Alteplase

Identification

Summary

Alteplase is a recombinant form of human tissue plasminogen activator used in the emergency treatment of myocardial infarction, ischemic stroke, and pulmonary emboli.

Brand Names
Activase, Cathflo, Cathflo Activase
Generic Name
Alteplase
DrugBank Accession Number
DB00009
Background

Human tissue plasminogen activator, purified, glycosylated, 527 residues purified from CHO cells

Type
Biotech
Groups
Approved
Biologic Classification
Protein Based Therapies
Thrombolytic agents
Protein Structure
Db00009
Protein Chemical Formula
C2569H3928N746O781S40
Protein Average Weight
59042.3 Da
Sequences
>Alteplase sequence
SYQVICRDEKTQMIYQQHQSWLRPVLRSNRVEYCWCNSGRAQCHSVPVKSCSEPRCFNGG
TCQQALYFSDFVCQCPEGFAGKCCEIDTRATCYEDQGISYRGTWSTAESGAECTNWNSSA
LAQKPYSGRRPDAIRLGLGNHNYCRNPDRDSKPWCYVFKAGKYSSEFCSTPACSEGNSDC
YFGNGSAYRGTHSLTESGASCLPWNSMILIGKVYTAQNPSAQALGLGKHNYCRNPDGDAK
PWCHVLKNRRLTWEYCDVPSCSTCGLRQYSQPQFRIKGGLFADIASHPWQAAIFAKHRRS
PGERFLCGGILISSCWILSAAHCFQERFPPHHLTVILGRTYRVVPGEEEQKFEVEKYIVH
KEFDDDTYDNDIALLQLKSDSSRCAQESSVVRTVCLPPADLQLPDWTECELSGYGKHEAL
SPFYSERLKEAHVRLYPSSRCTSQHLLNRTVTDNMLCAGDTRSGGPQANLHDACQGDSGG
PLVCLNDGRMTLVGIISWGLGCGQKDVPGVYTKVTNYLDWIRDNMRP
Download FASTA Format
Synonyms
  • Alteplasa
  • Alteplase
  • Alteplase (genetical recombination)
  • Alteplase, recombinant
  • Alteplase,recombinant
  • Plasminogen activator (human tissue-type protein moiety)
  • rt-PA
  • t-PA
  • t-plasminogen activator
  • Tissue plasminogen activator
  • Tissue plasminogen activator alteplase
  • Tissue plasminogen activator, recombinant
  • tPA

Pharmacology

Indication

For management of acute myocardial infarction, acute ischemic strok and for lysis of acute pulmonary emboli

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
Contraindications & Blackbox Warnings
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Pharmacodynamics

Alteplase binds to fibrin in a thrombus and converts the entrapped plasminogen to plasmin. It also produces limited conversion of plasminogen in the absence of fibrin.

Mechanism of action

Alteplase 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.

TargetActionsOrganism
APlasminogen
activator
Humans
AFibrinogen alpha chainNot AvailableHumans
UUrokinase plasminogen activator surface receptorNot AvailableHumans
UPlasminogen activator inhibitor 1Not AvailableHumans
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
Medicalerrors
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Toxicity

Not Available

Pathways
PathwayCategory
Alteplase Action PathwayDrug 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.
DrugInteraction
AbciximabThe risk or severity of bleeding can be increased when Abciximab is combined with Alteplase.
AceclofenacThe risk or severity of bleeding and hemorrhage can be increased when Aceclofenac is combined with Alteplase.
AcemetacinThe risk or severity of bleeding and hemorrhage can be increased when Acemetacin is combined with Alteplase.
AcenocoumarolThe risk or severity of bleeding can be increased when Acenocoumarol is combined with Alteplase.
Acetylsalicylic acidAcetylsalicylic acid may increase the anticoagulant activities of Alteplase.
Albutrepenonacog alfaThe therapeutic efficacy of Albutrepenonacog alfa can be decreased when used in combination with Alteplase.
AlclofenacThe risk or severity of bleeding and hemorrhage can be increased when Alclofenac is combined with Alteplase.
AldesleukinThe risk or severity of bleeding can be increased when Alteplase is combined with Aldesleukin.
AlemtuzumabThe risk or severity of bleeding can be increased when Alteplase is combined with Alemtuzumab.
AlogliptinThe risk or severity of angioedema can be increased when Alteplase is combined with Alogliptin.
Interactions
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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

