Tirofiban (Aggrastat®)

1999; Wiley; Volume: 17; Issue: 3 Linguagem: Indonésio

10.1111/j.1527-3466.1999.tb00015.x

ISSN

1527-3466

Autores

Jacquelynn J. Cook, Bohumil Bednár̂, Joseph J. Lynch, Robert J. Gould, Melissa S. Egbertson, Wasyl Halczenko, Mark E. Duggan, George D. Hartman, Man‐Wai Lo, Gail Murphy, Lawrence I. Deckelbaum, Frederick L. Sax, Eliav Barr,

Tópico(s)

Acute Myocardial Infarction Research

Resumo

Cardiovascular Drug ReviewsVolume 17, Issue 3 p. 199-224 Free Access Tirofiban (Aggrastat®) Jacquelynn J. Cook, Corresponding Author Jacquelynn J. Cook Merck Research Laboratories, West Point, PA, USAAddress correspondence and reprint requests to Jacquelynn J. Cook, WP46-300, Merck Research Laboratories, West Point, PA, USA 19486. FAX: (215)-652-3811;E-mail: jacquelynn-cook@merck.com.Search for more papers by this authorBohumil Bednar, Bohumil Bednar Merck Research Laboratories, West Point, PA, USASearch for more papers by this authorJoseph J. Lynch Jr., Joseph J. Lynch Jr. Merck Research Laboratories, West Point, PA, USASearch for more papers by this authorRobert J. Gould, Robert J. Gould Merck Research Laboratories, West Point, PA, USASearch for more papers by this authorMelissa S. Egbertson, Melissa S. Egbertson Merck Research Laboratories, West Point, PA, USASearch for more papers by this authorWasyl Halczenko, Wasyl Halczenko Merck Research Laboratories, West Point, PA, USASearch for more papers by this authorMark E. Duggan, Mark E. Duggan Merck Research Laboratories, West Point, PA, USASearch for more papers by this authorGeorge D. Hartman, George D. Hartman Merck Research Laboratories, West Point, PA, USASearch for more papers by this authorMan-Wai Lo, Man-Wai Lo Merck Research Laboratories, West Point, PA, USASearch for more papers by this authorGail M. Murphy, Gail M. Murphy Merck Research Laboratories, West Point, PA, USASearch for more papers by this authorLawrence I. Deckelbaum, Lawrence I. Deckelbaum Merck Research Laboratories, West Point, PA, USASearch for more papers by this authorFrederick L. Sax, Frederick L. Sax Merck Research Laboratories, West Point, PA, USASearch for more papers by this authorEliav Barr, Eliav Barr Merck Research Laboratories, West Point, PA, USASearch for more papers by this author Jacquelynn J. Cook, Corresponding Author Jacquelynn J. Cook Merck Research Laboratories, West Point, PA, USAAddress correspondence and reprint requests to Jacquelynn J. Cook, WP46-300, Merck Research Laboratories, West Point, PA, USA 19486. FAX: (215)-652-3811;E-mail: jacquelynn-cook@merck.com.Search for more papers by this authorBohumil Bednar, Bohumil Bednar Merck Research Laboratories, West Point, PA, USASearch for more papers by this authorJoseph J. Lynch Jr., Joseph J. Lynch Jr. Merck Research Laboratories, West Point, PA, USASearch for more papers by this authorRobert J. Gould, Robert J. Gould Merck Research Laboratories, West Point, PA, USASearch for more papers by this authorMelissa S. Egbertson, Melissa S. Egbertson Merck Research Laboratories, West Point, PA, USASearch for more papers by this authorWasyl Halczenko, Wasyl Halczenko Merck Research Laboratories, West Point, PA, USASearch for more papers by this authorMark E. Duggan, Mark E. Duggan Merck Research Laboratories, West Point, PA, USASearch for more papers by this authorGeorge D. Hartman, George D. Hartman Merck Research Laboratories, West Point, PA, USASearch for more papers by this authorMan-Wai Lo, Man-Wai Lo Merck Research Laboratories, West Point, PA, USASearch for more papers by this authorGail M. Murphy, Gail M. Murphy Merck Research