Target Information

Target General Infomation
Target ID
T50688
Former ID
TTDS00077
Target Name
Glycoprotein IIb/IIIa receptor
Synonyms
Alpha(IIb)beta(3) integrin receptor; Fibrinogen receptor; GPIIb-IIIa receptor; Glycoprotein GP IIb/IIIa; Glycoprotein IIb/IIIa; Gp IIb/IIIa; GpIIb/IIIa receptor; Integrin IIb beta3; Integrin IIbbeta3; Integrin alpha IIb beta 3; Integrin alphaIIbbeta3; Platelet GPIIb-IIIa; Platelet GPIIb/IIIa receptor; Platelet glycoprotein IIb/IIIa fibrinogen receptor complex; Platelet integrin IIbbeta3
Target Type
Successful
Disease Arterial thrombosis [ICD9: 437.6, 453, 671.5, 671.9; ICD10: I80-I82]
Angina pectoris [ICD9: 413; ICD10: I20]
Acute cardiac ischemic events [ICD9: 410; ICD10: I21, I22]
Acute coronary syndrome [ICD9: 444; ICD10: I74]
Arteriosclerosis [ICD9: 440; ICD10: I70]
Angiogenesis disorder [ICD10: I00-I99]
Cardiovascular disorder [ICD10: I00-I99]
Coronary artery disease [ICD9: 410-414, 429.2; ICD10: I20-I25]
Embolism [ICD10: I74, I82]
Restenosis [ICD10: I51.89]
Thrombosis [ICD9: 437.6, 453, 671.5, 671.9; ICD10: I80-I82]
Thromboembolism [ICD9: 437.6, 453, 671.5, 671.9; ICD10: I80-I82]
Unspecified [ICD code not available]
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 recognizes the sequence H-H-L-G-G-G-A-K-Q-A-G-D-V in fibrinogen gamma chain. Following activation integrin alpha- IIb/beta-3 brings about platelet/platelet interaction through binding of soluble fibrinogen. This step leads to rapid platelet aggregation which physically plugs ruptured endothelial cell surface.
Target Validation
T50688
UniProt ID
P08514||P05106
Drugs and Mode of Action
Drug(s) Abciximab Drug Info Approved Angina pectoris [536373], [541704]
Eptifibatide Drug Info Approved Acute cardiac ischemic events [536361], [541705]
Tirofiban Drug Info Approved Acute coronary syndrome [536361], [541706]
DMP-444 Drug Info Phase 3 Coronary artery disease [531571]
99mTc-rBitistatin Drug Info Phase 1/2 Embolism [522520]
AjvW2 Drug Info Phase 1 Thrombosis [546704]
Lefradafiban Drug Info Phase 1 Angina pectoris [524952]
RGD-891 Drug Info Phase 1 Thrombosis [525902]
SDZ-GPI-562 Drug Info Phase 1 Thrombosis [545840]
LAMIFIBAN Drug Info Discontinued in Phase 3 Angina pectoris [545506]
LOTRAFIBAN Drug Info Discontinued in Phase 3 Cardiovascular disorder [545754]
ORBOFIBAN Drug Info Discontinued in Phase 3 Angina pectoris [546385]
SIBRAFIBAN Drug Info Discontinued in Phase 3 Angina pectoris [546172]
Cromafiban Drug Info Discontinued in Phase 2 Coronary artery disease [546806]
ELAROFIBAN Drug Info Discontinued in Phase 2 Thrombosis [546842]
FK-633 Drug Info Discontinued in Phase 2 Restenosis [546141]
Gantofiban Drug Info Discontinued in Phase 2 Arteriosclerosis [546857]
MK-852 Drug Info Discontinued in Phase 2 Thrombosis [545011]
RPR-109891 Drug Info Discontinued in Phase 2 Angina pectoris [546386]
SR-121787 Drug Info Discontinued in Phase 2 Thrombosis [546615]
YM-337 Drug Info Discontinued in Phase 2 Angiogenesis disorder [545993]
ZD-2486 Drug Info Discontinued in Phase 2 Angina pectoris [546102]
DMP-728 Drug Info Discontinued in Phase 1 Thrombosis [545470]
FR-158999 Drug Info Discontinued in Phase 1 Thrombosis [547007]
L-734217 Drug Info Discontinued in Phase 1 Thrombosis [546058]
ME-3277 Drug Info Discontinued in Phase 1 Thrombosis [546256]
SC-52012 Drug Info Discontinued in Phase 1 Thrombosis [545517]
TAK-029 Drug Info Discontinued in Phase 1 Thrombosis [545841]
TP-9201 Drug Info Discontinued in Phase 1 Thrombosis [545013]
