Identification
- Summary
Abciximab is a monoclonal anti-glycoprotein IIb/IIIa receptor antibody used to prevent thrombosis during percutaneous coronary intervention.
- Generic Name
- Abciximab
- DrugBank Accession Number
- DB00054
- Background
Abciximab is a Fab fragment of the chimeric human-murine monoclonal antibody 7E3. Abciximab binds to the glycoprotein (GP) IIb/IIIa receptor of human platelets and inhibits platelet aggregation by preventing the binding of fibrinogen, von Willebrand factor, and other adhesive molecules. It also binds to vitronectin (αvβ3) receptor found on platelets and vessel wall endothelial and smooth muscle cells.
- Type
- Biotech
- Groups
- Approved
- Biologic Classification
- Protein Based Therapies
Monoclonal antibody (mAb) - Protein Structure
- Protein Chemical Formula
- C6462H9964N1690O2049S48
- Protein Average Weight
- 145651.1 Da
- Sequences
>pdb|6V4P|C Chain C, Abciximab, heavy chain EVQLQQSGTVLARPGASVKMSCEASGYTFTNYWMHWVKQRPGQGLEWIGAIYPGNSDTSY IQKFKGKAKLTAVTSTTSVYMELSSLTNEDSAVYYCTLYDGYYVFAYWGQGTLVTVSAAS TKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGL YSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSCDKTH
Download FASTA FormatReferences:
- BLAST, NIH [Link]
- Synonyms
- Abciximab
- Abciximab (genetical recombination)
- c7E3
Pharmacology
- Indication
Abciximab is indicated as an adjunct to percutaneous coronary intervention for the prevention of cardiac ischemic complications in patients undergoing percutaneous coronary intervention and in patients with unstable angina not responding to conventional medical therapy when percutaneous coronary intervention is planned within 24 hours. Abciximab is intended for use with aspirin and heparin and has been studied only in that setting.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Adjunct therapy in prevention of Ischemic cardiovascular events •••••••••••• •••••• •••••••••••• •••••••• •••••••• •••••• •••••••• ••••••••• Adjunct therapy in prevention of Ischemic cardiovascular events •••••••••••• ••••••••• - Contraindications & Blackbox Warnings
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Abciximab inhibits platelet aggregation by preventing the binding of fibrinogen, von Willebrand factor, and other adhesive molecules to GPIIb/IIIa receptor sites on activated platelets. A single intravenous bolus dose from 0.15 mg/kg to 0.30 mg/kg produced rapid dose-dependent inhibition of platelet function. After two hours post-injection with a dose of 0.25 - 0.30 mg/kg, 80% of the GPIIb/IIIa receptors were blocked and platelet aggregation was prevented. GPIIb/IIIa is the major surface receptor involved in the final pathway of platelet aggregation. Bleeding time increases to over 30 minutes at the aforementioned doses. To compare, baseline values were five minutes.
- Mechanism of action
Abciximab binds to the intact platelet GPIIb/IIIa receptor, which is a member of the integrin family of adhesion receptors and the major platelet surface receptor involved in platelet aggregation. This binding is thought to involve steric hindrance and/or conformational alterations which block access of large molecules to the receptor rather than direct interaction with the RGD (arginine-glycine-aspartic acid) binding site of GPIIb/IIIa. By binding to the vitronectin receptor (also known as the αvβ3 integrin), abciximab blocks effects mediated by this integrin which include cell adhesion. Furthermore, abciximab blocks Mac-1 receptor on monocytes and neutrophils thus inhibiting monocyte adhesion.
Target Actions Organism AIntegrin beta-3 antagonistHumans AIntegrin alpha-IIb antagonistHumans ULow affinity immunoglobulin gamma Fc region receptor II-a Not Available Humans ULow affinity immunoglobulin gamma Fc region receptor II-b Not Available Humans UVitronectin Not Available Humans - Absorption
Not Available
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
Most likely removed by opsonization via the reticuloendothelial system when bound to platelets, or by human antimurine antibody production. Excreted renally.
- Route of elimination
Not Available
- Half-life
Following intravenous bolus administration, free plasma concentrations of Abciximab decrease rapidly with an initial half-life of less than 10 minutes and a second phase half-life of about 30 minutes, probably related to rapid binding to the platelet GPIIb/IIIa receptors.
