approved
EnfuvirtideThe serum concentration of Enfuvirtide can be increased when it is combined with Argatroban.Approved, Investigational
EnoxaparinArgatroban may increase the anticoagulant activities of Enoxaparin.Approved
EnzalutamideThe serum concentration of Argatroban can be decreased when it is combined with Enzalutamide.Approved
EpimestrolEpimestrol may decrease the anticoagulant activities of Argatroban.Experimental
EpinastineEpinastine may increase the anticoagulant activities of Argatroban.Approved, Investigational
EpirizoleEpirizole may increase the anticoagulant activities of Argatroban.Approved
EplivanserinEplivanserin may increase the anticoagulant activities of Argatroban.Investigational
eplivanserineeplivanserine may increase the anticoagulant activities of Argatroban.Investigational
EpoprostenolEpoprostenol may increase the antiplatelet activities of Argatroban.Approved
EptifibatideEptifibatide may increase the anticoagulant activities of Argatroban.Approved, Investigational
EquolEquol may decrease the anticoagulant activities of Argatroban.Investigational
Ergoloid mesylateThe serum concentration of Ergoloid mesylate can be increased when it is combined with Argatroban.Approved
ErgonovineThe serum concentration of Ergonovine can be increased when it is combined with Argatroban.Approved
ErgotamineThe serum concentration of Ergotamine can be increased when it is combined with Argatroban.Approved
ErythromycinThe metabolism of Argatroban can be decreased when combined with Erythromycin.Approved, Vet Approved
EsmirtazapineThe serum concentration of Esmirtazapine can be increased when it is combined with Argatroban.Investigational
EstradiolThe serum concentration of Estradiol can be decreased when it is combined with Argatroban.Approved, Investigational, Vet Approved
EstramustineThe serum concentration of Estramustine can be decreased when it is combined with Argatroban.Approved
EstriolEstriol may decrease the anticoagulant activities of Argatroban.Approved, Investigational, Vet Approved
Estrogens, esterifiedThe serum concentration of Estrogens, esterified can be decreased when it is combined with Argatroban.Approved
EstroneEstrone may decrease the anticoagulant activities of Argatroban.Approved
Estrone sulfateThe serum concentration of Estrone sulfate can be decreased when it is combined with Argatroban.Approved
EtanerceptEtanercept may increase the anticoagulant activities of Argatroban.Approved, Investigational
EthenzamideEthenzamide may increase the anticoagulant activities of Argatroban.Experimental
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be decreased when it is combined with Argatroban.Approved
Ethyl biscoumacetateArgatroban may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
EtodolacEtodolac may increase the anticoagulant activities of Argatroban.Approved, Investigational, Vet Approved
EtofenamateEtofenamate may increase the anticoagulant activities of Argatroban.Approved, Investigational
EtonogestrelThe therapeutic efficacy of Argatroban can be decreased when used in combination with Etonogestrel.Approved, Investigational
EtoricoxibEtoricoxib may increase the anticoagulant activities of Argatroban.Approved, Investigational
EtravirineThe serum concentration of Etravirine can be decreased when it is combined with Argatroban.Approved
Evening primrose oilEvening primrose oil may increase the anticoagulant activities of Argatroban.Approved, Investigational
exisulindexisulind may increase the anticoagulant activities of Argatroban.Investigational
FelbinacFelbinac may increase the anticoagulant activities of Argatroban.Experimental
FenbufenFenbufen may increase the anticoagulant activities of Argatroban.Approved
FenoprofenFenoprofen may increase the anticoagulant activities of Argatroban.Approved
FentiazacFentiazac may increase the anticoagulant activities of Argatroban.Experimental
FeprazoneFeprazone may increase the anticoagulant activities of Argatroban.Experimental
Ferulic acidFerulic acid may increase the anticoagulant activities of Argatroban.Experimental
FibrinolysinFibrinolysin may increase the anticoagulant activities of Argatroban.Investigational
FloctafenineFloctafenine may increase the anticoagulant activities of Argatroban.Approved, Withdrawn
FluconazoleThe metabolism of Argatroban can be decreased when combined with Fluconazole.Approved
FluindioneArgatroban may increase the anticoagulant activities of Fluindione.Investigational
FlunixinFlunixin may increase the anticoagulant activities of Argatroban.Vet Approved
FlunoxaprofenFlunoxaprofen may increase the anticoagulant activities of Argatroban.Experimental
FlurbiprofenFlurbiprofen may increase the anticoagulant activities of Argatroban.Approved, Investigational
