Intravenous glycoprotein IIb/IIIa antagonists: Their benefits, problems and future developments

Current Pharmaceutical Design

Volumn 10, Issue 14, 2004, Pages 1577-1585

  Curtin, Ronan ^a  

^a ROYAL COLLEGE OF SURGEONS IN IRELAND   (Ireland)

Author keywords

Abciximab; Eptifibatide; Glycoprotein IIb IIIa antagonist; Lamifiban; Partial agonism; PlA polymorphism; Tirofiban

Indexed keywords

ABCIXIMAB; ACETYLSALICYLIC ACID; ANTITHROMBOCYTIC AGENT; CLOPIDOGREL; EPTIFIBATIDE; FIBRINOGEN RECEPTOR ANTAGONIST; GLYCOPROTEIN IIIA; HEPARIN; LAMIFIBAN; ORBOFIBAN; PYRIDINE DERIVATIVE; SIBRAFIBAN; TIROFIBAN;

ACUTE HEART INFARCTION; ANTICOAGULANT THERAPY; ANTICOAGULATION; ANTIINFLAMMATORY ACTIVITY; BLEEDING; CLINICAL TRIAL; DOSE RESPONSE; DRUG EFFICACY; DRUG HALF LIFE; DRUG MECHANISM; DRUG POTENCY; DRUG RESPONSE; GENETIC POLYMORPHISM; HEART MUSCLE ISCHEMIA; HUMAN; INDIVIDUALIZATION; PERCUTANEOUS CORONARY INTERVENTION; PREDICTION; PRIORITY JOURNAL; REVIEW; THROMBOCYTE AGGREGATION INHIBITION;

ANIMALS; CLINICAL TRIALS; CORONARY DISEASE; DRUG ADMINISTRATION SCHEDULE; HUMANS; INJECTIONS, INTRAVENOUS; PLATELET AGGREGATION INHIBITORS; PLATELET GLYCOPROTEIN GPIIB-IIIA COMPLEX;

EID: 2342440480     PISSN: 13816128     EISSN: None     Source Type: Journal    
DOI: 10.2174/1381612043384646     Document Type: Review

References (79)