- Clearance
Not Available
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
Not Available
- Pathways
Pathway Category Abciximab 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 softwareAbrocitinib The risk or severity of bleeding and thrombocytopenia can be increased when Abciximab is combined with Abrocitinib. Aceclofenac The risk or severity of bleeding and hemorrhage can be increased when Aceclofenac is combined with Abciximab. Acemetacin The risk or severity of bleeding and hemorrhage can be increased when Abciximab is combined with Acemetacin. Acenocoumarol The risk or severity of bleeding can be increased when Abciximab is combined with Acenocoumarol. Acetylsalicylic acid Acetylsalicylic acid may increase the antiplatelet activities of Abciximab. - Food Interactions
- Avoid herbs and supplements with anticoagulant/antiplatelet activity. Additive antiplatelet activity may increase the risk of bleeding. Examples include ginseng, ginkgo, ginger, and garlic.
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 Reopro Injection, solution 2 mg/1mL Intravenous Eli Lilly and Company 1993-12-16 2019-01-31 US 
Reopro Solution 2 mg / mL Intravenous Janssen Pharmaceuticals 1996-10-30 2018-06-14 Canada 
Reopro Injection, solution 2 mg/1mL Intravenous Janssen Biotech, Inc. 2017-01-03 2019-09-30 US
Categories
- ATC Codes
- B01AC13 — Abciximab
- Drug Categories
- Amino Acids, Peptides, and Proteins
- Antibodies
- Antibodies, Monoclonal
- Antibodies, Monoclonal, Humanized
- Anticoagulants
- Antiplatelet agents
- Blood and Blood Forming Organs
- Blood Proteins
- Globulins
- Glycoprotein IIb/IIIa Receptor-directed Monoclonal Antibodies
- Hematologic Agents
- Immunoglobulin Fab Fragments
- Immunoglobulin Fragments
- Immunoglobulins
- Immunoproteins
- Miscellaneous Therapeutic Agents
- Peptide Fragments
- Peptides
- Platelet Aggregation Inhibitors Excl. Heparin
- Proteins
- Serum Globulins
- 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
- X85G7936GV
- CAS number
- 143653-53-6
References
- General References
- Authors unspecified: Use of a monoclonal antibody directed against the platelet glycoprotein IIb/IIIa receptor in high-risk coronary angioplasty. The EPIC Investigation. N Engl J Med. 1994 Apr 7;330(14):956-61. [Article]
- Tcheng JE, Kandzari DE, Grines CL, Cox DA, Effron MB, Garcia E, Griffin JJ, Guagliumi G, Stuckey T, Turco M, Fahy M, Lansky AJ, Mehran R, Stone GW: Benefits and risks of abciximab use in primary angioplasty for acute myocardial infarction: the Controlled Abciximab and Device Investigation to Lower Late Angioplasty Complications (CADILLAC) trial. Circulation. 2003 Sep 16;108(11):1316-23. Epub 2003 Aug 25. [Article]
- External Links
- KEGG Drug
- D02778
- PubChem Substance
- 46505910
- 83929
- ChEMBL
- CHEMBL1201584
- Therapeutic Targets Database
- DAP000473
- PharmGKB
- PA448006
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Abciximab
- FDA label
- Download (220 KB)
- MSDS
- Download (19.7 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Treatment Acute Coronary Syndrome (ACS) 1 4 Completed Treatment Acute Myocardial Infarction (AMI) 3 4 Completed Treatment Angina Pectoris / Coronary Heart Disease (CHD) 1 4 Completed Treatment Coronary Artery Disease (CAD) / Ischaemia 1 4 Completed Treatment Coronary Heart Disease (CHD) / Myocardial Infarction 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Centocor Ortho Biotech Inc.
- Eli Lilly & Co.
- Hospira Inc.
- JHP Pharmaceuticals LLC
- Dosage Forms
Form Route Strength Injection, solution Intravenous 10 mg/5ml Injection, solution Intravenous 2 mg/1mL Solution Intravenous 2 mg / mL Solution Parenteral 10.000 mg Solution Parenteral - Prices
Unit description Cost Unit Reopro 2 mg/ml vial 155.77USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region CA1341357 No 2002-05-07 2019-05-07 Canada
Properties
- State
- Liquid
- Experimental Properties
Property Value Source melting point (°C) 61 °C (FAB fragment), 71 °C (whole mAb) Vermeer, A.W.P. & Norde, W., Biophys. J. 78:394-404 (2000) hydrophobicity -0.424 Not Available isoelectric point 6.16 Not Available
Targets
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Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Virus receptor activity
- Specific Function
- Integrin alpha-V/beta-3 (ITGAV:ITGB3) is a receptor for cytotactin, fibronectin, laminin, matrix metalloproteinase-2, osteopontin, osteomodulin, prothrombin, thrombospondin, vitronectin and von Wil...
