DT-Web

DB00775 - Tirofiban


Identification
Name Tirofiban
Accession Number DB00775 (APRD00304)
Type small molecule
Description Tirofiban prevents the blood from clotting during episodes of chest pain or a heart attack, or while the patient is undergoing a procedure to treat a blocked coronary artery. It is a non-peptide reversible antagonist of the platelet glycoprotein (GP) IIb/IIIa receptor, and inhibits platelet aggregation.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 440.597
Groups approved
Monoisotopic Weight 440.234492962
Pharmacology
Indication For treatment, in combination with heparin, of acute coronary syndrome, including patients who are to be managed medically and those undergoing PTCA or atherectomy.
Mechanism of action Tirofiban is a reversible antagonist of fibrinogen binding to the GP IIb/IIIa receptor, the major platelet surface receptor involved in platelet aggregation. Platelet aggregation inhibition is reversible following cessation of the infusion of tirofiban.
Absorption Not Available
Protein binding 65%
Biotransformation Metabolism appears to be limited.
Route of elimination It is cleared from the plasma largely by renal excretion, with about 65% of an administered dose appearing in urine and about 25% in feces, both largely as unchanged tirofiban.
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions
Drug Mechanism of interaction
Abciximab Additive effects. Concomitant use is contraindicated.
Eptifibatide Additive effects. Concomitant use is contraindicated.
Ginkgo biloba Additive anticoagulant/antiplatelet effects may increase bleed risk. Concomitant therapy should be avoided.
Treprostinil The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Tirofiban. Monitor for increased bleeding during concomitant thearpy.
Food Interactions Not Available

Targets


Integrin alpha-IIb
Name Integrin alpha-IIb
Gene Name ITGA2B
Pharmacological action yes
Actions antagonist
References
  • Theroux P, Alexander J Jr, Pharand C, Barr E, Snapinn S, Ghannam AF, Sax FL: Glycoprotein IIb/IIIa receptor blockade improves outcomes in diabetic patients presenting with unstable angina/non-ST-elevation myocardial infarction: results from the Platelet Receptor Inhibition in Ischemic Syndrome Management in Patients Limited by Unstable Signs and Symptoms (PRISM-PLUS) study. Circulation. 2000 Nov 14;102(20):2466-72. - Pubmed
  • Dickfeld T, Ruf A, Pogatsa-Murray G, Muller I, Engelmann B, Taubitz W, Fischer J, Meier O, Gawaz M: Differential antiplatelet effects of various glycoprotein IIb-IIIa antagonists. Thromb Res. 2001 Jan 15;101(2):53-64. - Pubmed
  • von Segesser LK, Mueller X, Marty B, Horisberger J, Corno A: Alternatives to unfractionated heparin for anticoagulation in cardiopulmonary bypass. Perfusion. 2001 Sep;16(5):411-6. - Pubmed
  • Kondo K, Umemura K: Clinical pharmacokinetics of tirofiban, a nonpeptide glycoprotein IIb/IIIa receptor antagonist: comparison with the monoclonal antibody abciximab. Clin Pharmacokinet. 2002;41(3):187-95. - Pubmed
  • Roffi M, Moliterno DJ, Meier B, Powers ER, Grines CL, DiBattiste PM, Herrmann HC, Bertrand M, Harris KE, Demopoulos LA, Topol EJ: Impact of different platelet glycoprotein IIb/IIIa receptor inhibitors among diabetic patients undergoing percutaneous coronary intervention: : Do Tirofiban and ReoPro Give Similar Efficacy Outcomes Trial (TARGET) 1-year follow-up. Circulation. 2002 Jun 11;105(23):2730-6. - Pubmed
  • Juwana YB, Suryapranata H, Ottervanger JP, van 't Hof AW: Tirofiban for myocardial infarction. Expert Opin Pharmacother. 2010 Apr;11(5):861-6. - Pubmed
DTHybrid score 0.8506
Integrin beta-3
Name Integrin beta-3
Gene Name ITGB3
Pharmacological action yes
Actions antagonist
References
  • Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. - Pubmed
  • Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. - Pubmed
  • Juwana YB, Suryapranata H, Ottervanger JP, van 't Hof AW: Tirofiban for myocardial infarction. Expert Opin Pharmacother. 2010 Apr;11(5):861-6. - Pubmed
DTHybrid score 1.2645

Predictions


Id Partner name Gene Name Score
1733 Vitronectin VTN 0.1099
3820 Low affinity immunoglobulin gamma Fc region receptor II-b FCGR2B 0.0947
2782 Complement C1s subcomponent C1S 0.067
6065 Integrin beta-1 ITGB1 0.0625
660 T-cell surface glycoprotein CD1a CD1A 0.0624
6063 Major histocompatibility complex class I-related gene protein MR1 0.0624
5955 T-cell surface glycoprotein CD4 CD4 0.0624
6066 Integrin alpha-V ITGAV 0.0624
3816 Complement C1q subcomponent subunit B C1QB 0.0617
3815 Complement C1q subcomponent subunit A C1QA 0.0617
3817 Complement C1q subcomponent subunit C C1QC 0.0617
1102 Low affinity immunoglobulin gamma Fc region receptor III-B FCGR3B 0.061
3818 Low affinity immunoglobulin gamma Fc region receptor III-A FCGR3A 0.061
3819 Low affinity immunoglobulin gamma Fc region receptor II-a FCGR2A 0.061
3821 Low affinity immunoglobulin gamma Fc region receptor II-c FCGR2C 0.061
3814 Complement C1r subcomponent C1R 0.061
784 High affinity immunoglobulin gamma Fc receptor I FCGR1A 0.0589
942 T-lymphocyte activation antigen CD86 CD86 0.0501
572 Integrin alpha-L ITGAL 0.0383
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