Laboratories, West Point, PA, USASearch for more papers by this authorLawrence I. Deckelbaum, Lawrence I. Deckelbaum Merck Research Laboratories, West Point, PA, USASearch for more papers by this authorFrederick L. Sax, Frederick L. Sax Merck Research Laboratories, West Point, PA, USASearch for more papers by this authorEliav Barr, Eliav Barr Merck Research Laboratories, West Point, PA, USASearch for more papers by this author First published: 07 June 2006 https://doi.org/10.1111/j.1527-3466.1999.tb00015.xCitations: 35AboutPDF ToolsRequest permissionExport citationAdd to favoritesTrack citation ShareShare Give accessShare full text accessShare full-text accessPlease review our Terms and Conditions of Use and check box below to share full-text version of article.I have read and accept the Wiley Online Library Terms and Conditions of UseShareable LinkUse the link below to share a full-text version of this article with your friends and colleagues. Learn more.Copy URL Share a linkShare onFacebookTwitterLinkedInRedditWechat References 1 Adgey AAJ. An overview of the results of clinical trials with glycoprotein IIb/IIIa inhibitors. Eur Heart J 1998; 19: D10– D21. 2 AGGRASTAT (tirofiban hydrochloride) product circular. In: Physician's desk reference 1999. Montvale , NJ : Medical Economics Company, Inc, 1999: 1721– 1725. 3 Ambrose JA, Weinrach M. Thrombosis in ischemic heart disease. Arch Intern Med 1996; 156: 1382– 1394. 4 Antiplatelet Trialists' Collaboration. Collaborative overview of randomized trials of antiplatelet therapy. I. Prevention of death, myocardial infarction, and stroke by prolonged antiplatelet therapy in various categories of patients. BMJ 1994; 308: 81– 106. 5 Barrett JS, Murphy G, Peerlinck K, et al. Pharmacokinetics and pharmacodynamics of MK-383, a selective non-peptide platelet glycoprotein IIb/IIIa receptor antagonist, in healthy men. Clin Pharmacol Ther 1994; 56: 377– 388. 6 Bednar B, Cook JJ, Holahan MA, et al. Fibrinogen receptor antagonist-induced thrombocytopenia in chimpanzee and rhesus monkey associated with preexisting drug-dependent antibodies to platelet glycoprotein IIb/IIIa. Blood 1999; 94: 587– 599. 7 Bednar B, Cunningham ME, McQueney PA, et al. Flow cytometric measurement of kinetic and equilibrium binding parameters of arginine-glycine-aspartic acid ligands in binding to glycoprotein IIb/IIIa on platelets. Cytometry 1997; 28: 58– 65. 8 Bednar RA, Gaul SL, Hamill TG, et al. Identification of low molecular weight GPIIb/IIIa antagonists that bind preferentially to activated platelets. J Pharmacol Exp Ther 1998; 285: 1317– 1326. 9 Bovill EG, Terrin ML, Stump DC, et al. Hemorrhagic events during therapy with recombinant tissue-type plasminogen activator, heparin, and aspirin for acute myocardial infarction. Results of the thrombolysis in myocardial infarction (TIMI) phase II trial. Ann Intern Med 1991; 115: 256– 265. 10 Braunwald E, Jones RH, Mark DB, et al. Diagnosing and managing unstable angina. Circulation 1994; 90: 613– 622. 11 Burke AP, Farb A, Malcom GT, et al. Coronary risk factors and plaque morphology in men with coronary disease who died suddenly. N Engl J Med 1997; 336: 1276– 1282. 12 Calvete JJ. Clues for understanding the structure and function of a prototypic human integrin: the platelet glycoprotein IIb/IIIa complex. Thromb Haemost 1994; 72: 1– 15. 13 Cohen M, Demers C, Gurfinkle EP, et al, for the Efficacy and Safety of Subcutaneous Enoxaparin in Non-Q-Wave Coronary Events Study Group. A comparison of low molecular weight heparin with unfractionated heparin for unstable coronary artery disease. N Engl J Med 1997; 337: 447– 452. 