1. Tam SH, Sassoli PM, Jordan RE, Nakada MT. Abciximab (ReoPro, chimeric 7E3 Fab) demonstrates equivalent affinity and functional blockade of glycoprotein IIb/IIIa and alpha v beta 3 integrins. Circulation 1998; 98: 1085-91.
2. Simon DI, Xu H, Ortlepp S, Rogers C, Rao NK. 7E3 monoclonal antibody directed against the platelet glycoprotein IIb/IIIa cross-reacts with the leukocyte integrin Mac-1 and blocks adhesion to fibrinogen and ICAM-1. Arterioscler Thromb Vasc Biol 1997; 17: 528-35.
3. Lele M, Sajid M, Wajih N, Stouffer GA. Eptifibatide and 7E3, but not tirofiban, inhibit alpha v beta 3 integrin-mediated binding of smooth muscle cells to thrombospondin and prothrombin. Circulation 2001; 104: 582-7.
4. Srivatsa SS, Fitzpatrick LA, Tsao PW, Reilly TM, Holmes DR Jr, Schwartz RS, et al. Selective alpha v beta 3 integrin blockade potently limits neointimal hyperplasia and lumen stenosis following deep coronary arterial stent injury: evidence for the functional importance of integrin alpha v beta 3 and osteopontin expression during neointima formation. Cardiovasc Res 1997; 36: 408-28.
5. Simpson PJ, Todd RF, Fantone JC, Mickelson JK, Griffin JD, Lucchesi BR. Reduction of experimental canine myocardial reperfusion injury by a monoclonal antibody (anti-Mol, anti-CD11b) that inhibits leukocyte adhesion. J Clin Invest 1988; 81: 624-9.
6. Quinn MJ, Murphy RT, Dooley M, Foley JB, Fitzgerald DJ. Occupancy of the internal and external pools of glycoprotein IIb/IIIa following abciximab bolus and infusion. J Pharmacol Exp Ther 2001; 297: 496-500.
7. Scarborough RM, Kleiman NS, Phillips DR. Platelet Gycoprotein IIb/IIIa antagonists. What are the relevant issues concerning their pharmacology and clinical use. Circulation 1999; 100: 437-44.
8. The EPIC Investigators. Use of a monoclonal antibody directed against the platelet glycoprotein IIb/IIIa receptor in high-risk coronary angioplasty. N Engl J Med 1994; 330: 956-61.
9. The CAPTURE Investigators. Randomised placebo-controlled trial of abciximab before and during coronary intervention in refractory unstable angina: the CAPTURE Study. Lancet 1997; 349: 1429-35.
10. The EPILOG Investigators. Platelet glycoprotein IIb/IIIa receptor blockade and low-dose heparin during percutaneous coronary revascularization. N Engl J Med 1997; 336: 1689-96.
11. The EPISTENT Investigators. Evaluation of Platelet IIb/IIIa Inhibitor for Stenting. Randomised placebo-controlled and balloon-angioplasty-controlled trial to assess safety of coronary stenting with use of platelet glycoprotein-IIb/IIIa blockade. Lancet 1998; 352: 87-92.
12. The IMPACT-II Investigators. Randomised placebo-controlled trial of effect of eptifibatide on complications of percutancous coronary intervention: IMPACT-II. Integrilin to Minimise Platelet Aggregation and Coronary Thrombosis-II. Lancet 1997; 349: 1422-8.
13. The RESTORE Investigators. Randomized Efficacy Study of Tirofiban for Outcomes and REstenosis. Effects of platelet glycoprotein IIb/IIIa blockade with tirofiban on adverse cardiac events in patients with unstable angina or acute myocardial infarction undergoing coronary angioplasty. Circulation 1997; 96: 1445-53.
14. The ESPRIT Investigators. Enhanced Suppression of the Platelet IIb/IIIa Receptor with Integrilin Therapy. Novel dosing regimen of eptifibatide in planned coronary stent implantation (ESPRIT): a randomised, placebo-controlled trial. Lancet 2000; 356: 2037-44.
15. Topol EJ, Moliterno DJ, Herrmann HC, Powers ER, Grines CL, Cohen DJ, et al. For the TARGET Investigators. Comparison of two platelet glycoprotein IIb/IIIa inhibitors, tirofiban and abciximab, for the prevention of ischemic events with percutaneous coronary revascularization. N Engl J Med 2001; 344: 1888-94.