FluvoxamineThe metabolism of Argatroban can be decreased when combined with Fluvoxamine.Approved, Investigational
FondaparinuxArgatroban may increase the anticoagulant activities of Fondaparinux.Investigational
Fondaparinux sodiumArgatroban may increase the anticoagulant activities of Fondaparinux sodium.Approved, Investigational
FosamprenavirThe metabolism of Argatroban can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Argatroban can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Argatroban can be increased when combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Argatroban can be increased when it is combined with Fusidic Acid.Approved
GabexateArgatroban may increase the anticoagulant activities of Gabexate.Investigational
GarlicThe serum concentration of Argatroban can be decreased when it is combined with Garlic.Approved
GenisteinGenistein may decrease the anticoagulant activities of Argatroban.Investigational
GestodeneThe therapeutic efficacy of Argatroban can be decreased when used in combination with Gestodene.Approved, Investigational
GestonoroneThe therapeutic efficacy of Argatroban can be decreased when used in combination with Gestonorone.Experimental
GestrinoneThe therapeutic efficacy of Argatroban can be decreased when used in combination with Gestrinone.Approved
GlucosamineGlucosamine may increase the antiplatelet activities of Argatroban.Approved
GuacetisalThe risk or severity of adverse effects can be increased when Argatroban is combined with Guacetisal.Experimental
HeminHemin may increase the anticoagulant activities of Argatroban.Approved
Hemoglobin crosfumarilThe risk or severity of adverse effects can be increased when Argatroban is combined with Hemoglobin crosfumaril.Experimental
HeparinArgatroban may increase the anticoagulant activities of Heparin.Approved, Investigational
HexestrolThe serum concentration of Hexestrol can be decreased when it is combined with Argatroban.Withdrawn
HigenamineHigenamine may increase the anticoagulant activities of Argatroban.Investigational
Hydroxyprogesterone caproateThe therapeutic efficacy of Argatroban can be decreased when used in combination with Hydroxyprogesterone caproate.Approved
HydroxytyrosolHydroxytyrosol may increase the anticoagulant activities of Argatroban.Investigational
Ibritumomab tiuxetanThe risk or severity of adverse effects can be increased when Argatroban is combined with Ibritumomab tiuxetan.Approved
IbrutinibThe risk or severity of adverse effects can be increased when Ibrutinib is combined with Argatroban.Approved
IbudilastIbudilast may increase the anticoagulant activities of Argatroban.Approved, Investigational
IbuprofenIbuprofen may increase the anticoagulant activities of Argatroban.Approved
IbuproxamIbuproxam may increase the anticoagulant activities of Argatroban.Withdrawn
IcatibantIcatibant may increase the anticoagulant activities of Argatroban.Approved
Icosapent ethylIcosapent ethyl may increase the anticoagulant activities of Argatroban.Approved, Nutraceutical
IdelalisibThe serum concentration of Argatroban can be increased when it is combined with Idelalisib.Approved
IdraparinuxArgatroban may increase the anticoagulant activities of Idraparinux.Investigational
IfenprodilIfenprodil may increase the anticoagulant activities of Argatroban.Approved, Investigational, Withdrawn
IfetrobanIfetroban may increase the anticoagulant activities of Argatroban.Investigational
IloprostIloprost may increase the antiplatelet activities of Argatroban.Approved, Investigational
ImatinibThe metabolism of Argatroban can be decreased when combined with Imatinib.Approved
Imidazole salicylateImidazole salicylate may increase the anticoagulant activities of Argatroban.Experimental
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Argatroban.Approved
IndinavirThe metabolism of Argatroban can be decreased when combined with Indinavir.Approved
IndobufenIndobufen may increase the anticoagulant activities of Argatroban.Investigational
IndomethacinIndomethacin may increase the anticoagulant activities of Argatroban.Approved, Investigational
IndoprofenIndoprofen may increase the anticoagulant activities of Argatroban.Withdrawn
IprindoleThe serum concentration of Iprindole can be increased when it is combined with Argatroban.Experimental
IsavuconazoniumThe metabolism of Argatroban can be decreased when combined with Isavuconazonium.Approved, Investigational
IsoxicamIsoxicam may increase the anticoagulant activities of Argatroban.Withdrawn
IsradipineThe metabolism of Argatroban can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Argatroban can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Argatroban can be increased when it is combined with Ivacaftor.Approved
