General Information of DTT (ID: TT38RM1)

DTT Name Glycoprotein IIb/IIIa receptor (GPIIb/IIIa) DTT Info
Gene Name ITGA2B

Molecule-Related Drug & Molecule List

Molecule-Related Drug List
Molecule Type:
DTT
DTP
DME
Drug Status:
Discontinued Drug(s)
Approved Drug(s)
Clinical Trial Drug(s)
Investigative Drug(s)
4 Approved Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Abciximab DMJO6GV Acute disease Approved [1]
Eptifibatide DMQXTJS Acute cardiac ischemic events BA40.Z Approved [2]
Hydroquinone DM6AVR4 Melasma ED60.1 Approved [3]
Tirofiban DMQG17S Acute coronary syndrome BA41 Approved [1]
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6 Clinical Trial Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
DMP-444 DMO7BQS Coronary artery disease BA80 Phase 3 [4]
99mTc-rBitistatin DMFAMNH Pulmonary embolism JB42 Phase 1/2 [5]
AjvW2 DM6PN4H Thrombosis DB61-GB90 Phase 1 [6]
Lefradafiban DMKZVLH Angina pectoris BA40 Phase 1 [7]
RGD-891 DMVJMF1 Thrombosis DB61-GB90 Phase 1 [8]
SDZ-GPI-562 DMU9ZGN Thrombosis DB61-GB90 Phase 1 [9]
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⏷ Show the Full List of 6 Clinical Trial Drug(s)
28 Discontinued Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
LAMIFIBAN DMHR1A7 Angina pectoris BA40 Discontinued in Phase 3 [10]
LOTRAFIBAN DMHE804 Cardiovascular disease BA00-BE2Z Discontinued in Phase 3 [11]
ORBOFIBAN DMEDLXJ Angina pectoris BA40 Discontinued in Phase 3 [12]
SIBRAFIBAN DMZU1TV Angina pectoris BA40 Discontinued in Phase 3 [13]
XEMILOFIBAN DMBRYT8 Cardiovascular disease BA00-BE2Z Discontinued in Phase 3 [14]
Cromafiban DMZLIUQ Coronary artery disease BA80 Discontinued in Phase 2 [15]
ELAROFIBAN DM7TM91 Thrombosis DB61-GB90 Discontinued in Phase 2 [16]
FK-633 DMQ3O4C Artery stenosis BD52 Discontinued in Phase 2 [17]
Gantofiban DMHAM2J Arteriosclerosis BD40 Discontinued in Phase 2 [18]
MK-852 DMBJLZG Thrombosis DB61-GB90 Discontinued in Phase 2 [15]
SR-121787 DMCEQKG Thrombosis DB61-GB90 Discontinued in Phase 2 [19]
YM-337 DMCZIGQ Angiogenesis disorder BE2Z Discontinued in Phase 2 [20]
ZD-2486 DMLFNMB Angina pectoris BA40 Discontinued in Phase 2 [15]
DMP-728 DMCK7LM Thrombosis DB61-GB90 Discontinued in Phase 1 [21]
FR-158999 DM5FW8Y Thrombosis DB61-GB90 Discontinued in Phase 1 [22]
L-734217 DMSB0J8 Thrombosis DB61-GB90 Discontinued in Phase 1 [23]
ME-3277 DMUMSFR Thrombosis DB61-GB90 Discontinued in Phase 1 [24]
SC-52012 DMFC19E Thrombosis DB61-GB90 Discontinued in Phase 1 [25]
TAK-029 DMN02XD Thrombosis DB61-GB90 Discontinued in Phase 1 [26]
TP-9201 DMCV2KQ Thrombosis DB61-GB90 Discontinued in Phase 1 [27]
BIBU-251 DMMNI5K Thrombosis DB61-GB90 Terminated [28]
Fradafiban DMN4E5H Thrombosis DB61-GB90 Terminated [29]
GR-144053 DMN8TH1 Thrombosis DB61-GB90 Terminated [30]
GR-233548 DMHM0EU Thrombosis DB61-GB90 Terminated [1]
L-703014 DM47MKE Thrombosis DB61-GB90 Terminated [31]
SB-208651 DMJD15H Thrombosis DB61-GB90 Terminated [32]
SC-49992 DMY7KHW Arterial thrombosis DB61-DD30 Terminated [33]
SKF-106760 DM7QPYK Thrombosis DB61-GB90 Terminated [1]
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⏷ Show the Full List of 28 Discontinued Drug(s)
3 Investigative Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
RGD DMFASRB Discovery agent N.A. Investigative [34]
RGD-039 DM0O9VG Thrombosis DB61-GB90 Investigative [35]
XV454 DML1K07 Discovery agent N.A. Investigative [36]
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Molecule Interaction Atlas

