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Identification
NameAnistreplase
Accession NumberDB00029  (BTD00102, BIOD00102)
TypeBiotech
GroupsApproved
DescriptionHuman tissue plasminogen activator, purified, glycosylated, 527 residues purified from CHO cells. Eminase is a lyophilized (freeze-dried) formulation of anistreplase, the p-anisoyl derivative of the primary Lys-plasminogen-streptokinase activator complex (a complex of Lys-plasminogen and streptokinase). A p-anisoyl group is chemically conjugated to a complex of bacterial-derived streptokinase and human Plasma-derived Lys-plasminogen proteins.
Protein structureDb00029
Related Articles
Protein chemical formulaC2569H3928N746O781S40
Protein average weight59042.3 Da
Sequences
>DB00029 sequence
SYQVICRDEKTQMIYQQHQSWLRPVLRSNRVEYCWCNSGRAQCHSVPVKSCSEPRCFNGG
TCQQALYFSDFVCQCPEGFAGKCCEIDTRATCYEDQGISYRGTWSTAESGAECTNWNSSA
LAQKPYSGRRPDAIRLGLGNHNYCRNPDRDSKPWCYVFKAGKYSSEFCSTPACSEGNSDC
YFGNGSAYRGTHSLTESGASCLPWNSMILIGKVYTAQNPSAQALGLGKHNYCRNPDGDAK
PWCHVLKNRRLTWEYCDVPSCSTCGLRQYSQPQFRIKGGLFADIASHPWQAAIFAKHRRS
PGERFLCGGILISSCWILSAAHCFQERFPPHHLTVILGRTYRVVPGEEEQKFEVEKYIVH
KEFDDDTYDNDIALLQLKSDSSRCAQESSVVRTVCLPPADLQLPDWTECELSGYGKHEAL
SPFYSERLKEAHVRLYPSSRCTSQHLLNRTVTDNMLCAGDTRSGGPQANLHDACQGDSGG
PLVCLNDGRMTLVGIISWGLGCGQKDVPGVYTKVTNYLDWIRDNMRP
Download FASTA Format
Synonyms
t- PA
t-plasminogen activator
Tissue-type plasminogen activator precursor
tPA
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Eminase 30 UnitsPowder, for solution30 unitIntravenousWellspring Pharmaceutical Canada Corp1997-12-152009-02-23Canada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
EminaseWulfing Pharma GmbH
Brand mixturesNot Available
SaltsNot Available
Categories
UNII5O8V541HJ6
CAS number81669-57-0
Pharmacology
IndicationFor lysis of acute pulmonary emboli, intracoronary emboli and management of myocardial infarction
Structured Indications Not Available
PharmacodynamicsAnistreplase cleaves the Arg/Val bond in plasminogen to form plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action. This helps eliminate blood clots or arterial blockages that cause myocardial infarction.
Mechanism of actionAnistreplase cleaves the Arg/Val bond in plasminogen to form plasmin. This in turn leads to the degradation of blood clots.