KebuzoneKebuzone may increase the anticoagulant activities of Argatroban.Experimental
KetanserinKetanserin may increase the anticoagulant activities of Argatroban.Investigational
KetoconazoleThe metabolism of Argatroban can be decreased when combined with Ketoconazole.Approved, Investigational
KetoprofenKetoprofen may increase the anticoagulant activities of Argatroban.Approved, Vet Approved
KetorolacKetorolac may increase the anticoagulant activities of Argatroban.Approved
LeflunomideLeflunomide may increase the anticoagulant activities of Argatroban.Approved, Investigational
LepirudinLepirudin may increase the anticoagulant activities of Argatroban.Approved
LetaxabanArgatroban may increase the anticoagulant activities of Letaxaban.Investigational
LimaprostThe risk or severity of adverse effects can be increased when Limaprost is combined with Argatroban.Approved, Investigational
LinsidomineLinsidomine may increase the anticoagulant activities of Argatroban.Experimental
LisofyllineLisofylline may increase the anticoagulant activities of Argatroban.Investigational
LofepramineThe serum concentration of Lofepramine can be increased when it is combined with Argatroban.Experimental
LonazolacLonazolac may increase the anticoagulant activities of Argatroban.Experimental
LopinavirThe metabolism of Argatroban can be decreased when combined with Lopinavir.Approved
LornoxicamLornoxicam may increase the anticoagulant activities of Argatroban.Approved, Investigational
LovastatinThe serum concentration of Lovastatin can be increased when it is combined with Argatroban.Approved, Investigational
LoxoprofenLoxoprofen may increase the anticoagulant activities of Argatroban.Approved, Investigational
LuliconazoleThe serum concentration of Argatroban can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Argatroban can be increased when combined with Lumacaftor.Approved
LumiracoxibLumiracoxib may increase the anticoagulant activities of Argatroban.Approved, Investigational
Magnesium salicylateMagnesium salicylate may increase the anticoagulant activities of Argatroban.Approved
MasoprocolMasoprocol may increase the anticoagulant activities of Argatroban.Approved, Investigational
Meclofenamic acidMeclofenamic acid may increase the anticoagulant activities of Argatroban.Approved, Vet Approved
MedrogestoneThe therapeutic efficacy of Argatroban can be decreased when used in combination with Medrogestone.Approved
Medroxyprogesterone acetateThe therapeutic efficacy of Argatroban can be decreased when used in combination with Medroxyprogesterone acetate.Approved, Investigational
Mefenamic acidMefenamic acid may increase the anticoagulant activities of Argatroban.Approved
MelagatranArgatroban may increase the anticoagulant activities of Melagatran.Experimental
MeloxicamMeloxicam may increase the anticoagulant activities of Argatroban.Approved, Vet Approved
MesalazineThe risk or severity of adverse effects can be increased when Argatroban is combined with Mesalazine.Approved
MestranolThe serum concentration of Mestranol can be decreased when it is combined with Argatroban.Approved
MetamizoleMetamizole may increase the anticoagulant activities of Argatroban.Investigational, Withdrawn
MethallenestrilThe serum concentration of Methallenestril can be decreased when it is combined with Argatroban.Experimental
MethylergometrineThe serum concentration of Methylergometrine can be increased when it is combined with Argatroban.Approved
MethylestrenoloneThe therapeutic efficacy of Argatroban can be decreased when used in combination with Methylestrenolone.Experimental
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Argatroban.Approved, Illicit
MifepristoneThe serum concentration of Argatroban can be increased when it is combined with Mifepristone.Approved, Investigational
MilrinoneMilrinone may increase the anticoagulant activities of Argatroban.Approved
MirtazapineThe serum concentration of Mirtazapine can be increased when it is combined with Argatroban.Approved
MitotaneThe serum concentration of Argatroban can be decreased when it is combined with Mitotane.Approved
MizoribineMizoribine may increase the anticoagulant activities of Argatroban.Investigational
MofebutazoneMofebutazone may increase the anticoagulant activities of Argatroban.Experimental
MoxestrolMoxestrol may decrease the anticoagulant activities of Argatroban.Experimental
Mycophenolate mofetilMycophenolate mofetil may increase the anticoagulant activities of Argatroban.Approved, Investigational
Mycophenolic acidMycophenolic acid may increase the anticoagulant activities of Argatroban.Approved
NabumetoneNabumetone may increase the anticoagulant activities of Argatroban.Approved