References

1 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
2 Barbourin. A GPIIb-IIIa-specific integrin antagonist from the venom of Sistrurus m. barbouri. J Biol Chem. 1991 May 25;266(15):9359-62.
3 Accutin, 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.
4 Evaluation 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.
5 Platelet binding and biodistribution of [99mTc]rBitistatin in animal species and humans. Nucl Med Biol. 2007 Oct;34(7):855-63.
6 Novel approaches to the treatment of thrombosis. Trends Pharmacol Sci. 2002 Jan;23(1):25-32.
7 Pharmacodynamics 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.
8 Pharmacokinetics, 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.
9 Heparin-induced thrombocytopenia: the role of platelet activation and therapeutic implications. Semin Thromb Hemost. 1999;25 Suppl 1:67-75.
10 Lamifiban. Drugs. 1999 Feb;57(2):215-21; discussion 222-3.
11 Lotrafiban: an oral platelet glycoprotein IIb/IIIa blocker.Expert Opin Investig Drugs.2000 Nov;9(11):2673-87.
12 Orbofiban: an orally active GPIIb/IIIa platelet receptor antagonist. Med Res Rev. 2001 May;21(3):211-26.
13 Pharmacokinetics and pharmacodynamics of sibrafiban, an orally administered GP IIb/IIIa antagonist, following coadministration of aspirin and heparin. J Clin Pharmacol. 2000 May;40(5):488-95.
14 Glycoprotein IIb/IIIa receptor number and occupancy during chronic administration of an oral antagonist. J Pharmacol Exp Ther. 2000 Nov;295(2):670-6.
15 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
16 1,2,4-triazolo[3,4-a]pyridine as a novel, constrained template for fibrinogen receptor (GPIIb/IIIa) antagonists. Bioorg Med Chem Lett. 2001 Oct 8;11(19):2619-22.
17 Efficacy of FK633, an ultra-short acting glycoprotein IIb/IIIa antagonist on platelet preservation during and after cardiopulmonary bypass. Eur J Cardiothorac Surg. 2004 Aug;26(2):289-93.
18 Enantioseparation of gantofiban precursors on chiral stationary phases of the poly-(N-acryloyl amino acid derivative)-type. J Pharm Biomed Anal. 2002 Jan 15;27(3-4):627-37.
19 Prevention of thrombosis and enhancement of thrombolysis in rabbits by SR 121787, a glycoprotein II/III antagonist. J Pharmacol Exp Ther. 1998 Aug;286(2):670-5.
20 Pharmacodynamic characterization of the interaction between the glycoprotein IIb/IIIa inhibitor YM337 and unfractionated heparin and aspirin in hum... Br J Clin Pharmacol. 2003 Sep;56(3):321-6.
21 Antiplatelet and antithrombotic efficacy of DMP 728, a novel platelet GPIIb/IIIa receptor antagonist. Circulation. 1994 Jan;89(1):3-12.
22 QSAR 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.
23 Nonpeptide glycoprotein IIb/IIIa inhibitors. 8. Antiplatelet activity and oral antithrombotic efficacy of L-734,217. J Pharmacol Exp Ther. 1996 Jul;278(1):62-73.
24 ME3277, 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.
25 Characterization of Binding of an RGD Mimetic, [(3)H]-SC-52012, to Platelet GPIIb/IIIa. Platelets. 1995;6(5):288-95.
26 Platelet protective effect of TAK-029, a novel glycoprotein IIb/IIIa antagonist: an in vitro study. Artif Organs. 1998 Apr;22(4):348-52.
27 TP-9201, a glycoprotein IIb/IIIa platelet receptor antagonist, prevents rethrombosis after successful arterial thrombolysis in the dog. Stroke. 1997 Sep;28(9):1789-96.
28 CN patent application no. 101312747, Anticoagulant antithrombotic dual inhibitors comprising a biotin label.
29 Profound 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.
30 GR144053, a fibrinogen receptor antagonist, enhances the suppression of neointima formation by losartan, an angiotensin II receptor antagonist, in ... Br J Pharmacol. 1997 Nov;122(6):1099-104.
31 Pharmacokinetics and pharmacodynamics of L-703,014, a potent fibrinogen receptor antagonist, after intravenous and oral administration in the dog. Pharm Res. 1994 Mar;11(3):426-31.
32 Design of a potent and orally active nonpeptide platelet fibrinogen receptor (GPIIb/IIIa) antagonist. Bioorg Med Chem. 1994 Sep;2(9):897-908.
33 SC-49992--a potent and specific inhibitor of platelet aggregation. Thromb Res. 1994 Jun 1;74(5):523-35.
34 AlphaIIbbeta3 and its antagonism at the new millennium. Thromb Haemost. 2001 Jul;86(1):34-40.
35 Pharmacokinetics 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.
36 Inhibition of tumor cell-induced platelet aggregation and lung metastasis by the oral GpIIb/IIIa antagonist XV454. Thromb Haemost. 2003 Sep;90(3):549-54.