DT-Web

DB00054 - Abciximab


Identification
Name Abciximab
Accession Number DB00054 (BIOD00041, BTD00041)
Type biotech
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 (?v?3) receptor found on platelets and vessel wall endothelial and smooth muscle cells.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 145651.1000
Groups approved
Monoisotopic Weight Not Available
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.
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 ?v?3 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.
Absorption Not Available
Protein binding Not Available
Biotransformation 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
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions
Drug Mechanism of interaction
Ginkgo biloba Additive anticoagulant/antiplatelet effects may increase bleed risk. Concomitant therapy should be avoided.
Tirofiban Additive effects. Concomitant use is contraindicated.
Trastuzumab Abciximab may increase the risk of a hypersensitivy reaction to Trastuzumab.
Treprostinil The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Abciximab. Monitor for increased bleeding during concomitant thearpy.
Food Interactions Not Available

Targets


Integrin beta-3
Name Integrin beta-3
Gene Name ITGB3
Pharmacological action yes
Actions antagonist
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. - Pubmed
  • 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
  • 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
  • Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. - Pubmed
  • Mazzaferri EL Jr, Young JJ: Abciximab: a review and update for clinicians. Expert Rev Cardiovasc Ther. 2008 Jun;6(5):609-18. - Pubmed
  • 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
DTHybrid score 1.4705
Integrin alpha-IIb
Name Integrin alpha-IIb
Gene Name ITGA2B
Pharmacological action yes
Actions antagonist
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. - Pubmed
  • Mazzaferri EL Jr, Young JJ: Abciximab: a review and update for clinicians. Expert Rev Cardiovasc Ther. 2008 Jun;6(5):609-18. - Pubmed
  • 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
DTHybrid score 1.0721
Low affinity immunoglobulin gamma Fc region receptor III-B
Name Low affinity immunoglobulin gamma Fc region receptor III-B
Gene Name FCGR3B
Pharmacological action unknown
Actions Not Available
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. - Pubmed
DTHybrid score 1.6824
Complement C1r subcomponent
Name Complement C1r subcomponent
Gene Name C1R
Pharmacological action unknown
Actions Not Available
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. - Pubmed
DTHybrid score 1.5903
Complement C1q subcomponent subunit A
Name Complement C1q subcomponent subunit A
Gene Name C1QA
Pharmacological action unknown
Actions Not Available
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. - Pubmed
DTHybrid score 1.6089
Complement C1q subcomponent subunit B
Name Complement C1q subcomponent subunit B
Gene Name C1QB
Pharmacological action unknown
Actions Not Available
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. - Pubmed
DTHybrid score 1.6097
Complement C1q subcomponent subunit C
Name Complement C1q subcomponent subunit C
Gene Name C1QC
Pharmacological action unknown
Actions Not Available
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. - Pubmed
DTHybrid score 1.6097
Low affinity immunoglobulin gamma Fc region receptor III-A
Name Low affinity immunoglobulin gamma Fc region receptor III-A
Gene Name FCGR3A
Pharmacological action unknown
Actions Not Available
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. - Pubmed
DTHybrid score 1.682
Complement C1s subcomponent
Name Complement C1s subcomponent
Gene Name C1S
Pharmacological action unknown
Actions Not Available
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. - Pubmed
DTHybrid score 1.2346
High affinity immunoglobulin gamma Fc receptor I
Name High affinity immunoglobulin gamma Fc receptor I
Gene Name FCGR1A
Pharmacological action unknown
Actions Not Available
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. - Pubmed
DTHybrid score 1.7657
Low affinity immunoglobulin gamma Fc region receptor II-a
Name Low affinity immunoglobulin gamma Fc region receptor II-a
Gene Name FCGR2A
Pharmacological action unknown
Actions Not Available
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. - Pubmed
DTHybrid score 1.6907
Low affinity immunoglobulin gamma Fc region receptor II-b
Name Low affinity immunoglobulin gamma Fc region receptor II-b
Gene Name FCGR2B
Pharmacological action unknown
Actions Not Available
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. - Pubmed
DTHybrid score 1.7192
Low affinity immunoglobulin gamma Fc region receptor II-c
Name Low affinity immunoglobulin gamma Fc region receptor II-c
Gene Name FCGR2C
Pharmacological action unknown
Actions Not Available
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. - Pubmed
DTHybrid score 1.6962
Vitronectin
Name Vitronectin
Gene Name VTN
Pharmacological action unknown
Actions Not Available
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. - Pubmed
  • 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
DTHybrid score 0.3862

