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
- 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 stroke and for lysis of acute pulmonary emboli.
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- Contraindications & Blackbox Warnings
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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.
Target Actions Organism APlasminogen activatorHumans AFibrinogen alpha chain Not Available Humans UUrokinase plasminogen activator surface receptor 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 Alteplase 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 Alteplase. Aceclofenac The risk or severity of bleeding and hemorrhage can be increased when Aceclofenac is combined with Alteplase. Acemetacin The risk or severity of bleeding and hemorrhage can be increased when Alteplase is combined with Acemetacin. Acenocoumarol The risk or severity of bleeding can be increased when Alteplase is combined with Acenocoumarol. Acetylsalicylic acid Acetylsalicylic acid may increase the anticoagulant activities of Alteplase. Albutrepenonacog alfa The therapeutic efficacy of Albutrepenonacog alfa can be decreased when used in combination with Alteplase. Alclofenac The risk or severity of bleeding and hemorrhage can be increased when Alclofenac is combined with Alteplase. Aldesleukin The risk or severity of bleeding can be increased when Alteplase is combined with Aldesleukin. Alemtuzumab The risk or severity of bleeding can be increased when Alteplase is combined with Alemtuzumab. Alogliptin The risk or severity of angioedema can be increased when Alteplase is combined with Alogliptin. 
Identify potential medication risksEasily compare up to 40 drugs with our drug interaction checker.Get severity rating, description, and management advice.Learn more - Food Interactions
- 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 Activase Kit 100 mg/100mL Intravenous Genentech, Inc. 1987-11-13 Not applicable US 
Activase Kit 50 mg/50mL Intravenous Genentech, Inc. 1987-11-13 Not applicable US Activase RT-PA Inj Powder, for solution 50 mg/50mL Intravenous Hoffmann La Roche 1987-12-31 1998-07-31 Canada 
Activase RT-PA Inj Powder, for solution 50 mg/50mL Intravenous Hoffmann La Roche 1987-12-31 1998-07-31 Canada Activase RT-PA Inj Powder, for solution 50 mg/50mL Intravenous Hoffmann La Roche 1987-12-31 1998-07-31 Canada Cathflo Powder, for solution 2 mg / vial Intravenous Hoffmann La Roche 2002-09-26 Not applicable Canada Cathflo Activase Injection, powder, lyophilized, for solution 2.2 mg/2mL Intravenous Genentech, Inc. 2001-09-04 Not applicable US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Activase RT-PA Alteplase (50 mg / kit) + Water (50 mL / kit) Liquid; Powder, for solution Intravenous Hoffmann La Roche 1998-04-12 Not applicable Canada Activase RT-PA Alteplase (100 mg / kit) + Water (100 mL / kit) Liquid; Powder, for solution Intravenous Hoffmann La Roche 1996-12-31 Not applicable Canada Lysatec RT - Pa Alteplase (50 mg / kit) + Water (50 mL / kit) Powder, for solution Intravenous Genentech, Inc. 1993-12-31 1997-08-26 Canada
Categories
- ATC Codes
- B01AD02 — Alteplase
- B01AD — Enzymes
- B01A — ANTITHROMBOTIC AGENTS
- B01 — ANTITHROMBOTIC AGENTS
- B — BLOOD AND BLOOD FORMING ORGANS
- Drug Categories
- Agents causing angioedema
- Amino Acids, Peptides, and Proteins
- Anticoagulants
- Blood and Blood Forming Organs
- Blood Proteins
- Cardiovascular Agents
- Endopeptidases
- Enzymes
- Enzymes and Coenzymes
- Fibrin Modulating Agents
- Fibrinolytic Agents
- Hematologic Agents
- Hydrolases
- Ophthalmologicals
- Peptide Hydrolases
- Plasminogen Activators
- Proteins
- Sensory Organs
- Serine Endopeptidases
- Serine Proteases
- Tissue Plasminogen Activator
- Tissue Plasminogen Activator, antagonists & inhibitors
- 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
- External Links
- UniProt
- P00750
- Genbank
- L00153
- KEGG Drug
- D02837
- PubChem Substance
- 46507035
- 8410
- ChEMBL
- CHEMBL1201593
- Therapeutic Targets Database
- DAP000203
- PharmGKB
- PA164776730
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Alteplase
- FDA label
- Download (1.98 MB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Treatment Acute Myocardial Infarction With ST Segment Elevation 1 4 Completed Treatment Cerebrovascular Accident 1 4 Completed Treatment Deep Vein Thrombosis / Post Thrombotic Syndrome 1 4 Completed Treatment Dysfunctional Central Venous Access Devices (CVADS) 1 4 Completed Treatment Empyema / Parapneumonic Effusion / Pleural Diseases / Pleural space infections 1 4 Completed Treatment Large-Artery Atherosclerosis (Embolus/Thrombosis) / Stroke, Ischemic / Thrombectomy 1 4 Completed Treatment Pleural Diseases 1 4 Completed Treatment Pleural Diseases / Pleural Effusions / Pleural Empyema 1 4 Completed Treatment Pulmonary Embolism 1 4 Completed Treatment Pulmonary Embolism and Thrombosis 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Genentech Inc.
- Dosage Forms
Form Route Strength Injection, powder, for solution Injection, powder, for solution Intravenous 2 MG Injection, powder, for solution Intravenous 20 MG/20ML Injection, powder, for solution Intravenous 50 MG/50ML Solution Intravenous 20 MG Solution Intravenous 50 MG Injection, powder, for solution Parenteral Injection, powder, lyophilized, for solution Intravenous Injection, powder, for solution Intravenous 50 mg Solution Intravenous Kit Intravenous 100 mg/100mL Kit Intravenous 50 mg/50mL Liquid; powder, for solution Intravenous Powder, for solution Intravenous 50 mg/50mL Powder, for solution Intravenous 2 mg / vial Injection, powder, lyophilized, for solution Intravenous 2.2 mg/2mL Powder, for solution Intravenous Powder 50 mg/1vial - Prices
Unit description Cost Unit Activase 100 mg vial 4779.71USD vial Activase 50 mg vial 2389.85USD vial Cathflo activase 2 mg vial 106.33USD vial DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Liquid
- Experimental Properties
Property Value Source melting point (°C) 60 °C Novokhatny, V.V. et al., J. Biol. Chem. 266:12994-123002 (1991) hydrophobicity -0.516 Not Available isoelectric point 7.61 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
- 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]
- 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
- 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
- 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 January 16, 2022 18:54