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Identification
NameReteplase
Accession NumberDB00015  (BIOD00013, BTD00013)
TypeBiotech
GroupsApproved
Description

Human 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
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
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
RetavasekitEKR Therapeutics, Inc.1996-10-30Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Retavasepowder for solution10.4 unitintravenousEkr Therapeutics Inc1999-02-192013-08-29Canada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
RetavasekitEKR Therapeutics, Inc.1996-10-30Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Generic Prescription ProductsNot Available
Over the Counter ProductsNot 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.
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
PathwaysNot Available
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
CountryPatent NumberApprovedExpires (estimated)
Canada21074762007-12-182012-04-15
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.
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.
ApixabanReteplase may increase the anticoagulant activities of Apixaban.
AprotininThe therapeutic efficacy of Reteplase can be decreased when used in combination with Aprotinin.
ArgatrobanReteplase may increase the anticoagulant activities of Argatroban.
Bismuth SubsalicylateThe risk or severity of adverse effects can be increased when Bismuth Subsalicylate is combined with Reteplase.
BivalirudinReteplase may increase the anticoagulant activities of Bivalirudin.
CaffeineCaffeine may increase the anticoagulant activities of Reteplase.
CangrelorCangrelor may increase the anticoagulant activities of Reteplase.
CilostazolCilostazol may increase the anticoagulant activities of Reteplase.
CitalopramCitalopram 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.
DesirudinReteplase may increase the anticoagulant activities of Desirudin.
DesvenlafaxineDesvenlafaxine may increase the anticoagulant activities of Reteplase.
DiclofenacDiclofenac may increase the anticoagulant activities of Reteplase.
DicoumarolReteplase may increase the anticoagulant activities of Dicoumarol.
DiflunisalDiflunisal may increase the anticoagulant activities of Reteplase.
DihydrocodeineDihydrocodeine may increase the anticoagulant activities of Reteplase.
DipyridamoleDipyridamole may increase the anticoagulant activities of Reteplase.
DuloxetineDuloxetine 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.
EpoprostenolThe risk or severity of adverse effects can be increased when Reteplase is combined with Epoprostenol.
EptifibatideEptifibatide may increase the anticoagulant activities of Reteplase.
EscitalopramEscitalopram may increase the anticoagulant activities of Reteplase.
Ethyl biscoumacetateReteplase may increase the anticoagulant activities of Ethyl biscoumacetate.
EtodolacEtodolac may increase the anticoagulant activities of Reteplase.
FenoprofenFenoprofen may increase the anticoagulant activities of Reteplase.
FloctafenineFloctafenine may increase the anticoagulant activities of Reteplase.
FluoxetineFluoxetine may increase the anticoagulant activities of Reteplase.
FlurbiprofenFlurbiprofen may increase the anticoagulant activities of Reteplase.
FluvoxamineFluvoxamine may increase the anticoagulant activities of Reteplase.
Fondaparinux sodiumReteplase may increase the anticoagulant activities of Fondaparinux sodium.
HeparinReteplase may increase the anticoagulant activities of Heparin.
IbuprofenIbuprofen may increase the anticoagulant activities of Reteplase.
IloprostThe risk or severity of adverse effects can be increased when Reteplase is combined with Iloprost.
IndomethacinIndomethacin may increase the anticoagulant activities of Reteplase.
KetoprofenKetoprofen may increase the anticoagulant activities of Reteplase.
KetorolacKetorolac may increase the anticoagulant activities of Reteplase.
LevomilnacipranLevomilnacipran may increase the anticoagulant activities of Reteplase.
LimaprostThe risk or severity of adverse effects can be increased when Limaprost is combined with Reteplase.
Magnesium salicylateThe risk or severity of adverse effects can be increased when Magnesium salicylate is combined with Reteplase.
Mefenamic acidMefenamic acid may increase the anticoagulant activities of Reteplase.
MeloxicamMeloxicam may increase the anticoagulant activities of Reteplase.
MilnacipranMilnacipran may increase the anticoagulant activities of Reteplase.
NabumetoneNabumetone may increase the anticoagulant activities of Reteplase.
NadroparinReteplase may increase the anticoagulant activities of Nadroparin.
NaproxenNaproxen may increase the anticoagulant activities of Reteplase.
OxaprozinOxaprozin may increase the anticoagulant activities of Reteplase.
ParoxetineParoxetine may increase the anticoagulant activities of Reteplase.
PhenindioneReteplase may increase the anticoagulant activities of Phenindione.
PhenprocoumonReteplase may increase the anticoagulant activities of Phenprocoumon.
PiroxicamPiroxicam may increase the anticoagulant activities of Reteplase.
PrasugrelPrasugrel may increase the anticoagulant activities of Reteplase.
RivaroxabanReteplase may increase the anticoagulant activities of Rivaroxaban.
Salicylate-sodiumThe risk or severity of adverse effects can be increased when Salicylate-sodium is combined with Reteplase.
SalsalateThe risk or severity of adverse effects can be increased when Salsalate is combined with Reteplase.
SertralineSertraline may increase the anticoagulant activities of Reteplase.
SulindacSulindac may increase the anticoagulant activities of Reteplase.
SulodexideReteplase may increase the anticoagulant activities of Sulodexide.
Tiaprofenic acidTiaprofenic acid may increase the anticoagulant activities of Reteplase.
TicagrelorTicagrelor may increase the anticoagulant activities of Reteplase.
TiclopidineTiclopidine may increase the anticoagulant activities of Reteplase.
TinzaparinReteplase may increase the anticoagulant activities of Tinzaparin.
TirofibanTirofiban may increase the anticoagulant activities of Reteplase.
TolmetinTolmetin may increase the anticoagulant activities of Reteplase.
TreprostinilReteplase may increase the anticoagulant activities of Treprostinil.
VenlafaxineVenlafaxine may increase the anticoagulant activities of Reteplase.
VilazodoneVilazodone may increase the anticoagulant activities of Reteplase.
VorapaxarVorapaxar may increase the anticoagulant activities of Reteplase.
VortioxetineVortioxetine may increase the anticoagulant activities of Reteplase.
WarfarinReteplase may increase the anticoagulant activities of Warfarin.
Food InteractionsNot Available

Targets

1. Plasminogen

Kind: Protein

Organism: Human

Pharmacological action: yes

Actions: activator

Components

Name UniProt ID Details
Plasminogen P00747 Details

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
  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
  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
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed

2. Fibrinogen alpha chain

Kind: Protein

Organism: Human

Pharmacological action: yes

Components

Name UniProt ID Details
Fibrinogen alpha chain P02671 Details

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
  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
  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

3. Urokinase plasminogen activator surface receptor

Kind: Protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Urokinase plasminogen activator surface receptor Q03405 Details

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
  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

4. Plasminogen activator inhibitor 1

Kind: Protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Plasminogen activator inhibitor 1 P05121 Details

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

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Drug created on June 13, 2005 07:24 / Updated on September 29, 2010 14:34