NadroparinArgatroban may increase the anticoagulant activities of Nadroparin.Approved
NafamostatNafamostat may increase the anticoagulant activities of Argatroban.Approved, Investigational
NaftifineNaftifine may increase the anticoagulant activities of Argatroban.Approved
NaftopidilNaftopidil may increase the anticoagulant activities of Argatroban.Investigational
NaproxenNaproxen may increase the anticoagulant activities of Argatroban.Approved, Vet Approved
NefazodoneThe serum concentration of Nefazodone can be increased when it is combined with Argatroban.Approved, Withdrawn
NelfinavirThe metabolism of Argatroban can be decreased when combined with Nelfinavir.Approved
NepafenacNepafenac may increase the anticoagulant activities of Argatroban.Approved
NetupitantThe serum concentration of Argatroban can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Argatroban can be increased when combined with Nevirapine.Approved
NifenazoneNifenazone may increase the anticoagulant activities of Argatroban.Experimental
Niflumic AcidNiflumic Acid may increase the anticoagulant activities of Argatroban.Approved
NilotinibThe metabolism of Argatroban can be decreased when combined with Nilotinib.Approved, Investigational
NimesulideNimesulide may increase the anticoagulant activities of Argatroban.Approved, Investigational, Withdrawn
NintedanibThe risk or severity of adverse effects can be increased when Argatroban is combined with Nintedanib.Approved
NitroaspirinThe risk or severity of adverse effects can be increased when Argatroban is combined with Nitroaspirin.Investigational
NomegestrolThe therapeutic efficacy of Argatroban can be decreased when used in combination with Nomegestrol.Approved
NorethisteroneThe therapeutic efficacy of Argatroban can be decreased when used in combination with Norethisterone.Approved
NorgestrienoneThe therapeutic efficacy of Argatroban can be decreased when used in combination with Norgestrienone.Experimental
NortriptylineThe serum concentration of Nortriptyline can be increased when it is combined with Argatroban.Approved
ObinutuzumabThe risk or severity of adverse effects can be increased when Argatroban is combined with Obinutuzumab.Approved
OlaparibThe metabolism of Argatroban can be decreased when combined with Olaparib.Approved
OlopatadineOlopatadine may increase the anticoagulant activities of Argatroban.Approved
OlsalazineOlsalazine may increase the anticoagulant activities of Argatroban.Approved
Omacetaxine mepesuccinateThe risk or severity of adverse effects can be increased when Argatroban is combined with Omacetaxine mepesuccinate.Approved
Omega-3 fatty acidsOmega-3 fatty acids may increase the anticoagulant activities of Argatroban.Approved, Nutraceutical
OpipramolThe serum concentration of Opipramol can be increased when it is combined with Argatroban.Investigational
OrgoteinOrgotein may increase the anticoagulant activities of Argatroban.Vet Approved
OsimertinibThe serum concentration of Argatroban can be increased when it is combined with Osimertinib.Approved
OtamixabanArgatroban may increase the anticoagulant activities of Otamixaban.Investigational
OxaprozinOxaprozin may increase the anticoagulant activities of Argatroban.Approved
OxyphenbutazoneOxyphenbutazone may increase the anticoagulant activities of Argatroban.Approved, Withdrawn
OzagrelOzagrel may increase the anticoagulant activities of Argatroban.Investigational
PalbociclibThe serum concentration of Argatroban can be increased when it is combined with Palbociclib.Approved
ParecoxibParecoxib may increase the anticoagulant activities of Argatroban.Approved
ParnaparinParnaparin may increase the anticoagulant activities of Argatroban.Approved, Investigational
ParthenolideParthenolide may increase the anticoagulant activities of Argatroban.Investigational
PentobarbitalThe metabolism of Argatroban can be increased when combined with Pentobarbital.Approved, Vet Approved
Pentosan PolysulfatePentosan Polysulfate may increase the anticoagulant activities of Argatroban.Approved
PentoxifyllinePentoxifylline may increase the antiplatelet activities of Argatroban.Approved, Investigational
PethidineThe risk or severity of adverse effects can be increased when Argatroban is combined with Pethidine.Approved
PhenindioneArgatroban may increase the anticoagulant activities of Phenindione.Approved, Investigational
PhenobarbitalThe metabolism of Argatroban can be increased when combined with Phenobarbital.Approved
PhenprocoumonArgatroban may increase the anticoagulant activities of Phenprocoumon.Approved, Investigational
PhenylbutazonePhenylbutazone may increase the anticoagulant activities of Argatroban.Approved, Vet Approved
PhenytoinThe metabolism of Argatroban can be increased when combined with Phenytoin.Approved, Vet Approved