Products
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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
ActivaseKit100 mg/100mLIntravenousGenentech, Inc.1987-11-13Not applicableUS flag
ActivaseKit50 mg/50mLIntravenousGenentech, Inc.1987-11-13Not applicableUS flag
Activase RT-PA InjPowder, for solution50 mg/50mLIntravenousHoffmann La Roche1987-12-311998-07-31Canada flag
Activase RT-PA InjPowder, for solution50 mg/50mLIntravenousHoffmann La Roche1987-12-311998-07-31Canada flag
Activase RT-PA InjPowder, for solution50 mg/50mLIntravenousHoffmann La Roche1987-12-311998-07-31Canada flag
CathfloPowder, for solution2 mg / vialIntravenousHoffmann La Roche2002-09-26Not applicableCanada flag
Cathflo ActivaseInjection, powder, lyophilized, for solution2.2 mg/2mLIntravenousGenentech, Inc.2001-09-04Not applicableUS flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Activase RT-PAAlteplase (100 mg / kit) + Water (100 mL / kit)Liquid; Powder, for solutionIntravenousHoffmann La Roche1996-12-31Not applicableCanada flag
Activase RT-PAAlteplase (50 mg / kit) + Water (50 mL / kit)Liquid; Powder, for solutionIntravenousHoffmann La Roche1998-04-12Not applicableCanada flag
Lysatec RT - PaAlteplase (50 mg / kit) + Water (50 mL / kit)Powder, for solutionIntravenousGenentech, Inc.1993-12-311997-08-26Canada flag

Categories

ATC Codes
B01AD02 — AlteplaseS01XA13 — Alteplase
Drug Categories
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
1RXS4UE564
CAS number
105857-23-6

References

General References
Not Available
UniProt
P00750
Genbank
L00153
KEGG Drug
D02837
PubChem Substance
46507035
RxNav
8410
ChEMBL
CHEMBL1201593
Therapeutic Targets Database
DAP000203
PharmGKB
PA164776730
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Alteplase
AHFS Codes
  • 20:12.20 — Thrombolytic Agents
FDA label
Download (1.98 MB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentAcute ST-segment Elevation Myocardial Infarction1
4CompletedTreatmentDeep Vein Thrombosis / Post Thrombotic Syndrome / Post-Thrombotic Syndrome1
4CompletedTreatmentDysfunctional Central Venous Access Devices (CVADS)1
4CompletedTreatmentEmpyema / Parapneumonic Effusion / Pleural Diseases / Pleural space infections1
4CompletedTreatmentPleural Diseases1
4CompletedTreatmentPleural Diseases / Pleural Effusions / Pleural Empyema1
4CompletedTreatmentPulmonary Embolism1
4CompletedTreatmentPulmonary Embolism and Thrombosis1
4CompletedTreatmentPulmonary Embolism / Thromboembolism1
4CompletedTreatmentStroke1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Genentech Inc.
Dosage Forms
FormRouteStrength
Injection, powder, for solution
Injection, powder, for solutionIntravenous
SolutionIntravenous
Injection, powder, for solutionParenteral
Injection, powder, lyophilized, for solutionIntravenous
KitIntravenous100 mg/100mL
KitIntravenous50 mg/50mL
Liquid; powder, for solutionIntravenous
Powder, for solutionIntravenous50 mg/50mL
Powder, for solutionIntravenous2 mg / vial
Injection, powder, lyophilized, for solutionIntravenous2.2 mg/2mL
Powder, for solutionIntravenous
Powder50 mg/1vial
Prices
Unit descriptionCostUnit
Activase 100 mg vial4779.71USD vial
Activase 50 mg vial2389.85USD vial
Cathflo activase 2 mg vial106.33USD vial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Liquid
Experimental Properties
PropertyValueSource
melting point (°C)60 °CNovokhatny, V.V. et al., J. Biol. Chem. 266:12994-123002 (1991)
hydrophobicity-0.516Not Available
isoelectric point7.61Not Available

Targets

Drugtargets
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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
  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. [Article]
  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. [Article]
  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. [Article]
  4. 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
  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. [Article]
  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. [Article]
  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. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Curator comments
Evidence for this target action is limited in the literature.
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-...
Gene Name
PLAUR
Uniprot ID
Q03405
Uniprot Name
Urokinase plasminogen activator surface receptor
Molecular Weight
36977.62 Da
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
  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. [Article]

Drug created on June 13, 2005 13:24 / Updated on May 14, 2021 11:41