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Identification
NameReteplase
Accession NumberDB00015  (BTD00013, BIOD00013)
TypeBiotech
GroupsApproved
DescriptionHuman tissue plasminogen activator, purified, glycosylated, 355 residues purified from CHO cells. Retavase is considered a "third-generation" thrombolytic agent, genetically engineered to retain and delete certain portions of human tPA. Retavase is a deletion mutein of human tPA formed by deleting various amino acids present in endogenous human tPA. Retavase contains 355 of the 527 amino acids of native human tPA (amino acids 1-3 and 176-527), and retains the activity-related kringle-2 and serine protease domains of human tPA. Three domains are deleted from retavase - kringle-1, finger, and epidermal growth factor (EGF).
Protein structureDb00015
Related Articles
Protein chemical formulaC1736H2671N499O522S22
Protein average weight39589.6 Da
Sequences
>DB00015 sequence
SYQGNSDCYFGNGSAYRGTHSLTESGASCLPWNSMILIGKVYTAQNPSAQALGLGKHNYC
RNPDGDAKPWCHVLKNRRLTWEYCDVPSCSTCGLRQYSQPQFRIKGGLFADIASHPWQAA
IFAKHRRSPGERFLCGGILISSCWILSAAHCFQERFPPHHLTVILGRTYRVVPGEEEQKF
EVEKYIVHKEFDDDTYDNDIALLQLKSDSSRCAQESSVVRTVCLPPADLQLPDWTECELS
GYGKHEALSPFYSERLKEAHVRLYPSSRCTSQHLLNRTVTDNMLCAGDTRSGGPQANLHD
ACQGDSGGPLVCLNDGRMTLVGIISWGLGCGQKDVPGVYTKVTNYLDWIRDNMRP
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
RetavasekitEKR Therapeutics, Inc.1996-10-30Not applicableUs
RetavasekitEKR Therapeutics, Inc.1996-10-30Not applicableUs
Retavasepowder for solution10.4 unitintravenousEkr Therapeutics Inc1999-02-192013-08-29Canada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIDQA630RIE9
CAS number133652-38-7
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
PharmacodynamicsReteplase 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 actionReteplase binds to fibrin rich clots via the fibronectin finger-like domain and the Kringle 2 domain. The protease domain then 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.
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
Reteplase Action PathwayDrug actionSMP00285
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Kit
Powder for solutionintravenous10.4 unit
Prices
Unit descriptionCostUnit
Retavase vial half-kit2605.93USD vial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2107476 No2007-12-182012-04-15Canada
Properties
StateLiquid
Experimental Properties
PropertyValueSource
melting point60 °CNovokhatny, V.V. et al., J. Biol. Chem. 266:12994-123002 (1991)
hydrophobicity-0.435Not Available
isoelectric point6.86Not Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesB01AD07
AHFS CodesNot Available
PDB Entries
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
AbciximabReteplase may increase the anticoagulant activities of Abciximab.
AcenocoumarolReteplase may increase the anticoagulant activities of Acenocoumarol.
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Reteplase.
AlprostadilAlprostadil may increase the anticoagulant activities of Reteplase.
Aminosalicylic AcidThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Reteplase.
AnagrelideAnagrelide may increase the anticoagulant activities of Reteplase.
AncrodReteplase may increase the anticoagulant activities of Ancrod.
Antithrombin III humanReteplase may increase the anticoagulant activities of Antithrombin III human.
ApixabanReteplase may increase the anticoagulant activities of Apixaban.
AprotininThe therapeutic efficacy of Reteplase can be decreased when used in combination with Aprotinin.
ArdeparinReteplase may increase the anticoagulant activities of Ardeparin.
ArgatrobanReteplase may increase the anticoagulant activities of Argatroban.
AzelastineAzelastine may increase the anticoagulant activities of Reteplase.
BecaplerminReteplase may increase the anticoagulant activities of Becaplermin.
BeraprostBeraprost may increase the anticoagulant activities of Reteplase.
BivalirudinReteplase may increase the anticoagulant activities of Bivalirudin.
CangrelorCangrelor may increase the anticoagulant activities of Reteplase.
CertoparinReteplase may increase the anticoagulant activities of Certoparin.
CilostazolCilostazol may increase the anticoagulant activities of Reteplase.
Citric AcidReteplase may increase the anticoagulant activities of Citric Acid.
ClopidogrelClopidogrel may increase the anticoagulant activities of Reteplase.
Dabigatran etexilateReteplase may increase the anticoagulant activities of Dabigatran etexilate.
DalteparinReteplase may increase the anticoagulant activities of Dalteparin.
DanaparoidReteplase may increase the anticoagulant activities of Danaparoid.
DefibrotideDefibrotide may increase the anticoagulant activities of Reteplase.
DesirudinReteplase may increase the anticoagulant activities of Desirudin.