16. Moliterno DJ, Yakubov SJ, DiBattiste PM, Herrmann HC, Stone GW, Macaya C, et al. Outcomes at 6 months for the direct comparison of tirofiban and abciximab during percutaneous coronary revascularisation with stent placement: the TARGET follow-up study. Lancet 2002; 360: 355-60.
17. Anderson KM, Califf RM, Stone GW, Neumann FJ, Montalescot G, Miller DP, et al. Long-term mortality benefit with abciximab in patients undergoing percutaneous coronary intervention. J Am Coll Cardiol 2001; 37: 2059-65.
18. Karvouni E, Katritsis DG, Ioannidis JP. Intravenous glycoprotein IIb/IIIa receptor antagonists reduce mortality after percutaneous coronary interventions. J Am Coll Cardiol 2003; 41: 26-32.
19. Bhatt DL, Marso SP, Lincoff AM, Wolski KE, Ellis SG, Topol EJ. Abciximab reduces mortality in diabetics following percutaneous coronary intervention. J Am Coll Cardiol 2000; 35: 922-8.
20. Roffi M, Chew DP, Mukherjee D, Bhatt DL, White JA, Heeschen C, et al. Platelet glycoprotein IIb/IIIa inhibitors reduce mortality in diabetic patients with non-ST-segment-elevation acute coronary syndromes. Circulation 2001; 104: 2767-71.
21. Kleiman NS, Lincoff AM, Kereiakes DJ, Miller DP, Aguirre FV, Anderson KM, et al. Diabetes mellitus, glycoprotein IIb/IIIa blockade, and heparin: evidence for a complex interaction in a multicenter trial. EPILOG Investigators. Circulation 1998; 97: 1912-20.
22. Labinaz M, Madan M, O'Shea JO, Kilaru R, Chin W, Pieper K, et al. Comparison of one-year outcomes following coronary artery stenting in diabetic versus nondiabetic patients (from the Enhanced Suppression of the Platelet IIb/IIIa Receptor With Integrilin Therapy [ESPRIT] Trial). Am J Cardiol 2002; 90: 585-90.
23. Roffi M, Mukherjee D, Chew DP, Bhatt DL, Cho L, Robbins MA, et al. Lack of benefit from intravenous platelet glycoprotein IIb/IIIa receptor inhibition as adjunctive treatment for percutaneous interventions of aortocoronary bypass grafts: a pooled analysis of five randomized clinical trials. Circulation 2002; 106: 3063-7.
24. Mehta SR, Yusuf S, Peters RJ, Bertrand ME, Lewis BS, Natarajan MK, et al. Effects of pretreatment with clopidogrel and aspirin followed by long-term therapy in patients undergoing percutaneous coronary intervention: the PCI-CURE study. Lancet 2001; 358: 527-33.
25. Steinhubl SR, Berger PB, Mann JT, 3rd, Fry ET, DeLago A, Wilmer C, et al. Early and sustained dual oral antiplatelet therapy following percutaneous coronary intervention; a randomized controlled trial. JAMA 2002; 288: 2411-20.
26. Bonz AW, Lengenfelder B, Strotmann J, Held S, Turschner O, Harre K, et al. Effect of additional temporary glycoprotein IIb/IIIa receptor inhibition on troponin release in elective percutaneous coronary interventions after pretreatment with aspirin and clopidogrel (TOPSTAR trial). J Am Coll Cardiol 2002; 40: 662-8.
27. Brener SJ, Barr LA, Burchenal JE, Katz S, George BS, Jones AA, et al. Randomized, placebo-controlled trial of platelet glycoprotein IIb/IIIa blockade with primary angioplasty for acute myocardial infarction. ReoPro and Primary PTCA Organization and Randomized Trial (RAPPORT) Investigators. Circulation 1998; 98: 734-41.
28. Neumann FJ, Blasini R, Schmitt C, Alt E, Dirschinger J, Gawaz M, et al. Effect of glycoprotein IIb/IIIa receptor blockade on recovery of coronary flow and left ventricular function after the placement of coronary-artery stents in acute myocardial infarction. Circulation 1998; 98: 2695-701.
29. Neumann FJ, Kastrati A, Schmitt C, Blasini R, Hadamitzky M, Mehilli J, et al. Effect of glycoprotein IIb/IIIa receptor blockade with abciximab on clinical and angiographic restenosis rate after the placement of coronary stents following acute myocardial infarction. J Am Coll Cardiol 2000; 35: 915-21.