PicotamidePicotamide may increase the anticoagulant activities of Argatroban.Experimental
PimecrolimusPimecrolimus may increase the anticoagulant activities of Argatroban.Approved, Investigational
PimozideThe serum concentration of Pimozide can be increased when it is combined with Argatroban.Approved
PirfenidonePirfenidone may increase the anticoagulant activities of Argatroban.Approved, Investigational
PiroxicamPiroxicam may increase the anticoagulant activities of Argatroban.Approved, Investigational
PirprofenPirprofen may increase the anticoagulant activities of Argatroban.Experimental
Polyestradiol phosphatePolyestradiol phosphate may decrease the anticoagulant activities of Argatroban.Approved
PosaconazoleThe metabolism of Argatroban can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PranoprofenPranoprofen may increase the anticoagulant activities of Argatroban.Experimental, Investigational
PrasugrelPrasugrel may increase the anticoagulant activities of Argatroban.Approved
PrimidoneThe metabolism of Argatroban can be increased when combined with Primidone.Approved, Vet Approved
ProgesteroneThe therapeutic efficacy of Argatroban can be decreased when used in combination with Progesterone.Approved, Vet Approved
ProglumetacinProglumetacin may increase the anticoagulant activities of Argatroban.Experimental
PromegestoneThe therapeutic efficacy of Argatroban can be decreased when used in combination with Promegestone.Experimental
PromestrienePromestriene may decrease the anticoagulant activities of Argatroban.Investigational
PropacetamolPropacetamol may increase the anticoagulant activities of Argatroban.Approved, Investigational
PropyphenazonePropyphenazone may increase the anticoagulant activities of Argatroban.Experimental
ProquazoneProquazone may increase the anticoagulant activities of Argatroban.Experimental
Protein CArgatroban may increase the anticoagulant activities of Protein C.Approved
Protein S humanArgatroban may increase the anticoagulant activities of Protein S human.Approved
ProtocatechualdehydeArgatroban may increase the anticoagulant activities of Protocatechualdehyde.Approved
ProtriptylineThe serum concentration of Protriptyline can be increased when it is combined with Argatroban.Approved
PTC299PTC299 may increase the anticoagulant activities of Argatroban.Investigational
QuinestrolQuinestrol may decrease the anticoagulant activities of Argatroban.Approved
RamatrobanRamatroban may increase the anticoagulant activities of Argatroban.Investigational
RanolazineThe metabolism of Argatroban can be decreased when combined with Ranolazine.Approved, Investigational
ResveratrolResveratrol may increase the anticoagulant activities of Argatroban.Approved, Experimental, Investigational
ReteplaseReteplase may increase the anticoagulant activities of Argatroban.Approved
ReviparinArgatroban may increase the anticoagulant activities of Reviparin.Approved, Investigational
RidogrelRidogrel may increase the anticoagulant activities of Argatroban.Approved
RifabutinThe metabolism of Argatroban can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Argatroban can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Argatroban can be increased when combined with Rifapentine.Approved
RiociguatThe serum concentration of Riociguat can be increased when it is combined with Argatroban.Approved
RitonavirThe metabolism of Argatroban can be decreased when combined with Ritonavir.Approved, Investigational
RofecoxibRofecoxib may increase the anticoagulant activities of Argatroban.Investigational, Withdrawn
RosiglitazoneRosiglitazone may increase the anticoagulant activities of Argatroban.Approved, Investigational
RosuvastatinThe serum concentration of Rosuvastatin can be increased when it is combined with Argatroban.Approved
SalicylamideSalicylamide may increase the anticoagulant activities of Argatroban.Approved
Salicylic acidThe risk or severity of adverse effects can be increased when Argatroban is combined with Salicylic acid.Approved, Vet Approved
SalsalateSalsalate may increase the anticoagulant activities of Argatroban.Approved
SaquinavirThe metabolism of Argatroban can be decreased when combined with Saquinavir.Approved, Investigational
SarpogrelateSarpogrelate may increase the anticoagulant activities of Argatroban.Investigational
SaruplaseSaruplase may increase the anticoagulant activities of Argatroban.Experimental
SecoisolariciresinolSecoisolariciresinol may decrease the anticoagulant activities of Argatroban.Investigational
SelexipagSelexipag may increase the anticoagulant activities of Argatroban.Approved
SemapimodSemapimod may increase the anticoagulant activities of Argatroban.Investigational