BIBU-251 Drug Info Terminated Thromboembolism [545782]
Fradafiban Drug Info Terminated Thromboembolism [545962]
GR-144053 Drug Info Terminated Thromboembolism [541707], [545648]
GR-233548 Drug Info Terminated Thrombosis [546874]
L-703014 Drug Info Terminated Thromboembolism [545810]
SB-208651 Drug Info Terminated Thrombosis [545786]
SC-49992 Drug Info Terminated Arterial thrombosis [545012]
SKF-106760 Drug Info Terminated Thromboembolism [545630]
Modulator 99mTc-rBitistatin Drug Info [529086]
Abciximab Drug Info [556264]
BIBU-251 Drug Info [550135]
Cromafiban Drug Info [1572591]
CS-551 Drug Info
DMP-444 Drug Info [526689]
DMP-728 Drug Info
ELAROFIBAN Drug Info [526139]
Eptifibatide Drug Info [530803]
FK-633 Drug Info
Fradafiban Drug Info [534455]
Gantofiban Drug Info
GR-144053 Drug Info
GR-233548 Drug Info [556264]
L-703014 Drug Info
L-734217 Drug Info
LAMIFIBAN Drug Info
Lefradafiban Drug Info [526006]
LOTRAFIBAN Drug Info
ME-3277 Drug Info [525831]
MK-852 Drug Info [1572591]
ORBOFIBAN Drug Info
RGD-039 Drug Info [525886], [525902]
RGD-891 Drug Info [525902]
RPR-109891 Drug Info [525810]
SB-208651 Drug Info
SC-49992 Drug Info
SC-52012 Drug Info [531247]
SDZ-GPI-562 Drug Info
SIBRAFIBAN Drug Info
SKF-106760 Drug Info [556264]
SR-121787 Drug Info
TAK-029 Drug Info
Tirofiban Drug Info [556264]
TP-9201 Drug Info [534473]
YM-337 Drug Info
ZD-2486 Drug Info [1572591]
Antagonist Accutin Drug Info [538134]
FR-158999 Drug Info [551652], [551871]
XV454 Drug Info [535788]
Binder RGD Drug Info [535229]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
Reactome Platelet degranulation
Elastic fibre formation
PECAM1 interactions
Molecules associated with elastic fibres
Integrin cell surface interactions
Syndecan interactions
ECM proteoglycans
Integrin alphaIIb beta3 signaling
SOS provides linkage to MAPK signaling for Integrins
p130Cas linkage to MAPK signaling for integrins
VEGFA-VEGFR2 Pathway
MAP2K and MAPK activation
WikiPathways Focal Adhesion
Hematopoietic Stem Cell Differentiation
Human Complement System
Extracellular matrix organization
Arrhythmogenic Right Ventricular Cardiomyopathy
Integrin-mediated Cell Adhesion
L1CAM interactions
Integrin cell surface interactions
Integrin alphaIIb beta3 signaling
References
Ref 522520ClinicalTrials.gov (NCT00808626) Phase II Investigation of 99mTc-rBitistatin for Imaging Venous Thrombosis. U.S. National Institutes of Health.
Ref 524952ClinicalTrials.gov (NCT02264106) Influence of Pantoprazole on the Pharmacokinetics of Fradafiban After Multiple Oral Doses of Lefradafiban Over 5 Days in Healthy Subjects. U.S. National Institutes ofHealth.
Ref 525902Pharmacokinetics, pharmacodynamics, and safety of a platelet GPIIb/IIIa antagonist, RGD891, following intravenous administration in healthy male volunteers. J Clin Pharmacol. 2000 Nov;40(11):1245-56.
Ref 531571Evaluation of 99mTc-labeled cyclic RGD peptide with a PEG4 linker for thrombosis imaging: comparison with DMP444. Bioconjug Chem. 2011 Aug 17;22(8):1715-22.
Ref 536361Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20.
Ref 536373Advances in ischemic stroke treatment: neuroprotective and combination therapies. Expert Opin Emerg Drugs. 2007 Mar;12(1):97-112.
Ref 541704(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6584).
Ref 541705(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6585).
Ref 541706(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6586).
Ref 541707(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6587).
