Identification
- Summary
Reteplase is a purified form of human tissue plasminogen activator used in the emergency treatment of myocardial infarction, ischemic stroke, and pulmonary emboli.
- Brand Names
- Retavase
- Generic Name
- Reteplase
- DrugBank Accession Number
- DB00015
- Background
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).
- Type
- Biotech
- Groups
- Approved, Investigational
- Biologic Classification
- Protein Based Therapies
Thrombolytic agents - Protein Structure
- Protein Chemical Formula
- C1736H2671N499O522S22
- Protein Average Weight
- 39589.6 Da
- Sequences
>DB00015 sequence SYQGNSDCYFGNGSAYRGTHSLTESGASCLPWNSMILIGKVYTAQNPSAQALGLGKHNYC RNPDGDAKPWCHVLKNRRLTWEYCDVPSCSTCGLRQYSQPQFRIKGGLFADIASHPWQAA IFAKHRRSPGERFLCGGILISSCWILSAAHCFQERFPPHHLTVILGRTYRVVPGEEEQKF EVEKYIVHKEFDDDTYDNDIALLQLKSDSSRCAQESSVVRTVCLPPADLQLPDWTECELS GYGKHEALSPFYSERLKEAHVRLYPSSRCTSQHLLNRTVTDNMLCAGDTRSGGPQANLHD ACQGDSGGPLVCLNDGRMTLVGIISWGLGCGQKDVPGVYTKVTNYLDWIRDNMRP
Download FASTA Format- Synonyms
- Human t-PA (residues 1-3 and 176-527)
- Reteplasa
- Reteplase
- Reteplase, recombinant
- Reteplase,recombinant
- External IDs
- BM 06.022
- BM-06.022
- BM-06022
Pharmacology
- Indication
For lysis of acute pulmonary emboli, intracoronary emboli, and management of myocardial infarction.
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- Contraindications & Blackbox Warnings
Avoid life-threatening adverse drug eventsImprove clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support.- Pharmacodynamics
Reteplase 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
Reteplase 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.
Target Actions Organism APlasminogen activatorHumans AFibrinogen alpha chain Not Available Humans UPlasminogen activator inhibitor 1 Not Available Humans - 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
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
Not Available
- Pathways
Pathway Category Reteplase Action Pathway Drug action - Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbciximab The risk or severity of bleeding can be increased when Abciximab is combined with Reteplase. Aceclofenac The risk or severity of bleeding and hemorrhage can be increased when Aceclofenac is combined with Reteplase. Acemetacin The risk or severity of bleeding and hemorrhage can be increased when Reteplase is combined with Acemetacin. Acenocoumarol The risk or severity of bleeding can be increased when Reteplase is combined with Acenocoumarol. Acetylsalicylic acid Acetylsalicylic acid may increase the anticoagulant activities of Reteplase. Albutrepenonacog alfa The therapeutic efficacy of Albutrepenonacog alfa can be decreased when used in combination with Reteplase. Alclofenac The risk or severity of bleeding and hemorrhage can be increased when Alclofenac is combined with Reteplase. Aldesleukin The risk or severity of bleeding can be increased when Reteplase is combined with Aldesleukin. Alemtuzumab The risk or severity of bleeding can be increased when Reteplase is combined with Alemtuzumab. Alogliptin The risk or severity of angioedema can be increased when Reteplase is combined with Alogliptin. 
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- Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Rapilysin Injection, powder, for solution 10 U Intravenous Actavis Group Ptc Ehf. 2020-12-22 Not applicable EU 
Retavase Kit 1.81 mg/1mL Intravenous Ekr Therapeutics 1996-10-30 2017-07-01 US 
Retavase Powder, for solution 10.4 unit / vial Intravenous Ekr Therapeutics 1999-02-19 2013-08-29 Canada 
Retavase Kit 1.81 mg/1mL Intravenous Chiesi USA, Inc. 1996-10-30 Not applicable US Retavase Kit 1.81 mg/1mL Intravenous Ekr Therapeutics 1996-10-30 2017-07-01 US Retavase Kit 1.81 mg/1mL Intravenous Chiesi USA, Inc. 1996-10-30 Not applicable US
Categories
- ATC Codes
- B01AD07 — Reteplase
- Drug Categories
- Agents causing angioedema
- Amino Acids, Peptides, and Proteins
- Anticoagulants
- Biological Factors
- Blood and Blood Forming Organs
- Blood Proteins
- Cardiovascular Agents
- Endopeptidases
- Enzymes
- Enzymes and Coenzymes
- Fibrin Modulating Agents
- Fibrinolytic Agents
- Hematologic Agents
- Hydrolases
- Peptide Hydrolases
- Plasminogen Activators
- Proteins
- Serine Endopeptidases
- Serine Proteases
- Tissue Plasminogen Activator
- Chemical TaxonomyProvided by Classyfire
- 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
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- DQA630RIE9
- CAS number
- 133652-38-7
References
- General References
- Not Available
- External Links
- UniProt
- P00750
- Genbank
- L00153
- PubChem Substance
- 46506092
- 76895
- ChEMBL
- CHEMBL2107885
- Therapeutic Targets Database
- DAP001195
- PharmGKB
- PA164743728
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Reteplase
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Treatment Acute Myocardial Infarction (AMI) 1 4 Completed Treatment Acute Myocardial Infarction (AMI) / Cardiovascular Disease (CVD) / Myocardial Infarction 1 3 Not Yet Recruiting Treatment Restoration of Function to CVADs 1 3 Recruiting Treatment Acute Myocardial Infarction With ST Segment Elevation 1 3 Recruiting Treatment Catheter Occlusion / Thrombotic events 1 2 Completed Treatment Cerebrovascular Accident 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- EKR Therapeutics Inc.
- Hospira Inc.
- PDL BioPharma Inc.
- Dosage Forms
Form Route Strength Injection, powder, for solution Intravenous 10 U Injection, powder, lyophilized, for solution Intravenous Kit Intravenous 1.81 mg/1mL Powder, for solution Intravenous 10.4 unit / vial Injection, powder, lyophilized, for solution Intravenous 18 mg - Prices
Unit description Cost Unit Retavase vial half-kit 2605.93USD vial DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region CA2107476 No 2007-12-18 2012-04-15 Canada
Properties
- State
- Liquid
- Experimental Properties
Property Value Source melting point (°C) 60 °C Novokhatny, V.V. et al., J. Biol. Chem. 266:12994-123002 (1991) hydrophobicity -0.435 Not Available isoelectric point 6.86 Not Available
Targets
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- Kind
- Protein
- Organism
- Humans
- 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
- 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. [Article]
- 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. [Article]
- 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. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Kind
- Protein
- Organism
- Humans
- 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
- 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. [Article]
- 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. [Article]
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- 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
- 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. [Article]
Drug created at June 13, 2005 13:24 / Updated at October 03, 2021 00:33