SeratrodastSeratrodast may increase the anticoagulant activities of Argatroban.Approved
SerrapeptaseSerrapeptase may increase the anticoagulant activities of Argatroban.Investigational
SevofluraneSevoflurane may increase the anticoagulant activities of Argatroban.Approved, Vet Approved
SildenafilThe serum concentration of Sildenafil can be increased when it is combined with Argatroban.Approved, Investigational
SiltuximabThe serum concentration of Argatroban can be decreased when it is combined with Siltuximab.Approved
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Argatroban.Approved
SRT501SRT501 may increase the anticoagulant activities of Argatroban.Investigational
St. John's WortThe serum concentration of Argatroban can be decreased when it is combined with St. John's Wort.Investigational, Nutraceutical
StiripentolThe serum concentration of Argatroban can be increased when it is combined with Stiripentol.Approved
StreptokinaseStreptokinase may increase the anticoagulant activities of Argatroban.Approved, Investigational
SugammadexSugammadex may increase the anticoagulant activities of Argatroban.Approved
SulfasalazineSulfasalazine may increase the anticoagulant activities of Argatroban.Approved
SulfisoxazoleThe metabolism of Argatroban can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SulindacSulindac may increase the anticoagulant activities of Argatroban.Approved
SulodexideArgatroban may increase the anticoagulant activities of Sulodexide.Approved, Investigational
SuprofenSuprofen may increase the anticoagulant activities of Argatroban.Approved, Withdrawn
SuxibuzoneSuxibuzone may increase the anticoagulant activities of Argatroban.Experimental
Synthetic Conjugated Estrogens, AThe serum concentration of Synthetic Conjugated Estrogens, A can be decreased when it is combined with Argatroban.Approved
Synthetic Conjugated Estrogens, BSynthetic Conjugated Estrogens, B may decrease the anticoagulant activities of Argatroban.Approved
TacrolimusThe metabolism of Tacrolimus can be decreased when combined with Argatroban.Approved, Investigational
TarenflurbilTarenflurbil may increase the anticoagulant activities of Argatroban.Investigational
TelaprevirThe metabolism of Argatroban can be decreased when combined with Telaprevir.Approved, Withdrawn
TelithromycinThe metabolism of Argatroban can be decreased when combined with Telithromycin.Approved
TemsirolimusThe risk or severity of adverse effects can be increased when Argatroban is combined with Temsirolimus.Approved
TenecteplaseTenecteplase may increase the anticoagulant activities of Argatroban.Approved
TenidapTenidap may increase the anticoagulant activities of Argatroban.Experimental
TenoxicamTenoxicam may increase the anticoagulant activities of Argatroban.Approved
TepoxalinTepoxalin may increase the anticoagulant activities of Argatroban.Vet Approved
TeriflunomideTeriflunomide may increase the anticoagulant activities of Argatroban.Approved
TesmilifeneTesmilifene may increase the anticoagulant activities of Argatroban.Investigational
TheophyllineThe serum concentration of Theophylline can be decreased when it is combined with Argatroban.Approved
TianeptineThe serum concentration of Tianeptine can be increased when it is combined with Argatroban.Approved, Investigational
Tiaprofenic acidTiaprofenic acid may increase the anticoagulant activities of Argatroban.Approved
TiboloneTibolone may increase the anticoagulant activities of Argatroban.Approved, Investigational
TicagrelorTicagrelor may increase the anticoagulant activities of Argatroban.Approved
TiclopidineThe metabolism of Argatroban can be decreased when combined with Ticlopidine.Approved
TinoridineTinoridine may increase the anticoagulant activities of Argatroban.Investigational
TinzaparinTinzaparin may increase the anticoagulant activities of Argatroban.Approved
TioclomarolTioclomarol may increase the anticoagulant activities of Argatroban.Experimental
TipranavirTipranavir may increase the anticoagulant activities of Argatroban.Approved, Investigational
TirofibanTirofiban may increase the anticoagulant activities of Argatroban.Approved
TocilizumabThe serum concentration of Argatroban can be decreased when it is combined with Tocilizumab.Approved
Tolfenamic AcidTolfenamic Acid may increase the anticoagulant activities of Argatroban.Approved
TolmetinTolmetin may increase the anticoagulant activities of Argatroban.Approved
TositumomabThe risk or severity of adverse effects can be increased when Argatroban is combined with Tositumomab.Approved, Investigational
TranilastTranilast may increase the anticoagulant activities of Argatroban.Approved, Investigational
TrapidilTrapidil may increase the anticoagulant activities of Argatroban.Approved
