Identification

Name
Anistreplase
Accession Number
DB00029  (BTD00102, BIOD00102)
Type
Biotech
Groups
Approved
Biologic Classification
Protein Based Therapies
Thrombolytic agents
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 structure
Db00029
Protein chemical formula
C2569H3928N746O781S40
Protein average weight
59042.3 Da
Sequences
>DB00029 sequence
SYQVICRDEKTQMIYQQHQSWLRPVLRSNRVEYCWCNSGRAQCHSVPVKSCSEPRCFNGG
TCQQALYFSDFVCQCPEGFAGKCCEIDTRATCYEDQGISYRGTWSTAESGAECTNWNSSA
LAQKPYSGRRPDAIRLGLGNHNYCRNPDRDSKPWCYVFKAGKYSSEFCSTPACSEGNSDC
YFGNGSAYRGTHSLTESGASCLPWNSMILIGKVYTAQNPSAQALGLGKHNYCRNPDGDAK
PWCHVLKNRRLTWEYCDVPSCSTCGLRQYSQPQFRIKGGLFADIASHPWQAAIFAKHRRS
PGERFLCGGILISSCWILSAAHCFQERFPPHHLTVILGRTYRVVPGEEEQKFEVEKYIVH
KEFDDDTYDNDIALLQLKSDSSRCAQESSVVRTVCLPPADLQLPDWTECELSGYGKHEAL
SPFYSERLKEAHVRLYPSSRCTSQHLLNRTVTDNMLCAGDTRSGGPQANLHDACQGDSGG
PLVCLNDGRMTLVGIISWGLGCGQKDVPGVYTKVTNYLDWIRDNMRP
Download FASTA Format
Synonyms
  • Anisoylated plasminogen streptokinase activator complex
  • APSAC
External IDs
BRL 26921 / BRL-26921
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Eminase 30 UnitsPowder, for solution30 unitIntravenousWell Spring Pharmaceutical Corporation1997-12-152009-02-23Canada
International/Other Brands
Eminase (Wulfing Pharma GmbH)
Categories
UNII
5O8V541HJ6
CAS number
81669-57-0

Pharmacology

Indication

For lysis of acute pulmonary emboli, intracoronary emboli and management of myocardial infarction

Structured Indications
Not Available
Pharmacodynamics

Anistreplase 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 action

Anistreplase cleaves the Arg/Val bond in plasminogen to form plasmin. This in turn leads to the degradation of blood clots.

TargetActionsOrganism
APlasminogen
activator
Human
AFibrinogen alpha chainNot AvailableHuman
UUrokinase plasminogen activator surface receptorNot AvailableHuman
UPlasminogen activator inhibitor 1Not AvailableHuman
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half life
Not Available
Clearance
Not Available
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Anistreplase Action PathwayDrug action
Pharmacogenomic Effects/ADRs
Not 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
AloxiprinThe risk or severity of adverse effects can be increased when Aloxiprin is combined with Anistreplase.Experimental
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
AndrographolideAndrographolide may increase the anticoagulant activities of Anistreplase.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
BuflomedilBuflomedil may increase the anticoagulant activities of Anistreplase.Experimental
ButylphthalideButylphthalide may increase the anticoagulant activities of Anistreplase.Investigational
CangrelorCangrelor may increase the anticoagulant activities of Anistreplase.Approved
Carbaspirin calciumThe risk or severity of adverse effects can be increased when Carbaspirin calcium is combined with Anistreplase.Experimental
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
CloricromenCloricromen may increase the anticoagulant activities of Anistreplase.Experimental
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
DarexabanAnistreplase may increase the anticoagulant activities of Darexaban.Investigational
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
EplivanserinEplivanserin may increase the anticoagulant activities of Anistreplase.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
Ferulic acidAnistreplase may increase the anticoagulant activities of Ferulic acid.Experimental
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
GuacetisalThe risk or severity of adverse effects can be increased when Guacetisal is combined with Anistreplase.Experimental
Hemoglobin crosfumarilThe risk or severity of adverse effects can be increased when Hemoglobin crosfumaril is combined with Anistreplase.Experimental
HeparinAnistreplase may increase the anticoagulant activities of Heparin.Approved, Investigational
HydroxytyrosolHydroxytyrosol may increase the anticoagulant activities of Anistreplase.Investigational
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
IfetrobanIfetroban may increase the anticoagulant activities of Anistreplase.Investigational
IloprostIloprost may increase the anticoagulant activities of Anistreplase.Approved, Investigational
IndobufenIndobufen may increase the anticoagulant activities of Anistreplase.Investigational
KetanserinKetanserin may increase the anticoagulant activities of Anistreplase.Investigational
LepirudinAnistreplase may increase the anticoagulant activities of Lepirudin.Approved
LetaxabanAnistreplase may increase the anticoagulant activities of Letaxaban.Investigational
LimaprostThe risk or severity of adverse effects can be increased when Limaprost is combined with Anistreplase.Approved
LinsidomineLinsidomine may increase the anticoagulant activities of Anistreplase.Experimental
MelagatranAnistreplase may increase the anticoagulant activities of Melagatran.Experimental
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.Approved, Investigational
NaftopidilNaftopidil may increase the anticoagulant activities of 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
PicotamidePicotamide may increase the anticoagulant activities of Anistreplase.Experimental
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
SarpogrelateSarpogrelate 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
TroxerutinAnistreplase may increase the anticoagulant activities of Troxerutin.Investigational
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
Food Interactions
Not Available

References

General References
Not Available
External Links
UniProt
P00750
Genbank
L00153
ChEMBL
CHEMBL2108250
Therapeutic Targets Database
DAP001197
PharmGKB
PA164769075
Wikipedia
Anistreplase
ATC Codes
B01AD03 — Anistreplase

Clinical Trials

Clinical Trials
Not Available

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Dosage forms
FormRouteStrength
Powder, for solutionIntravenous30 unit
Prices
Not Available
Patents
Not Available

Properties

State
Liquid
Experimental Properties
PropertyValueSource
melting point (°C)60 °CNovokhatny, V.V. et al., J. Biol. Chem. 266:12994-123002 (1991)
hydrophobicity-0.516Not Available
isoelectric point7.61Not Available

Taxonomy

Description
Not Available
Kingdom
Organic Compounds
Super Class
Organic Acids
Class
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Peptides
Alternative Parents
Not Available
Substituents
Not Available
Molecular Framework
Not Available
External Descriptors
Not Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
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...
Gene Name
PLG
Uniprot ID
P00747
Uniprot Name
Plasminogen
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 ...
Gene Name
FGA
Uniprot ID
P02671
Uniprot Name
Fibrinogen alpha chain
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-...
Gene Name
PLAUR
Uniprot ID
Q03405
Uniprot Name
Urokinase plasminogen activator surface receptor
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 con...
Gene Name
SERPINE1
Uniprot ID
P05121
Uniprot Name
Plasminogen activator inhibitor 1
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]

Drug created on June 13, 2005 07:24 / Updated on June 08, 2017 11:41