- Gene Name
- ITGB3
- Uniprot ID
- P05106
- Uniprot Name
- Integrin beta-3
- Molecular Weight
- 87056.975 Da
References
- Amoroso G, van Boven AJ, van Veldhuisen DJ, Tio RA, Balje-Volkers CP, Petronio AS, van Oeveren W: Eptifibatide and abciximab exhibit equivalent antiplatelet efficacy in an experimental model of stenting in both healthy volunteers and patients with coronary artery disease. J Cardiovasc Pharmacol. 2001 Oct;38(4):633-41. [Article]
- Weber AA, Meila D, Jacobs C, Weber S, Kelm M, Strauer BE, Zotz RB, Scharf RE, Schror K: Low incidence of paradoxical platelet activation by glycoprotein IIb/IIIa inhibitors. Thromb Res. 2002 Apr 1;106(1):25-9. [Article]
- Hall PR, Malone L, Sillerud LO, Ye C, Hjelle BL, Larson RS: Characterization and NMR solution structure of a novel cyclic pentapeptide inhibitor of pathogenic hantaviruses. Chem Biol Drug Des. 2007 Mar;69(3):180-90. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Mazzaferri EL Jr, Young JJ: Abciximab: a review and update for clinicians. Expert Rev Cardiovasc Ther. 2008 Jun;6(5):609-18. doi: 10.1586/14779072.6.5.609. [Article]
- Ibbotson T, McGavin JK, Goa KL: Abciximab: an updated review of its therapeutic use in patients with ischaemic heart disease undergoing percutaneous coronary revascularisation. Drugs. 2003;63(11):1121-63. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Metal ion binding
- Specific Function
- Integrin alpha-IIb/beta-3 is a receptor for fibronectin, fibrinogen, plasminogen, prothrombin, thrombospondin and vitronectin. It recognizes the sequence R-G-D in a wide array of ligands. It recogn...
- Gene Name
- ITGA2B
- Uniprot ID
- P08514
- Uniprot Name
- Integrin alpha-IIb
- Molecular Weight
- 113375.96 Da
References
- Gibbs NM: Point-of-care assessment of antiplatelet agents in the perioperative period: a review. Anaesth Intensive Care. 2009 May;37(3):354-69. [Article]
- Mazzaferri EL Jr, Young JJ: Abciximab: a review and update for clinicians. Expert Rev Cardiovasc Ther. 2008 Jun;6(5):609-18. doi: 10.1586/14779072.6.5.609. [Article]
- Ibbotson T, McGavin JK, Goa KL: Abciximab: an updated review of its therapeutic use in patients with ischaemic heart disease undergoing percutaneous coronary revascularisation. Drugs. 2003;63(11):1121-63. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Curator comments
- Evidence regarding this target action is limited in the literature
- General Function
- Not Available
- Specific Function
- Binds to the Fc region of immunoglobulins gamma. Low affinity receptor. By binding to IgG it initiates cellular responses against pathogens and soluble antigens. Promotes phagocytosis of opsonized ...
- Gene Name
- FCGR2A
- Uniprot ID
- P12318
- Uniprot Name
- Low affinity immunoglobulin gamma Fc region receptor II-a
- Molecular Weight
- 35000.42 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Curator comments
- Evidence regarding this target action is limited in the literature
- General Function
- Not Available
- Specific Function
- Receptor for the Fc region of complexed or aggregated immunoglobulins gamma. Low affinity receptor. Involved in a variety of effector and regulatory functions such as phagocytosis of immune complex...
- Gene Name
- FCGR2B
- Uniprot ID
- P31994
- Uniprot Name
- Low affinity immunoglobulin gamma Fc region receptor II-b
- Molecular Weight
- 34043.355 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Scavenger receptor activity
- Specific Function
- Vitronectin is a cell adhesion and spreading factor found in serum and tissues. Vitronectin interact with glycosaminoglycans and proteoglycans. Is recognized by certain members of the integrin fami...
- Gene Name
- VTN
- Uniprot ID
- P04004
- Uniprot Name
- Vitronectin
- Molecular Weight
- 54305.135 Da
References
- Romagnoli E, Burzotta F, Trani C, Biondi-Zoccai GG, Giannico F, Crea F: Rationale for intracoronary administration of abciximab. J Thromb Thrombolysis. 2007 Feb;23(1):57-63. [Article]
- Ibbotson T, McGavin JK, Goa KL: Abciximab: an updated review of its therapeutic use in patients with ischaemic heart disease undergoing percutaneous coronary revascularisation. Drugs. 2003;63(11):1121-63. [Article]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55