TargetKindPharmacological actionActionsOrganismUniProt ID
PlasminogenProteinyes
activator
HumanP00747 details
Fibrinogen alpha chainProteinyesNot AvailableHumanP02671 details
Urokinase plasminogen activator surface receptorProteinunknownNot AvailableHumanQ03405 details
Plasminogen activator inhibitor 1ProteinunknownNot AvailableHumanP05121 details
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Anistreplase Action PathwayDrug actionSMP00281
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
AbciximabAnistreplase may increase the anticoagulant activities of Abciximab.Approved
AcenocoumarolAnistreplase may increase the anticoagulant activities of Acenocoumarol.Approved
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Anistreplase.Approved, Vet Approved
AlprostadilAlprostadil may increase the anticoagulant activities of Anistreplase.Approved, Investigational
Aminosalicylic AcidThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Anistreplase.Approved
AnagrelideAnagrelide may increase the anticoagulant activities of Anistreplase.Approved
AncrodAnistreplase may increase the anticoagulant activities of Ancrod.Investigational
Antithrombin III humanAnistreplase may increase the anticoagulant activities of Antithrombin III human.Approved
ApixabanAnistreplase may increase the anticoagulant activities of Apixaban.Approved
AprotininThe therapeutic efficacy of Anistreplase can be decreased when used in combination with Aprotinin.Approved, Withdrawn
ArdeparinAnistreplase may increase the anticoagulant activities of Ardeparin.Approved, Withdrawn
ArgatrobanAnistreplase may increase the anticoagulant activities of Argatroban.Approved, Investigational
AzelastineAzelastine may increase the anticoagulant activities of Anistreplase.Approved
BalsalazideThe risk or severity of adverse effects can be increased when Balsalazide is combined with Anistreplase.Approved, Investigational
BecaplerminAnistreplase may increase the anticoagulant activities of Becaplermin.Approved, Investigational
BeraprostBeraprost may increase the anticoagulant activities of Anistreplase.Investigational
BivalirudinAnistreplase may increase the anticoagulant activities of Bivalirudin.Approved, Investigational
ButylphthalideButylphthalide may increase the anticoagulant activities of Anistreplase.Investigational
CangrelorCangrelor may increase the anticoagulant activities of Anistreplase.Approved
CertoparinAnistreplase may increase the anticoagulant activities of Certoparin.Approved
CilostazolCilostazol may increase the anticoagulant activities of Anistreplase.Approved
Citric AcidAnistreplase may increase the anticoagulant activities of Citric Acid.Nutraceutical, Vet Approved
ClopidogrelClopidogrel may increase the anticoagulant activities of Anistreplase.Approved, Nutraceutical
Dabigatran etexilateAnistreplase may increase the anticoagulant activities of Dabigatran etexilate.Approved
DalteparinAnistreplase may increase the anticoagulant activities of Dalteparin.Approved
DanaparoidAnistreplase may increase the anticoagulant activities of Danaparoid.Approved, Withdrawn
DefibrotideDefibrotide may increase the anticoagulant activities of Anistreplase.Approved, Investigational
dersalazineThe risk or severity of adverse effects can be increased when dersalazine is combined with Anistreplase.Investigational
DesirudinAnistreplase may increase the anticoagulant activities of Desirudin.Approved
DextranAnistreplase may increase the anticoagulant activities of Dextran.Approved, Vet Approved
Dextran 40Anistreplase may increase the anticoagulant activities of Dextran 40.Approved
Dextran 70Anistreplase may increase the anticoagulant activities of Dextran 70.Approved
Dextran 75Anistreplase may increase the anticoagulant activities of Dextran 75.Approved
DicoumarolAnistreplase may increase the anticoagulant activities of Dicoumarol.Approved
DiflunisalThe risk or severity of adverse effects can be increased when Diflunisal is combined with Anistreplase.Approved
DipyridamoleDipyridamole may increase the anticoagulant activities of Anistreplase.Approved
Edetic AcidAnistreplase may increase the anticoagulant activities of Edetic Acid.Approved, Vet Approved
EdoxabanAnistreplase may increase the anticoagulant activities of Edoxaban.Approved
EnoxaparinAnistreplase may increase the anticoagulant activities of Enoxaparin.Approved
EpinastineEpinastine may increase the anticoagulant activities of Anistreplase.Approved, Investigational
eplivanserineeplivanserine may increase the anticoagulant activities of Anistreplase.Investigational