Predictions


Id Partner name Gene Name Score
75 B-lymphocyte antigen CD20 MS4A1 0.368
724 Interleukin-2 receptor alpha chain IL2RA 0.2111
717 Interleukin-2 receptor subunit beta IL2RB 0.2111
844 Epidermal growth factor receptor EGFR 0.1751
777 Tumor necrosis factor TNF 0.1699
744 Myeloid cell surface antigen CD33 CD33 0.1557
93 CAMPATH-1 antigen CD52 0.1474
757 Fusion glycoprotein F0 F 0.147
4875 Fusion glycoprotein F0 F 0.147
572 Integrin alpha-L ITGAL 0.1464
793 T-cell surface antigen CD2 CD2 0.1302
5901 T-cell surface glycoprotein CD3 zeta chain CD247 0.1247
1789 Lymphotoxin-alpha LTA 0.1247
302 T-cell surface glycoprotein CD3 epsilon chain CD3E 0.1247
5900 T-cell surface glycoprotein CD3 gamma chain CD3G 0.1247
5899 T-cell surface glycoprotein CD3 delta chain CD3D 0.1246
1269 Tumor necrosis factor receptor superfamily member 1B TNFRSF1B 0.1246
1783 Intercellular adhesion molecule 1 ICAM1 0.1174
647 Integrin alpha-4 ITGA4 0.1173
955 Complement C5 C5 0.1033
5898 Complement C3 C3 0.103
567 Receptor tyrosine-protein kinase erbB-2 ERBB2 0.0964
183 Vascular endothelial growth factor A VEGFA 0.0927
6065 Integrin beta-1 ITGB1 0.0798
660 T-cell surface glycoprotein CD1a CD1A 0.0797
6063 Major histocompatibility complex class I-related gene protein MR1 0.0797
5955 T-cell surface glycoprotein CD4 CD4 0.0796
6066 Integrin alpha-V ITGAV 0.0796
554 Low-density lipoprotein receptor LDLR 0.0664
942 T-lymphocyte activation antigen CD86 CD86 0.0639
3811 Cytochrome P450 19A1 CYP19A1 0.0627
290 Prostaglandin G/H synthase 2 PTGS2 0.0526
4878 Glycoprotein hormones alpha chain CGA 0.0024
1072 Granzyme B GZMB 0.0024
4189 Alpha-galactosidase A GLA 0.0024
1052 Cytotoxic T-lymphocyte protein 4 CTLA4 0.0024
4889 Ig epsilon chain C region IGHE 0.0024
4877 Beta-mannanase man 0.0024
4871 Endo-beta-N-acetylglucosaminidase F3 endOF3 0.0024
4850 Beta-2-glycoprotein 1 APOH 0.0024
4852 Reticulon-4 receptor RTN4R 0.0024
4880 Membrane cofactor protein CD46 0.0024
4856 CD209 antigen CD209 0.0024
4869 Major capsid protein A430L 0.0024
4845 ADAM 33 ADAM33 0.0024
1563 Platelet glycoprotein Ib alpha chain GP1BA 0.0024
1354 Beta-glucuronidase GUSB 0.0024
442 Envelope glycoprotein gp41 0.0024
4859 Envelope glycoprotein env 0.0024
4882 Dipeptidyl aminopeptidase-like protein 6 DPP6 0.0024
4721 Beta-1,4-mannanase manA 0.0024
3352 Structural polyprotein Not Available 0.0024
3628 Structural polyprotein Not Available 0.0024
4892 Structural polyprotein Not Available 0.0024
1184 Interferon beta IFNB1 0.0021
6858 Inactive carboxylesterase 4 CES1P1 0.0021
4857 Zinc-alpha-2-glycoprotein AZGP1 0.0021
4193 Atrial natriuretic peptide clearance receptor NPR3 0.0021
4890 Hemagglutinin HA 0.0021
6566 Hemagglutinin Not Available 0.0021
4861 Interleukin-6 receptor alpha chain IL6R 0.0021
119 Carcinoembryonic antigen-related cell adhesion molecule 1 CEACAM1 0.0021
1379 Interleukin-12 subunit beta IL12B 0.0021
3837 Cytokine receptor common beta chain CSF2RB 0.0021
3444 Cyanovirin-N Not Available 0.002