30. Montalescot G, Barragan P, Wittenberg O, Ecollan P, Elhadad S, Villain P, et al. Platelet glycoprotein IIb/IIIa inhibition with coronary stenting for acute myocardial infarction. N Engl J Med 2001; 344: 1895-903.
31. Stone GW, Grines CL, Cox DA, Garcia E, Tcheng JE, Griffin JJ, et al. Comparison of angioplasty with stenting, with or without abciximab, in acute myocardial infarction. N Engl J Med 2002; 346: 957-66.
32. Lee DP, Herity NA, Hiatt BL, Fearon WF, Rezaee M, Carter AJ, et al. Adjunctive platelet glycoprotein receptor inhibition with tirofiban before primary angioplasty improves angiographic outcomes: results of the TIrofiban Given in the Emergency Room before Primary Angioplasty (TIGER-PA) pilot trial. Circulation 2003; 107: 1497-501.
33. Antman EM, Giugliano RP, Gibson CM, McCabe CH, Coussement P, Kleiman NS, et al. Abciximab facilitates the rate and extent of thrombolysis: results of the thrombolysis in myocardial infarction (TIMI) 14 trial. The TIMI 14 Investigators. Circulation 1999; 99: 2720-32.
34. Trial of abciximab with and without low-dose reteplase for acute myocardial infarction. Strategies for Patency Enhancement in the Emergency Department (SPEED) Group. Circulation 2000; 101: 2788-94.
35. Topol EJ. Reperfusion therapy for acute myocardial infarction with fibrinolytic therapy or combination reduced fibrinolytic therapy and platelet glycoprotein IIb/IIIa inhibition: the GUSTO V randomised trial. Lancet 2001; 357: 1905-14.
36. Lincoff AM, Califf RM, Van de Werf F, Willerson JT, White HD, Armstrong PW, et al. Mortality at 1 year with combination platelet glycoprotein IIb/IIIa inhibition and reduced-dose fibrinolytic therapy vs conventional fibrinolytic therapy for acute myocardial infarction: GUSTO V randomized trial. JAMA 2002; 288: 2130-5.
37. Simoons ML. GUSTO IV-ACS Investigators. Effect of glycoprotein IIb/IIIa receptor blocker abciximab on outcome in patients with acute coronary syndromes without early coronary revascularisation: the GUSTO IV-ACS randomised trial. Lancet 2001; 357: 1915-24.
38. The PURSUIT Trial Investigators. Platelet Glycoprotein IIb/IIIa in Unstable Angina: Receptor Suppression Using Integrilin Therapy. Inhibition of platelet glycoprotein IIb/IIIa with eptifibatide in patients with acute coronary syndromes. N Engl J Med 1998; 339: 436-43.
39. PRISM Study Investigators. A comparison of aspirin plus tirofiban with aspirin plus heparin for unstable angina. N Engl J Med 1998; 338: 1498-505.
40. The PARAGON Investigators. International, randomized, controlled trial of lamifiban (a platelet glycoprotein IIb/IIIa inhibitor), heparin, or both in unstable angina. Circulation 1998; 97: 2386-95.
41. Global Organization Network (PARAGON)-B Investigators. Randomized, placebo-controlled trial of titrated intravenous lamifiban for acute coronary syndromes. Circulation 2002; 105: 316-21.
42. Boersma E, Harrington RA, Moliterno DJ, White H, Theroux P, Van de Werf F, et al. Platelet glycoprotein IIb/IIIa inhibitors in acute coronary syndromes: a meta-analysis of all major randomised clinical trials. Lancet 2002; 359: 189-98.
43. Yusuf S, Zhao F, Mehta SR, Chrolavicius S, Tognoni G, Fox KK. Clopidogrel in Unstable Angina to Prevent Recurrent Events Trial Investigators. Effects of clopidogrel in addition to aspirin in patients with acute coronary syndromes without ST-segment elevation. N Engl J Med 2001; 345: 494-502.
44. Bhatt DL, Topol EJ. Current role of platelet glycoprotein IIb/IIIa inhibitors in acute coronary syndromes. Journal of the Amerian Medical Association 2000; 284: 1549-58.