EpoprostenolEpoprostenol may increase the anticoagulant activities of Anistreplase.Approved
EptifibatideEptifibatide may increase the anticoagulant activities of Anistreplase.Approved, Investigational
Ethyl biscoumacetateAnistreplase may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
FluindioneAnistreplase may increase the anticoagulant activities of Fluindione.Investigational
FondaparinuxAnistreplase may increase the anticoagulant activities of Fondaparinux.Investigational
Fondaparinux sodiumAnistreplase may increase the anticoagulant activities of Fondaparinux sodium.Approved, Investigational
GabexateAnistreplase may increase the anticoagulant activities of Gabexate.Investigational
HeparinAnistreplase may increase the anticoagulant activities of Heparin.Approved, Investigational
HirulogAnistreplase may increase the anticoagulant activities of Hirulog.Experimental
IbudilastIbudilast may increase the anticoagulant activities of Anistreplase.Approved, Investigational
Icosapent ethylIcosapent ethyl may increase the anticoagulant activities of Anistreplase.Approved, Nutraceutical
idraparinuxAnistreplase may increase the anticoagulant activities of idraparinux.Investigational
IfenprodilIfenprodil may increase the anticoagulant activities of Anistreplase.Approved, Withdrawn
IloprostIloprost may increase the anticoagulant activities of Anistreplase.Approved, Investigational
KetanserinKetanserin may increase the anticoagulant activities of Anistreplase.Investigational
LepirudinAnistreplase may increase the anticoagulant activities of Lepirudin.Approved
LimaprostThe risk or severity of adverse effects can be increased when Limaprost is combined with Anistreplase.Approved
MesalazineThe risk or severity of adverse effects can be increased when Mesalazine is combined with Anistreplase.Approved
MilrinoneMilrinone may increase the anticoagulant activities of Anistreplase.Approved
NadroparinAnistreplase may increase the anticoagulant activities of Nadroparin.Approved
NafamostatAnistreplase may increase the anticoagulant activities of Nafamostat.Investigational
NaftopidilNaftopidil may increase the anticoagulant activities of Anistreplase.Investigational
NCX 4016The risk or severity of adverse effects can be increased when NCX 4016 is combined with Anistreplase.Investigational
NimesulideNimesulide may increase the anticoagulant activities of Anistreplase.Approved, Withdrawn
NitroaspirinThe risk or severity of adverse effects can be increased when Nitroaspirin is combined with Anistreplase.Investigational
OlsalazineThe risk or severity of adverse effects can be increased when Olsalazine is combined with Anistreplase.Approved
OtamixabanAnistreplase may increase the anticoagulant activities of Otamixaban.Investigational
Pentosan PolysulfateAnistreplase may increase the anticoagulant activities of Pentosan Polysulfate.Approved
PentoxifyllinePentoxifylline may increase the anticoagulant activities of Anistreplase.Approved, Investigational
PhenindioneAnistreplase may increase the anticoagulant activities of Phenindione.Approved
PhenprocoumonAnistreplase may increase the anticoagulant activities of Phenprocoumon.Approved
PrasugrelPrasugrel may increase the anticoagulant activities of Anistreplase.Approved
Protein CAnistreplase may increase the anticoagulant activities of Protein C.Approved
Protein S humanAnistreplase may increase the anticoagulant activities of Protein S human.Approved
ProtocatechualdehydeAnistreplase may increase the anticoagulant activities of Protocatechualdehyde.Approved
RamatrobanRamatroban may increase the anticoagulant activities of Anistreplase.Investigational
ResveratrolResveratrol may increase the anticoagulant activities of Anistreplase.Experimental, Investigational
ReviparinAnistreplase may increase the anticoagulant activities of Reviparin.Approved
RidogrelRidogrel may increase the anticoagulant activities of Anistreplase.Approved
RivaroxabanAnistreplase may increase the anticoagulant activities of Rivaroxaban.Approved
Salicylic acidThe risk or severity of adverse effects can be increased when Salicylic acid is combined with Anistreplase.Approved, Vet Approved
SCH-530348SCH-530348 may increase the anticoagulant activities of Anistreplase.Investigational
SevofluraneSevoflurane may increase the anticoagulant activities of Anistreplase.Approved, Vet Approved
SRT501SRT501 may increase the anticoagulant activities of Anistreplase.Investigational
SulodexideAnistreplase may increase the anticoagulant activities of Sulodexide.Approved, Investigational