DextranReteplase may increase the anticoagulant activities of Dextran.
Dextran 40Reteplase may increase the anticoagulant activities of Dextran 40.
Dextran 70Reteplase may increase the anticoagulant activities of Dextran 70.
Dextran 75Reteplase may increase the anticoagulant activities of Dextran 75.
DicoumarolReteplase may increase the anticoagulant activities of Dicoumarol.
DiflunisalThe risk or severity of adverse effects can be increased when Diflunisal is combined with Reteplase.
DipyridamoleDipyridamole may increase the anticoagulant activities of Reteplase.
Edetic AcidReteplase may increase the anticoagulant activities of Edetic Acid.
EdoxabanReteplase may increase the anticoagulant activities of Edoxaban.
EnoxaparinReteplase may increase the anticoagulant activities of Enoxaparin.
EpinastineEpinastine may increase the anticoagulant activities of Reteplase.
EpoprostenolEpoprostenol may increase the anticoagulant activities of Reteplase.
EpoprostenolThe risk or severity of adverse effects can be increased when Reteplase is combined with Epoprostenol.
EptifibatideEptifibatide may increase the anticoagulant activities of Reteplase.
Ethyl biscoumacetateReteplase may increase the anticoagulant activities of Ethyl biscoumacetate.
Fondaparinux sodiumReteplase may increase the anticoagulant activities of Fondaparinux sodium.
HeparinReteplase may increase the anticoagulant activities of Heparin.
HirulogReteplase may increase the anticoagulant activities of Hirulog.
IbudilastIbudilast may increase the anticoagulant activities of Reteplase.
Icosapent ethylIcosapent ethyl may increase the anticoagulant activities of Reteplase.
IfenprodilIfenprodil may increase the anticoagulant activities of Reteplase.
IloprostIloprost may increase the anticoagulant activities of Reteplase.
IloprostThe risk or severity of adverse effects can be increased when Reteplase is combined with Iloprost.
LepirudinReteplase may increase the anticoagulant activities of Lepirudin.
LimaprostThe risk or severity of adverse effects can be increased when Limaprost is combined with Reteplase.
MesalazineThe risk or severity of adverse effects can be increased when Mesalazine is combined with Reteplase.
MilrinoneMilrinone may increase the anticoagulant activities of Reteplase.
NadroparinReteplase may increase the anticoagulant activities of Nadroparin.
NCX 4016NCX 4016 may increase the anticoagulant activities of Reteplase.
NimesulideNimesulide may increase the anticoagulant activities of Reteplase.
OtamixabanReteplase may increase the anticoagulant activities of Otamixaban.
Pentosan PolysulfateReteplase may increase the anticoagulant activities of Pentosan Polysulfate.
PentoxifyllinePentoxifylline may increase the anticoagulant activities of Reteplase.
PhenindioneReteplase may increase the anticoagulant activities of Phenindione.
PhenprocoumonReteplase may increase the anticoagulant activities of Phenprocoumon.
PrasugrelPrasugrel may increase the anticoagulant activities of Reteplase.
Protein CReteplase may increase the anticoagulant activities of Protein C.
ProtocatechualdehydeReteplase may increase the anticoagulant activities of Protocatechualdehyde.
ResveratrolResveratrol may increase the anticoagulant activities of Reteplase.
ReviparinReteplase may increase the anticoagulant activities of Reviparin.
RidogrelRidogrel may increase the anticoagulant activities of Reteplase.
RivaroxabanReteplase may increase the anticoagulant activities of Rivaroxaban.
Salicylic acidThe risk or severity of adverse effects can be increased when Salicylic acid is combined with Reteplase.
SCH-530348SCH-530348 may increase the anticoagulant activities of Reteplase.
SevofluraneSevoflurane may increase the anticoagulant activities of Reteplase.
SRT501SRT501 may increase the anticoagulant activities of Reteplase.
SulodexideReteplase may increase the anticoagulant activities of Sulodexide.
TesmilifeneTesmilifene may increase the anticoagulant activities of Reteplase.
TiclopidineTiclopidine may increase the anticoagulant activities of Reteplase.
TirofibanTirofiban may increase the anticoagulant activities of Reteplase.
TranilastTranilast may increase the anticoagulant activities of Reteplase.
TrapidilTrapidil may increase the anticoagulant activities of Reteplase.
TreprostinilThe risk or severity of adverse effects can be increased when Reteplase is combined with Treprostinil.
TriflusalTriflusal may increase the anticoagulant activities of Reteplase.
VorapaxarVorapaxar may increase the anticoagulant activities of Reteplase.
WarfarinReteplase may increase the anticoagulant activities of Warfarin.
XimelagatranReteplase may increase the anticoagulant activities of Ximelagatran.
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. 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 ]
  2. 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 ]
  3. 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 ]
  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. 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 ]
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 August 17, 2016 12:23