18 High affinity immunoglobulin epsilon receptor subunit alpha FCER1A 0.002
1859 Prostatic acid phosphatase ACPP 0.002
2998 Sialic acid-binding Ig-like lectin 7 SIGLEC7 0.002
852 Heparin cofactor 2 SERPIND1 0.002
3258 Mannosyl-oligosaccharide alpha-1,2-mannosidase MSDC 0.002
3140 Hemagglutinin-neuraminidase HN 0.002
3609 Hemagglutinin-neuraminidase HN 0.002
6120 Cation-independent mannose-6-phosphate receptor IGF2R 0.002
2297 Genome polyprotein Not Available 0.002
2322 Genome polyprotein Not Available 0.002
2694 Genome polyprotein Not Available 0.002
2719 Genome polyprotein Not Available 0.002
2860 Genome polyprotein Not Available 0.002
2928 Genome polyprotein Not Available 0.002
3160 Genome polyprotein Not Available 0.002
3260 Genome polyprotein Not Available 0.002
4783 Genome polyprotein Not Available 0.002
5726 Genome polyprotein Not Available 0.002
5779 Genome polyprotein Not Available 0.002
5867 Genome polyprotein Not Available 0.002
6253 Genome polyprotein Not Available 0.002
6301 Genome polyprotein Not Available 0.002
6380 Genome polyprotein Not Available 0.002
6381 Genome polyprotein Not Available 0.002
6437 Genome polyprotein Not Available 0.002
6520 Genome polyprotein Not Available 0.002
6521 Genome polyprotein Not Available 0.002
6652 Genome polyprotein Not Available 0.002
6734 Genome polyprotein Not Available 0.002
6735 Genome polyprotein Not Available 0.002
6736 Genome polyprotein Not Available 0.002
6737 Genome polyprotein Not Available 0.002
6738 Genome polyprotein Not Available 0.002
6739 Genome polyprotein Not Available 0.002
6744 Genome polyprotein Not Available 0.002
6748 Genome polyprotein Not Available 0.002
6894 Genome polyprotein Not Available 0.002
6898 Genome polyprotein Not Available 0.002
4666 Fucose-binding lectin PA-IIL lecB 0.0019
2372 Bifunctional tail protein 9 0.0019
4787 Envelope glycoprotein gp160 env 0.0019
4820 Envelope glycoprotein gp160 env 0.0019
5727 Envelope glycoprotein gp160 env 0.0019
2577 Endoplasmic reticulum mannosyl-oligosaccharide 1,2-alpha-mannosidase MAN1B1 0.0018
3480 Mannan endo-1,4-beta-mannosidase manA 0.0017
64 Neuraminidase NA 0.0017
641 Neuraminidase NA 0.0017
2676 Neuraminidase NA 0.0017
3026 Neuraminidase NA 0.0017
3519 Neuraminidase NA 0.0017
6007 Neuraminidase NA 0.0017
595 Fibrinogen alpha chain FGA 0.0017
1782 Neutrophil gelatinase-associated lipocalin LCN2 0.0017
1439 Lactotransferrin LTF 0.0017
1243 Cathepsin D CTSD 0.0016
2430 Chondroitinase B cslB 0.0016
958 Insulin-like growth factor 1 receptor IGF1R 0.0016
6307 Ig gamma-2 chain C region IGHG2 0.0015
309 Antithrombin-III SERPINC1 0.0015
2581 Chondroitinase AC cslA 0.0015
6847 Lactase-phlorizin hydrolase LCT 0.0015
6500 Phospholipase A2 PLA2G1B 0.0015
2207 Rhodopsin RHO 0.0014
4785 Ig gamma-1 chain C region IGHG1 0.0013
4604 Liver carboxylesterase 1 CES1 0.0013
76 Nitric-oxide synthase, brain NOS1 0.0013
952 Dipeptidyl peptidase 4 DPP4 0.0011
3923 Cholinesterase BCHE 0.0011
20 Prostaglandin G/H synthase 1 PTGS1 0.001
↑