TesmilifeneTesmilifene may increase the anticoagulant activities of Anistreplase.Investigational
TiclopidineTiclopidine may increase the anticoagulant activities of Anistreplase.Approved
TirofibanTirofiban may increase the anticoagulant activities of Anistreplase.Approved
TranilastTranilast may increase the anticoagulant activities of Anistreplase.Approved, Investigational
TrapidilTrapidil may increase the anticoagulant activities of Anistreplase.Approved
TreprostinilThe risk or severity of adverse effects can be increased when Anistreplase is combined with Treprostinil.Approved, Investigational
TriflusalTriflusal may increase the anticoagulant activities of Anistreplase.Approved
VorapaxarVorapaxar may increase the anticoagulant activities of Anistreplase.Approved
WarfarinAnistreplase may increase the anticoagulant activities of Warfarin.Approved
XimelagatranAnistreplase may increase the anticoagulant activities of Ximelagatran.Approved, Investigational, Withdrawn
Ym150Anistreplase may increase the anticoagulant activities of Ym150.Investigational
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesB01AD03
AHFS Codes
  • 20:12.20
PDB Entries
FDA labelNot Available
MSDSNot Available
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Powder, for solutionIntravenous30 unit
PricesNot Available
PatentsNot Available
Properties
StateLiquid
Experimental Properties
PropertyValueSource
melting point60 °CNovokhatny, V.V. et al., J. Biol. Chem. 266:12994-123002 (1991)
hydrophobicity-0.516Not Available
isoelectric point7.61Not Available
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
activator
General Function:
Serine-type peptidase activity
Specific Function:
Plasmin dissolves the fibrin of blood clots and acts as a proteolytic factor in a variety of other processes including embryonic development, tissue remodeling, tumor invasion, and inflammation. In ovulation, weakens the walls of the Graafian follicle. It activates the urokinase-type plasminogen activator, collagenases and several complement zymogens, such as C1 and C5. Cleavage of fibronectin ...
Gene Name:
PLG
Uniprot ID:
P00747
Molecular Weight:
90568.415 Da
References
  1. Longstaff C, Williams S, Thelwell C: Fibrin binding and the regulation of plasminogen activators during thrombolytic therapy. Cardiovasc Hematol Agents Med Chem. 2008 Jul;6(3):212-23. [PubMed:18673235 ]
  2. Melandri G, Vagnarelli F, Calabrese D, Semprini F, Nanni S, Branzi A: Review of tenecteplase (TNKase) in the treatment of acute myocardial infarction. Vasc Health Risk Manag. 2009;5(1):249-56. Epub 2009 Apr 8. [PubMed:19436656 ]
  3. Hilleman DE, Tsikouris JP, Seals AA, Marmur JD: Fibrinolytic agents for the management of ST-segment elevation myocardial infarction. Pharmacotherapy. 2007 Nov;27(11):1558-70. [PubMed:17963464 ]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
General Function:
Structural molecule activity
Specific Function:
Cleaved by the protease thrombin to yield monomers which, together with fibrinogen beta (FGB) and fibrinogen gamma (FGG), polymerize to form an insoluble fibrin matrix. Fibrin has a major function in hemostasis as one of the primary components of blood clots. In addition, functions during the early stages of wound repair to stabilize the lesion and guide cell migration during re-epithelializati...
Gene Name:
FGA
Uniprot ID:
P02671
Molecular Weight:
94972.455 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Urokinase plasminogen activator receptor activity
Specific Function:
Acts as a receptor for urokinase plasminogen activator. Plays a role in localizing and promoting plasmin formation. Mediates the proteolysis-independent signal transduction activation effects of U-PA. It is subject to negative-feedback regulation by U-PA which cleaves it into an inactive form.
Gene Name:
PLAUR
Uniprot ID:
Q03405
Molecular Weight:
36977.62 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Serine-type endopeptidase inhibitor activity
Specific Function:
Serine protease inhibitor. This inhibitor acts as 'bait' for tissue plasminogen activator, urokinase, protein C and matriptase-3/TMPRSS7. Its rapid interaction with PLAT may function as a major control point in the regulation of fibrinolysis.
Gene Name:
SERPINE1
Uniprot ID:
P05121
Molecular Weight:
45059.695 Da
References
  1. Hilleman DE, Tsikouris JP, Seals AA, Marmur JD: Fibrinolytic agents for the management of ST-segment elevation myocardial infarction. Pharmacotherapy. 2007 Nov;27(11):1558-70. [PubMed:17963464 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23