Ref 545011Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001868)
Ref 545012Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001873)
Ref 545013Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001874)
Ref 545470Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003382)
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Ref 545782Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004683)
Ref 545786Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004708)
Ref 545810Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004828)
Ref 545840Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005009)
Ref 545841Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005011)
Ref 545962Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005534)
Ref 545993Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005765)
Ref 546058Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006092)
Ref 546102Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006364)
Ref 546141Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006561)
Ref 546172Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006751)
Ref 546256Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007141)
Ref 546385Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007819)
Ref 546386Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007824)
Ref 546615Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009197)
Ref 546704Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009728)
Ref 546806Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010404)
Ref 546842Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010575)
Ref 546857Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010688)
Ref 546874Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010798)
Ref 547007Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011969)
Ref
Ref 525810First report of an intravenous and oral glycoprotein IIb/IIIa inhibitor (RPR 109891) in patients with recent acute coronary syndromes: results of the TIMI 15A and 15B trials. Am Heart J. 2000 Jul;140(1):81-93.
Ref 525831ME3277, a GPIIb/IIIa antagonist reduces cerebral infarction without enhancing intracranial hemorrhage in photothrombotic occlusion of rabbit middle cerebral artery. J Cereb Blood Flow Metab. 2000 Jun;20(6):988-97.
Ref 525886Pharmacokinetics and concentration-effect analysis of intravenous RGD891, a platelet GPIIb/IIIa antagonist, using mixed-effects modeling (NONMEM). J Clin Pharmacol. 2000 Oct;40(10):1129-40.
Ref 525902Pharmacokinetics, pharmacodynamics, and safety of a platelet GPIIb/IIIa antagonist, RGD891, following intravenous administration in healthy male volunteers. J Clin Pharmacol. 2000 Nov;40(11):1245-56.
Ref 526006Pharmacodynamics and safety of lefradafiban, an oral platelet glycoprotein IIb/IIIa receptor antagonist, in patients with stable coronary artery disease undergoing elective angioplasty. Heart. 2001 Apr;85(4):444-50.
Ref 526139Bioorg Med Chem Lett. 2001 Oct 8;11(19):2619-22.1,2,4-triazolo[3,4-a]pyridine as a novel, constrained template for fibrinogen receptor (GPIIb/IIIa) antagonists.
Ref 526689Evaluation of Tc-99m-labeled glycoprotein IIb/IIIa receptor antagonist DMP444 SPECT in patients with infective endocarditis. Clin Nucl Med. 2003 Jun;28(6):480-4.
Ref 529086Platelet binding and biodistribution of [99mTc]rBitistatin in animal species and humans. Nucl Med Biol. 2007 Oct;34(7):855-63. Epub 2007 Jun 8.
Ref 530803Barbourin. A GPIIb-IIIa-specific integrin antagonist from the venom of Sistrurus m. barbouri. J Biol Chem. 1991 May 25;266(15):9359-62.
Ref 531247Characterization of Binding of an RGD Mimetic, [(3)H]-SC-52012, to Platelet GPIIb/IIIa. Platelets. 1995;6(5):288-95.
Ref 534455Profound and sustained inhibition of platelet aggregation by Fradafiban, a nonpeptide platelet glycoprotein IIb/IIIa antagonist, and its orally active prodrug, Lefradafiban, in men. Circulation. 1997Aug 19;96(4):1130-8.
Ref 534473TP-9201, a glycoprotein IIb/IIIa platelet receptor antagonist, prevents rethrombosis after successful arterial thrombolysis in the dog. Stroke. 1997 Sep;28(9):1789-96.
Ref 535229AlphaIIbbeta3 and its antagonism at the new millennium. Thromb Haemost. 2001 Jul;86(1):34-40.
Ref 535352Novel approaches to the treatment of thrombosis. Trends Pharmacol Sci. 2002 Jan;23(1):25-32.
Ref 535788Inhibition of tumor cell-induced platelet aggregation and lung metastasis by the oral GpIIb/IIIa antagonist XV454. Thromb Haemost. 2003 Sep;90(3):549-54.
Ref 538134Accutin, a new disintegrin, inhibits angiogenesis in vitro and in vivo by acting as integrin alphavbeta3 antagonist and inducing apoptosis. Blood. 1998 Nov 1;92(9):3268-76.
Ref 550135CN patent application no. 101312747, Anticoagulant antithrombotic dual inhibitors comprising a biotin label.
Ref 551652QSAR study of the peptidic fibrinogen inhibitors FK633, FR158999 and related derivatives, using a novel and useful hydrophobic descriptor (logPmw). Bioorganic & Medicinal Chemistry Letters Volume 8, Issue 18, 22 September 1998, Pages 2483-2488.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 556264Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
Ref 1572591Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.

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