TreprostinilTreprostinil may increase the antiplatelet activities of Argatroban.Approved, Investigational
TriazolamThe serum concentration of Triazolam can be increased when it is combined with Argatroban.Approved
TribenosideTribenoside may increase the anticoagulant activities of Argatroban.Experimental
TriflusalTriflusal may increase the anticoagulant activities of Argatroban.Approved, Investigational
TrimipramineThe serum concentration of Trimipramine can be increased when it is combined with Argatroban.Approved
TriptolideTriptolide may increase the anticoagulant activities of Argatroban.Investigational
TroxerutinArgatroban may increase the anticoagulant activities of Troxerutin.Investigational
UrokinaseUrokinase may increase the anticoagulant activities of Argatroban.Approved, Investigational, Withdrawn
ValdecoxibValdecoxib may increase the anticoagulant activities of Argatroban.Investigational, Withdrawn
Valproic AcidThe serum concentration of Valproic Acid can be decreased when it is combined with Argatroban.Approved, Investigational
VenlafaxineThe metabolism of Argatroban can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Verapamil can be decreased when combined with Argatroban.Approved
Vitamin EVitamin E may increase the anticoagulant activities of Argatroban.Approved, Nutraceutical, Vet Approved
VorapaxarThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Argatroban.Approved
VoriconazoleThe metabolism of Argatroban can be decreased when combined with Voriconazole.Approved, Investigational
WarfarinArgatroban may increase the anticoagulant activities of Warfarin.Approved
XimelagatranArgatroban may increase the anticoagulant activities of Ximelagatran.Approved, Investigational, Withdrawn
ZaltoprofenZaltoprofen may increase the anticoagulant activities of Argatroban.Approved, Investigational
ZeranolZeranol may decrease the anticoagulant activities of Argatroban.Vet Approved
ZidovudineThe serum concentration of Zidovudine can be decreased when it is combined with Argatroban.Approved
ZileutonZileuton may increase the anticoagulant activities of Argatroban.Approved, Investigational, Withdrawn
ZiprasidoneThe metabolism of Argatroban can be decreased when combined with Ziprasidone.Approved
ZomepiracZomepirac may increase the anticoagulant activities of Argatroban.Withdrawn
Food Interactions
  • Herbs and food with anticoagulant/antiplatelet activity. Major interactions may occur with danshen, dong quai, evening primrose oil, gingko, policosanol, willow bark

References

Synthesis Reference

Tomiya Mano, Jin Shiomura, "Argatroban preparations for ophthalmic use." U.S. Patent US5506241, issued October, 1986.

US5506241
General References
  1. Di Nisio M, Middeldorp S, Buller HR: Direct thrombin inhibitors. N Engl J Med. 2005 Sep 8;353(10):1028-40. [PubMed:16148288]
External Links
Human Metabolome Database
HMDB14423
KEGG Compound
C04931
PubChem Compound
152951
PubChem Substance
46507650
ChemSpider
134807
BindingDB
50101744
ChEMBL
CHEMBL59461
Therapeutic Targets Database
DAP000758
PharmGKB
PA164745516
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Argatroban
ATC Codes
B01AE03 — Argatroban
AHFS Codes
  • 20:12.04.12 — Direct Thrombin Inhibitors
FDA label
Download (83.7 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1, 2CompletedTreatmentStroke, Ischemic1
2CompletedNot AvailableStaphylococcus Aureus Bacteraemia1
2CompletedTreatmentCoronary Artery Disease / Unstable Angina (UA)1
2CompletedTreatmentHeparin-induced Thrombocytopenia Type II1
2CompletedTreatmentIschemia, Cerebral / Strokes1
2RecruitingTreatmentAchievement of a Sufficient Thrombosis Prohpylaxis in Clitically Ill Patients With Heparin Resistance1
2TerminatedTreatmentStroke, Ischemic1
3CompletedTreatmentCardiac surgery, heparin-induced thrombocytopenia and thrombosis syndrome1
3RecruitingTreatmentArgatroban / Low Molecular Weight Heparin / Neoplasms, Gynecologic / Venous Thromboembolism1
4CompletedTreatmentCVD2
4CompletedTreatmentKidney Failure,Chronic / Renal Disease, End-Stage1
4CompletedTreatmentThrombocytopenias / Thrombosis1
4TerminatedNot AvailableCoronary Artery Bypass Graft Surgery / Presence of Heparin/Platelet Factor 4 Antibody1
4TerminatedTreatmentCardiac surgery, heparin-induced thrombocytopenia and thrombosis syndrome1
Not AvailableCompletedNot AvailableAcute HIT II (Heparin-induced Thrombocytopenia Type II)1

Pharmacoeconomics

Manufacturers
Packagers
Dosage forms
FormRouteStrength
InjectionIntravenous1 mg/mL
InjectionIntravenous250 mg/2.5mL
InjectionIntravenous50 mg/50mL
Injection, solutionIntravenous1 mg/mL
Injection, solutionIntravenous100 mg/mL
SolutionIntravenous100 mg
SolutionIntravenous125 mg/125mL
Prices
Unit descriptionCostUnit
