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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 weight39589.6000
Sequences
>DB00015 sequence
SYQGNSDCYFGNGSAYRGTHSLTESGASCLPWNSMILIGKVYTAQNPSAQALGLGKHNYC
RNPDGDAKPWCHVLKNRRLTWEYCDVPSCSTCGLRQYSQPQFRIKGGLFADIASHPWQAA
IFAKHRRSPGERFLCGGILISSCWILSAAHCFQERFPPHHLTVILGRTYRVVPGEEEQKF
EVEKYIVHKEFDDDTYDNDIALLQLKSDSSRCAQESSVVRTVCLPPADLQLPDWTECELS
GYGKHEALSPFYSERLKEAHVRLYPSSRCTSQHLLNRTVTDNMLCAGDTRSGGPQANLHD
ACQGDSGGPLVCLNDGRMTLVGIISWGLGCGQKDVPGVYTKVTNYLDWIRDNMRP
Download FASTA Format
Synonyms
SynonymLanguageCode
t- PANot AvailableNot Available
t-plasminogen activatorNot AvailableNot Available
Tissue-type plasminogen activator precursorNot AvailableNot Available
tPANot AvailableNot Available
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
RetavasekitEKR Therapeutics, Inc.1996-10-30Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
RetavasekitEKR Therapeutics, Inc.1996-10-30Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Generic Prescription ProductsNot Available
Over the Counter ProductsNot Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
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
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 ReferenceNot Available
External Links
ATC CodesB01AD07
AHFS CodesNot Available
PDB Entries
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
AbciximabThrombolytic Agents may enhance the anticoagulant effect of Anticoagulants.
AcenocoumarolThrombolytic Agents may enhance the anticoagulant effect of Anticoagulants.
Acetylsalicylic acidMay enhance the adverse/toxic effect of Thrombolytic Agents. An increased risk of bleeding may occur.
Aminosalicylic AcidSalicylates may enhance the adverse/toxic effect of Thrombolytic Agents. An increased risk of bleeding may occur.
AnagrelideAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
ApixabanMay enhance the anticoagulant effect of Anticoagulants.
AprotininMay diminish the therapeutic effect of Thrombolytic Agents.
ArgatrobanMay enhance the anticoagulant effect of Anticoagulants.
Bismuth SubsalicylateSalicylates may enhance the adverse/toxic effect of Thrombolytic Agents. An increased risk of bleeding may occur.
BivalirudinMay enhance the anticoagulant effect of Anticoagulants.
CilostazolAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
CitalopramAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
Citric AcidThrombolytic Agents may enhance the anticoagulant effect of Anticoagulants.
ClopidogrelAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
Dabigatran etexilateThrombolytic Agents may enhance the anticoagulant effect of Dabigatran Etexilate.
DalteparinThrombolytic Agents may enhance the anticoagulant effect of Anticoagulants.
DanaparoidMay enhance the anticoagulant effect of Anticoagulants.
DesvenlafaxineAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
DicoumarolThrombolytic Agents may enhance the anticoagulant effect of Anticoagulants.
DiflunisalAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
DipyridamoleAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
DuloxetineAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
Edetic AcidThrombolytic Agents may enhance the anticoagulant effect of Anticoagulants.
EnoxaparinThrombolytic Agents may enhance the anticoagulant effect of Anticoagulants.
EpoprostenolMay enhance the adverse/toxic effect of Prostacyclin Analogues. Specifically, the antiplatelet effects of prostacyclin analogues may lead to an increased risk of bleeding when combined with thrombolytic agents.
EptifibatideAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
EscitalopramAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
Ethyl biscoumacetateThrombolytic Agents may enhance the anticoagulant effect of Anticoagulants.
EtodolacAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
FenoprofenAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
FloctafenineAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
FluoxetineAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
FluvoxamineAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
Fondaparinux sodiumThrombolytic Agents may enhance the anticoagulant effect of Anticoagulants.
HeparinThrombolytic Agents may enhance the anticoagulant effect of Anticoagulants.
IbuprofenAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
IloprostMay enhance the adverse/toxic effect of Prostacyclin Analogues. Specifically, the antiplatelet effects of prostacyclin analogues may lead to an increased risk of bleeding when combined with thrombolytic agents.
IndomethacinAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
KetoprofenAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
KetorolacAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
LevomilnacipranAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
Magnesium salicylateSalicylates may enhance the adverse/toxic effect of Thrombolytic Agents. An increased risk of bleeding may occur.
Mefenamic acidAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
MeloxicamAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
MilnacipranAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
NabumetoneAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
NadroparinMay enhance the anticoagulant effect of Anticoagulants.
NaproxenAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
OxaprozinAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
ParoxetineAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
PhenindioneThrombolytic Agents may enhance the anticoagulant effect of Anticoagulants.
PhenprocoumonThrombolytic Agents may enhance the anticoagulant effect of Anticoagulants.
PiroxicamAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
PrasugrelAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
RivaroxabanMay enhance the anticoagulant effect of Anticoagulants.
Salicylate-sodiumMay enhance the adverse/toxic effect of Thrombolytic Agents. An increased risk of bleeding may occur.
SalsalateSalicylates may enhance the adverse/toxic effect of Thrombolytic Agents. An increased risk of bleeding may occur.
SertralineAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
SulindacAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
SulodexideThrombolytic Agents may enhance the anticoagulant effect of Anticoagulants.
Tiaprofenic acidAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
TicagrelorAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
TiclopidineAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
TinzaparinMay enhance the anticoagulant effect of Anticoagulants.
TirofibanAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
TolmetinAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
TreprostinilThrombolytic Agents may enhance the anticoagulant effect of Anticoagulants.
VenlafaxineAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
VilazodoneAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
VorapaxarAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
WarfarinThrombolytic Agents may enhance the anticoagulant effect of Anticoagulants.
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