45. Curtin R, Fitzgerald DJ. A cold start for oral glycoprotein IIb/IIIa antagonists. Eur Heart J 2000; 21: 1992-4.
46. George JN, Caen JP, Nurden AT. Glanzmann thrombasthenia: the spectrum of clinical disease. Blood 1990; 75: 1383-95.
47. Gold HK, Coller BS, Yasuda T, Saito T, Fallon JT, Guerrero JL, et al. Rapid and sustained coronary artery recanalization with combined bolus injection of recombinant tissue-type plasminogen activator and monoclonal antiplatelet GPIIb/IIIa antibody in a canine preparation. Circulation 1988; 77: 670-7.
48. Yasuda T, Gold HK, Fallon JT, Leinbach RC, Guerrero JL, Scudder LE, et al. Monoclonal antibody against the platelet glycoprotein (GP) IIb/IIIa receptor prevents coronary artery reocclusion after reperfusion with recombinant tissue-type plasminogen activator in dogs. J Clin Invest 1988; 81: 1284-91.
49. 2+ on GP IIb-IIIa interactions with integrilin: enhanced GP IIb-IIIa binding and inhibition of platelet aggregation by reductions in the concentration of ionized calcium in plasma anticoagulated with citrate. Circulation 1997; 96: 1488-94.
50. Batchelor WB, Tolleson TR, Huang Y, Larsen RL, Mantell RM, Dillard P, et al. Randomized COMparison of platelet inhibition with abciximab, tiRofiban and eptifibatide during percutaneous coronary intervention in acute coronary syndromes: the COMPARE trial. Comparison Of Measurements of Platelet aggregation with Aggrastat, Reopro, and Eptifibatide. Circulation 2002; 106: 1470-6.
51. Kereiakes DJ, Broderick TM, Roth EM, Whang D, Shimshak T, Runyon JP, et al. Time course, magnitude, and consistency of platelet inhibition by abciximab, tirofiban, or eptifibatide in patients with unstable angina pectoris undergoing percutaneous coronary intervention. Am J Cardiol 1999; 84: 391-5.
52. Kabbani SS, Watkins MW, Ashikaga T, Terrien EF, Holoch PA, Sobel BE, et al. Platelet reactivity characterized prospectively: a determinant of outcome 90 days after percutaneous coronary intervention. Circulation 2001; 104: 181-6.
53. Lakkis N, Lakiss N, Bobek J, Farmer J. Platelet inhibition with tirofiban early during percutaneous coronary intervention: dosing revisited. Catheter Cardiovasc Interv 2002; 56: 474-7.
54. The PRISM-PLUS Study Investigators. Inhibition of the platelet glycoprotein IIb/IIIa receptor with tirofiban in unstable angina and non-Q-wave myocardial infarction. N Engl J Med 1998; 338: 1488-97.
55. Tardiff BE, Jennings LK, Harrington RA, Gretler D, Potthoff RF, Vorchheimer DA, et al. Pharmacodynamics and pharmacokinetics of eptifibatide in patients with acute coronary syndromes: prospective analysis from PURSUIT. Circulation 2001; 104: 399-405.
56. Gilchrist IC, O'Shea JC, Kosoglou T, Jennings LK, Lorenz TJ, Kitt MM, et al. Pharmacodynamics and pharmacokinetics of higher-dose, double-bolus eptifibatide in percutaneous coronary intervention. Circulation 2001; 104: 406-11.
57. Smith JW, Steinhubl SR, Lincoff AM, Coleman JC, Lee TT, Hillman RS, et al. Rapid platelet-function assay: an automated and quantitative cartridge-based method. Circulation 1999; 99: 620-5.
58. Steinhubl SR, Talley JD, Braden GA, Tcheng JE, Casterella PJ, Moliterno DJ, et al. Point-of-care measured platelet inhibition correlates with a reduced risk of an adverse cardiac event after percutaneous coronary intervention: results of the GOLD (AU-Assessing Ultegra) multicenter study. Circulation 2001; 103: 2572-8.
59. Shenkman B, Savion N, Dardik R, Tamarin I, Varon D. Testing of platelet deposition on polystyrene surface under flow conditions by the cone and plate(let) analyzer: role of platelet activation, fibrinogen and von Willebrand factor. Thromb Res 1988; 99: 353-61.
