Reteplase

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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Drug Discovery

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Associated Conditions

Contraindications & Blackbox Warnings

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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	activator	Humans
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

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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
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Abciximab	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 Acemetacin is combined with Reteplase.
Acenocoumarol	The risk or severity of bleeding can be increased when Acenocoumarol is combined with Reteplase.
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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Food Interactions

Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.

Products

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Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Rapilysin	Injection, powder, for solution	10 U	Intravenous	Actavis Group Ptc Ehf.	2020-12-22	Not applicable
Retavase	Kit	1.81 mg/1mL	Intravenous	Ekr Therapeutics	1996-10-30	2017-07-01
Retavase	Kit	1.81 mg/1mL	Intravenous	Chiesi USA, Inc.	1996-10-30	Not applicable
Retavase	Kit	1.81 mg/1mL	Intravenous	Ekr Therapeutics	1996-10-30	2017-07-01
Retavase	Kit	1.81 mg/1mL	Intravenous	Chiesi USA, Inc.	1996-10-30	Not applicable
Retavase	Powder, for solution	10.4 unit / vial	Intravenous	Ekr Therapeutics	1999-02-19	2013-08-29

Chemical Identifiers

UNII: DQA630RIE9
CAS number: 133652-38-7

References

General References

Not Available

External Links

UniProt: P00750
Genbank: L00153
PubChem Substance: 46506092
RxNav: 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	Acute Myocardial Infarction With ST Segment Elevation	1
3	Not Yet Recruiting	Treatment	Restoration of Function to CVADs	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

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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Details1. Plasminogen

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]

Details2. Fibrinogen alpha chain

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]

Details3. Plasminogen activator inhibitor 1

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 on June 13, 2005 13:24 / Updated on July 03, 2021 08:55

Reteplase

Identification

Pharmacology

Interactions

Products

Categories

Chemical Identifiers

References

Clinical Trials

Pharmacoeconomics

Properties

Targets

References

References

References