Argatroban 100 mg/ml Solution 2.5ml Vial1546.46USD vial
Argatroban 100 mg/ml vial743.49USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5214052No1994-06-302014-06-30Us
US7589106No2007-09-262027-09-26Us
US7687516No2007-09-262027-09-26Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
logP1Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.221 mg/mLALOGPS
logP0.19ALOGPS
logP-0.97ChemAxon
logS-3.4ALOGPS
pKa (Strongest Acidic)3.07ChemAxon
pKa (Strongest Basic)10.91ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count9ChemAxon
Hydrogen Donor Count5ChemAxon
Polar Surface Area180.21 Å2ChemAxon
Rotatable Bond Count8ChemAxon
Refractivity133.54 m3·mol-1ChemAxon
Polarizability53.9 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.6195
Blood Brain Barrier-0.8933
Caco-2 permeable-0.7293
P-glycoprotein substrateSubstrate0.8193
P-glycoprotein inhibitor INon-inhibitor0.6701
P-glycoprotein inhibitor IINon-inhibitor0.6802
Renal organic cation transporterNon-inhibitor0.8147
CYP450 2C9 substrateNon-substrate0.5571
CYP450 2D6 substrateNon-substrate0.8861
CYP450 3A4 substrateNon-substrate0.5477
CYP450 1A2 substrateNon-inhibitor0.8849
CYP450 2C9 inhibitorNon-inhibitor0.662
CYP450 2D6 inhibitorNon-inhibitor0.8789
CYP450 2C19 inhibitorNon-inhibitor0.7706
CYP450 3A4 inhibitorNon-inhibitor0.8316
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9636
Ames testNon AMES toxic0.6238
CarcinogenicityNon-carcinogens0.7551
BiodegradationNot ready biodegradable0.9966
Rat acute toxicity1.5767 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9833
hERG inhibition (predictor II)Non-inhibitor0.6071
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as dipeptides. These are organic compounds containing a sequence of exactly two alpha-amino acids joined by a peptide bond.
Kingdom
Organic compounds
Super Class
Organic acids and derivatives
Class
Carboxylic acids and derivatives
Sub Class
Amino acids, peptides, and analogues
Direct Parent
Dipeptides
Alternative Parents
Alpha amino acid amides / Hydroquinolines / Piperidinecarboxylic acids / N-acylpiperidines / Secondary alkylarylamines / Aralkylamines / Benzenoids / Organosulfonamides / Tertiary carboxylic acid amides / Aminosulfonyl compounds
show 11 more
Substituents
Alpha-dipeptide / Alpha-amino acid amide / Alpha-amino acid or derivatives / Tetrahydroquinoline / N-acyl-piperidine / Piperidinecarboxylic acid / Secondary aliphatic/aromatic amine / Aralkylamine / Piperidine / Organosulfonic acid amide
show 29 more
Molecular Framework
Aromatic heteropolycyclic compounds
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. Kawada T, Okada Y, Hoson M, Endo S, Yokoyama M, Kitanaka Y, Kimura K, Abe H, Yamate N: Argatroban, an attractive anticoagulant, for left heart bypass with centrifugal pump for repair of traumatic aortic rupture. Jpn J Thorac Cardiovasc Surg. 1999 Mar;47(3):104-9. [PubMed:10226408]
  2. Sakai M, Ohteki H, Narita Y, Naitoh K, Natsuaki M, Itoh T: Argatroban as a potential anticoagulant in cardiopulmonary bypass-studies in a dog model. Cardiovasc Surg. 1999 Mar;7(2):187-94. [PubMed:10353669]
  3. Jang IK, Brown DF, Giugliano RP, Anderson HV, Losordo D, Nicolau JC, Dutra OP, Bazzino O, Viamonte VM, Norbady R, Liprandi AS, Massey TJ, Dinsmore R, Schwarz RP Jr: A multicenter, randomized study of argatroban versus heparin as adjunct to tissue plasminogen activator (TPA) in acute myocardial infarction: myocardial infarction with novastan and TPA (MINT) study. J Am Coll Cardiol. 1999 Jun;33(7):1879-85. [PubMed:10362188]
  4. Matsuo T, Kario K, Matsuda S, Yamaguchi N, Kakishita E: Effect of Thrombin Inhibition on Patients with Peripheral Arterial Obstructive Disease: A Multicenter Clinical Trial of Argatroban. J Thromb Thrombolysis. 1995;2(2):131-136. [PubMed:10608016]
  5. Serebruany VL, Jang IK, Giugliano RP, Massey TJ, Schwarz Jr RP: A Randomized, Blinded Study of Two Doses of Novastan(R) (Brand of Argatroban) Versus Heparin as Adjunctive Therapy to Recombinant Tissue Plasminogen Activator (Accelerated Administration) in Acute Myocardial Infarction: Rationale and Design of the Myocardial Infarction using Novastan(R) and T-PA (MINT) Study. J Thromb Thrombolysis. 1998;5(1):49-52. [PubMed:10608050]
  6. 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
Vitamin d3 25-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 performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 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]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
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 un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 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]

Drug created on June 13, 2005 07:24 / Updated on November 13, 2017 21:49