60. Kundu SK, Heilmann EJ, Sio R, Garcia C, Davidson RM, Ostgaard RA. Description of an in vitro platelet function analyzer - PFA-100. Semin Thromb Hemost 1995; 21(Suppl 2): 106-12.
61. Shattil SJ, Kashiwagi H, Pampori N. Integrin signaling: the platelet paradigm. Blood 1998; 91: 2645-57.
62. Stephens G, O'Luanaigh N, Reilly D, Harriott P, Walker B, Fitzgerald D, et al. A sequence within the cytoplasmic tail of GpIIb independently activates platelet aggregation and thromboxane synthesis. J Biol Chem 1998; 273: 20317-22.
63. Blystone SD. Kinetic regulation of beta 3 integrin tyrosine phosphorylation. J Biol Chem 2002; 277: 46886-90.
64. Cox D, Smith R, Quinn M, Theroux P, Crean P, Fitzgerald DJ. Evidence of platelet activation during treatment with a GPIIb/IIIa antagonist in patients presenting with acute coronary syndromes. J Am Coll Cardiol 2000; 36: 1514-9.
65. Nannizzi-Alaimo L, Alves VL, Phillips DR. Inhibitory effects of glycoprotein IIb/IIIa antagonists and aspirin on the release of soluble CD40 ligand during platelet stimulation. Circulation 2003; 107: 1123-8.
66. Sarma J, Laan CA, Alam S, Jha A, Fox KA, Dransfield I. Increased platelet binding to circulating monocytes in acute coronary syndromes. Circulation 2002; 105: 2166-71.
67. Gottsauner-Wolf M, Zasmeta G, Hornykewycz S, Nikfardjam M, Stepan E, Wexberg P, et al. Plasma levels of C-reactive protein after coronary stent implantation. Eur Heart J 2000; 21: 1152-8.
68. Almagor M, Keren A, Banai S. Increased C-reactive protein level after coronary stent implantation in patients with stable coronary artery disease. Am Heart J 2003; 145: 248-53.
69. Lincoff AM, Kereiakes DJ, Mascelli MA, Deckelbaum LI, Barnathan ES, Patel KK, et al. Abciximab suppresses the rise in levels of circulating inflammatory markers after percutaneous coronary revascularization. Circulation 2001; 104: 163-7.
70. Merino Otermin A, Artaiz Urdaci M, Bergada Garcia J, Riera Sagrera M, Vidal Salva B, Rodriguez Fernandez A. Eptifibatide blocks the increase in C-reactive protein concentration after coronary angioplasty. Rev Esp Cardiol 2002; 55: 186-9.
71. 33 amino acid polymorphism in membrane glycoprotein IIIa, and are distinguishable by DNA typing. J Clin Invest 1989; 83: 1778-881.
72. Kim HO, Jin Y, Kickler TS, Blakemore K, Kwon OH, Bray PF. Gene frequencies of the five major human platelet antigens in African American, white, and Korean populations. Transfusion 1995; 35: 863-7.
73. A2 polymorphism of the platelet IIb/IIIa receptor: increased risk of early recurrent ischaemic events in acute coronary syndromes, increased platelet aggregability, and effective platelet inhibition by an oral IIb/IIIa inhibitor: results from TIMI 12. Circulation 1998; 98 (Suppl. I): I-171.
74. Cannon CP, McCabe CH, Wilcox RG, Langer A, Caspi A, Berink P, et al. Oral glycoprotein IIb/IIIa inhibition with orbofiban in patients with unstable coronary syndromes (OPUS-TIMI 16) trial. Circulation 2000; 102: 149-56.
75. O'Connor FF, Shields DC, Fitzgerald A, Cannon CP, Braunwald E, Fitzgerald DJ. Genetic variation in glycoprotein IIb/IIIa (GPIIb/IIIa) as a determinant of the responses to an oral GPIIb/IIIa antagonist in patients with unstable coronary syndromes. Blood 2001; 98: 3256-60.
76. 3-integrins in platelets. Blood 2001; 97: 3093-9.
77. Jackson DY. Alpha 4 integrin antagonists. Curr Pharm Design 2002; 8(14): 1229-53.
78. Mousa SA. Antiplatelet therapies: platelet GPIIb/IIIa antagonists and beyond. Curr Pharm Design 2003; 9(28): 2317-22.
79. Windecker S, Roffi M. and Meier B. Sirolimus eluting stent: a new era in interventional cardiology? Curr Pharm Design 2003; 9(13): 1077-94.