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Identification
NameAnistreplase
Accession NumberDB00029  (BTD00102, BIOD00102)
TypeBiotech
GroupsApproved
Description

Human 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
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
Pharmacology
IndicationFor lysis of acute pulmonary emboli, intracoronary emboli and management of myocardial infarction
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.
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
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
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesB01AD03
AHFS Codes
  • 20:12.20
PDB Entries
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
AbciximabAbciximab may increase the anticoagulant activities of Anistreplase.
AcenocoumarolAnistreplase may increase the anticoagulant activities of Acenocoumarol.
Acetylsalicylic acidAcetylsalicylic acid may increase the anticoagulant activities of Anistreplase.
Aminosalicylic AcidThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Anistreplase.
AnagrelideAnagrelide may increase the anticoagulant activities of Anistreplase.
ApixabanAnistreplase may increase the anticoagulant activities of Apixaban.
AprotininThe therapeutic efficacy of Anistreplase can be decreased when used in combination with Aprotinin.
ArgatrobanAnistreplase may increase the anticoagulant activities of Argatroban.
Bismuth SubsalicylateThe risk or severity of adverse effects can be increased when Bismuth Subsalicylate is combined with Anistreplase.
BivalirudinAnistreplase may increase the anticoagulant activities of Bivalirudin.
CaffeineCaffeine may increase the anticoagulant activities of Anistreplase.
CangrelorCangrelor may increase the anticoagulant activities of Anistreplase.
CilostazolCilostazol may increase the anticoagulant activities of Anistreplase.
CitalopramCitalopram may increase the anticoagulant activities of Anistreplase.
ClopidogrelClopidogrel may increase the anticoagulant activities of Anistreplase.
Dabigatran etexilateAnistreplase may increase the anticoagulant activities of Dabigatran etexilate.
DalteparinAnistreplase may increase the anticoagulant activities of Dalteparin.
DanaparoidAnistreplase may increase the anticoagulant activities of Danaparoid.
DesirudinAnistreplase may increase the anticoagulant activities of Desirudin.
DesvenlafaxineDesvenlafaxine may increase the anticoagulant activities of Anistreplase.
DiclofenacDiclofenac may increase the anticoagulant activities of Anistreplase.
DiflunisalDiflunisal may increase the anticoagulant activities of Anistreplase.
DihydrocodeineDihydrocodeine may increase the anticoagulant activities of Anistreplase.
DipyridamoleDipyridamole may increase the anticoagulant activities of Anistreplase.
DuloxetineDuloxetine may increase the anticoagulant activities of Anistreplase.
EdoxabanAnistreplase may increase the anticoagulant activities of Edoxaban.
EnoxaparinAnistreplase may increase the anticoagulant activities of Enoxaparin.
EpoprostenolThe risk or severity of adverse effects can be increased when Anistreplase is combined with Epoprostenol.
EptifibatideEptifibatide may increase the anticoagulant activities of Anistreplase.
EscitalopramEscitalopram may increase the anticoagulant activities of Anistreplase.
EtodolacEtodolac may increase the anticoagulant activities of Anistreplase.
FenoprofenFenoprofen may increase the anticoagulant activities of Anistreplase.
FloctafenineFloctafenine may increase the anticoagulant activities of Anistreplase.
FluoxetineFluoxetine may increase the anticoagulant activities of Anistreplase.
FlurbiprofenFlurbiprofen may increase the anticoagulant activities of Anistreplase.
FluvoxamineFluvoxamine may increase the anticoagulant activities of Anistreplase.
Fondaparinux sodiumAnistreplase may increase the anticoagulant activities of Fondaparinux sodium.
HeparinAnistreplase may increase the anticoagulant activities of Heparin.
IbuprofenIbuprofen may increase the anticoagulant activities of Anistreplase.
IloprostThe risk or severity of adverse effects can be increased when Anistreplase is combined with Iloprost.
IndomethacinIndomethacin may increase the anticoagulant activities of Anistreplase.
KetoprofenKetoprofen may increase the anticoagulant activities of Anistreplase.
KetorolacKetorolac may increase the anticoagulant activities of Anistreplase.
LevomilnacipranLevomilnacipran may increase the anticoagulant activities of Anistreplase.
Magnesium salicylateThe risk or severity of adverse effects can be increased when Magnesium salicylate is combined with Anistreplase.
Mefenamic acidMefenamic acid may increase the anticoagulant activities of Anistreplase.
MeloxicamMeloxicam may increase the anticoagulant activities of Anistreplase.
MilnacipranMilnacipran may increase the anticoagulant activities of Anistreplase.
NabumetoneNabumetone may increase the anticoagulant activities of Anistreplase.
NadroparinAnistreplase may increase the anticoagulant activities of Nadroparin.
NaproxenNaproxen may increase the anticoagulant activities of Anistreplase.
OxaprozinOxaprozin may increase the anticoagulant activities of Anistreplase.
ParoxetineParoxetine may increase the anticoagulant activities of Anistreplase.
PiroxicamPiroxicam may increase the anticoagulant activities of Anistreplase.
PrasugrelPrasugrel may increase the anticoagulant activities of Anistreplase.
RivaroxabanAnistreplase may increase the anticoagulant activities of Rivaroxaban.
SalsalateThe risk or severity of adverse effects can be increased when Salsalate is combined with Anistreplase.
SertralineSertraline may increase the anticoagulant activities of Anistreplase.
SulindacSulindac may increase the anticoagulant activities of Anistreplase.
Tiaprofenic acidTiaprofenic acid may increase the anticoagulant activities of Anistreplase.
TicagrelorTicagrelor may increase the anticoagulant activities of Anistreplase.
TiclopidineTiclopidine may increase the anticoagulant activities of Anistreplase.
TinzaparinAnistreplase may increase the anticoagulant activities of Tinzaparin.
TirofibanTirofiban may increase the anticoagulant activities of Anistreplase.
TolmetinTolmetin may increase the anticoagulant activities of Anistreplase.
TreprostinilThe risk or severity of adverse effects can be increased when Anistreplase is combined with Treprostinil.
VenlafaxineVenlafaxine may increase the anticoagulant activities of Anistreplase.
VilazodoneVilazodone may increase the anticoagulant activities of Anistreplase.
VorapaxarVorapaxar may increase the anticoagulant activities of Anistreplase.
VortioxetineVortioxetine may increase the anticoagulant activities of Anistreplase.
WarfarinAnistreplase may increase the anticoagulant activities of Warfarin.
Food InteractionsNot 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 ]
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Drug created on June 13, 2005 07:24 / Updated on March 14, 2016 09:57