Abciximab

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
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.

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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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
Adverseeffects
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Toxicity

Not Available

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 Abciximab is combined with Acemetacin.
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.
AducanumabThe risk or severity of adverse effects can be increased when Abciximab is combined with Aducanumab.
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 bleeding can be increased when Abciximab is combined with Alemtuzumab.
Interactions
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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

Products2
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dosage, form, labeller, route of administration, and marketing period.
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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
ReoproSolution2 mg / mLIntravenousJanssen Pharmaceuticals1996-10-302018-06-14Canada flag
ReoproInjection, solution2 mg/1mLIntravenousJanssen Biotech, Inc.2017-01-032019-09-30US flag
ReoproInjection, solution2 mg/1mLIntravenousEli Lilly and Company1993-12-162019-01-31US flag

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
Affected organisms
  • Humans and other mammals

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. [Article]
  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. [Article]
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
FDA label
Download (220 KB)
MSDS
Download (19.7 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentAcute Coronary Syndrome (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
4CompletedTreatmentShock, Cardiogenic1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Centocor Ortho Biotech Inc.
  • Eli Lilly & Co.
  • Hospira Inc.
  • JHP Pharmaceuticals LLC
Dosage Forms
FormRouteStrength
Injection, solutionIntravenous
Injection, solutionIntravenous10 mg/5ml
Injection, solutionIntravenous2 mg/1mL
SolutionIntravenous2 mg / mL
SolutionParenteral
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 flag

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

Drugtargets2
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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
  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. [Article]
  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. [Article]
  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. [Article]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
  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. [Article]
  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. [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
  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. [Article]
  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. [Article]
  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. [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
  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. [Article]
  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. [Article]

Drug created on June 13, 2005 13:24 / Updated on October 24, 2021 16:00