Abciximab

Identification

Name
Abciximab
Accession Number
DB00054
Description

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
Db00054
Protein Chemical Formula
C6462H9964N1690O2049S48
Protein Average Weight
145651.1 Da
Sequences
>pdb|6V4P|C Chain C, Abciximab, heavy chain
EVQLQQSGTVLARPGASVKMSCEASGYTFTNYWMHWVKQRPGQGLEWIGAIYPGNSDTSY
IQKFKGKAKLTAVTSTTSVYMELSSLTNEDSAVYYCTLYDGYYVFAYWGQGTLVTVSAAS
TKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGL
YSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSCDKTH
References:
  1. BLAST, NIH [Link]
Download FASTA Format
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.

Associated Conditions
Contraindications & Blackbox Warnings
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Pharmacodynamics

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.

TargetActionsOrganism
AIntegrin beta-3
antagonist
Humans
AIntegrin alpha-IIb
antagonist
Humans
ULow affinity immunoglobulin gamma Fc region receptor II-aNot AvailableHumans
ULow affinity immunoglobulin gamma Fc region receptor II-bNot AvailableHumans
UVitronectinNot AvailableHumans
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
Learn about our commercial Adverse Effects data.
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Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Abciximab 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
AceclofenacThe risk or severity of bleeding and hemorrhage can be increased when Aceclofenac is combined with Abciximab.
AcemetacinThe risk or severity of bleeding and hemorrhage can be increased when Acemetacin is combined with Abciximab.
AcenocoumarolThe risk or severity of bleeding can be increased when Abciximab is combined with Acenocoumarol.
Acetylsalicylic acidAcetylsalicylic acid may increase the antiplatelet activities of Abciximab.
AdalimumabThe risk or severity of adverse effects can be increased when Adalimumab is combined with Abciximab.
Albutrepenonacog alfaThe therapeutic efficacy of Albutrepenonacog alfa can be decreased when used in combination with Abciximab.
AlclofenacThe risk or severity of bleeding and hemorrhage can be increased when Alclofenac is combined with Abciximab.
AldesleukinThe risk or severity of bleeding can be increased when Abciximab is combined with Aldesleukin.
AlemtuzumabThe risk or severity of adverse effects can be increased when Abciximab is combined with Alemtuzumab.
AlirocumabThe risk or severity of adverse effects can be increased when Abciximab is combined with Alirocumab.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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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

Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
ReoproInjection, solution2 mg/1mLIntravenousJanssen Biotech, Inc.2017-01-032019-09-30Us
ReoproInjection, solution2 mg/1mLIntravenousEli Lilly and Company1993-12-162019-01-31Us
ReoproSolution2 mgIntravenousJanssen Pharmaceuticals1996-10-302018-06-14Canada
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Categories

ATC Codes
B01AC13 — Abciximab
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

Chemical Identifiers

UNII
X85G7936GV
CAS number
143653-53-6

References

General References
  1. 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. [PubMed:8121459]
  2. 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. [PubMed:12939213]
KEGG Drug
D02778
PubChem Substance
46505910
RxNav
83929
ChEMBL
CHEMBL1201584
Therapeutic Targets Database
DAP000473
PharmGKB
PA448006
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Abciximab
AHFS Codes
  • 92:00.00 — Miscellaneous Therapeutic Agents
FDA label
Download (220 KB)
MSDS
Download (19.7 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedNot AvailableCoronary Artery Disease (CAD)1
4CompletedTreatmentAcute Coronary Syndromes (ACS)1
4CompletedTreatmentAcute Myocardial Infarction (AMI)3
4CompletedTreatmentAngina Pectoris / Coronary Heart Disease (CHD)1
4CompletedTreatmentCoronary Artery Disease (CAD) / Ischaemia1
4CompletedTreatmentCoronary Heart Disease (CHD) / Myocardial Infarction1
4CompletedTreatmentCoronary Heart Disease (CHD) / Unstable Angina Pectoris1
4CompletedTreatmentDiabetes Mellitus1
4CompletedTreatmentIschaemia / Myocardial Infarction2
4CompletedTreatmentMyocardial Infarction3

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Centocor Ortho Biotech Inc.
  • Eli Lilly & Co.
  • Hospira Inc.
  • JHP Pharmaceuticals LLC
Dosage Forms
FormRouteStrength
Injection, solutionIntravenous2 mg/1mL
SolutionIntravenous2 mg
Prices
Unit descriptionCostUnit
Reopro 2 mg/ml vial155.77USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
CA1341357No2002-05-072019-05-07Canada
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

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Properties

State
Liquid
Experimental Properties
PropertyValueSource
melting point (°C)61 °C (FAB fragment), 71 °C (whole mAb)Vermeer, A.W.P. & Norde, W., Biophys. J. 78:394-404 (2000)
hydrophobicity-0.424Not Available
isoelectric point6.16Not Available

Targets

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
  1. 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. [PubMed:11588534]
  2. 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. [PubMed:12165285]
  3. 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. [PubMed:17441904]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  5. 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. [PubMed:18510478]
  6. 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. [PubMed:12749745]
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
  1. Gibbs NM: Point-of-care assessment of antiplatelet agents in the perioperative period: a review. Anaesth Intensive Care. 2009 May;37(3):354-69. [PubMed:19499855]
  2. 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. [PubMed:18510478]
  3. 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. [PubMed:12749745]
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
  1. 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. [PubMed:17160551]
  2. 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. [PubMed:12749745]

Drug created on June 13, 2005 07:24 / Updated on August 05, 2020 23:36

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