14 Cook NS, Bruttger O, Pally C, Hagenbach A. The effects of two synthetic glycoprotein IIb/IIIa antagonists, Ro 43-8857 and L-700,462, on platelet aggregation and bleeding in guinea pigs and dogs: evidence that Ro 43-8857 is orally active. Thromb Haemost 1993; 70: 838– 847. 15 Curtis BR, McFarland JG, Wu G-G, Visentin GP, Aster RH. Antibodies in sulfonamide-induced immune thrombocytopenia recognize calcium-dependent epitopes on the glycoprotein IIb/IIIa complex. Blood 1994; 84: 176– 183. 16 DeFeyter PJ, Ruygrok PN. Antiplatelet, antithrombotic, and lytic therapy for unstable angina, and the appropriate role of revascularization. Curr Opin Cardiol 1995; 10: 389– 398. 17 Egbertson MS, Bednar B, Bednar RA, et al. Nonpeptide glycoprotein IIb/IIIa inhibitors. 9. Centrally constrained alpha-sulfonamides are useful tools for exploring platelet function. Bioorg Med Chem Lett 1996; 6: 1415– 1420. 18 Egbertson MS, Chang CT-C, Duggan ME, et al. Non-peptide fibrinogen receptor antagonists. 2. Optimization of a tyrosine template as a mimic for Arg–Gly–Asp. J Med Chem 1994; 37: 2537– 2551. 19 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– 961. 20 Ferguson JJ, Waly HM, Wilson JM. Fundamentals of coagulation and glycoprotein IIb/IIIa receptor inhibition. Eur Heart J 1998; 19: D3– D9. 21 Frelinger AF, Cohen I, Smith MA, Roberts J, Lam ST-C, Ginsberg MH. Selective inhibition of integrin function by antibodies specific for ligand-occupied receptor conformers. J Biol Chem 1990; 265: 6346– 6352. 22 Frelinger AF, Lam ST-C, Plow EF, Smith MA, Loftus JC, Ginsberg MH. Occupancy of an adhesive glycoprotein receptor modulates expression of an antigenic site involved in cell adhesion. J Biol Chem 1988; 263: 12397– 12402. 23 Fuster V, Badimon L, Badimon JJ, Chesebro JH. The pathogenesis of coronary artery disease and the acute coronary syndromes (Part 1). N Engl J Med 1992; 326: 242– 250. 24 Fuster V, Badimon L, Badimon JJ, Chesebro JH. The pathogenesis of coronary artery disease and the acute coronary syndromes (Part 2). N Engl J Med 1992; 326: 310– 318. 25 Fuster V, Dyken ML, Vokonas PS, et al. Aspirin as a therapeutic agent in cardiovascular disease. Circulation 1993; 87: 659– 675. 26 Gould RJ, Chang CT-C, Lynch RJ, et al. MK-0383 is a potent non-peptide mimic of RGD that inhibits glycoprotein IIb/IIIa. (Abstract). Thromb Haemost 1993; 69: 976. 27 Gould R, Davidson J, Siegl P, et al. MK-0383, a novel IIb/IIIa fibrinogen receptor antagonist, prevents occlusive thrombus formation in an aspirin-resistant baboon model of vascular graft thrombosis. FASEB J 1993; 7: A209. 28 Gould RJ, Lynch JJ, Schaffer L, et al. MK-0383, a non-peptide fibrinogen receptor antagonist, prevents thrombosis in canine and primate models. (Abstract). Thromb Haemost 1993; 69: 539. 29 Hartman GD, Egbertson MS, Halczenko W, et al. Non-peptide fibrinogen receptor antagonists. 1. Discovery and design of exosite inhibitors. J Med Chem 1992; 35: 4640– 4642. 30 Hiramatsu Y, Gikakis N, Anderson HL, et al. Tirofiban provides "platelet anesthesia" during cardiopulmonary bypass in baboons. J Thorac Cardiovasc Surg 1997; 113: 182– 193. 31 Hoki S, Umemura K, Kondo K, Ikeda Y, Suzuki Y, Nakashima M. Inhibitory effect of T-250, a novel GPIIb/IIIa antagonist, in the guinea pig thrombosis model, compared with tirofiban. (Abstract). Jpn J Pharmacol 1998; 76: 182P. 32 Honda S, Yomiyama Y, Pellitier AJ, et al. Topography of ligand-induced binding sites, including a novel cation-sensitive epitope (AP5) at the amino terminus, of the human integrin β3 subunit. J Biol Chem 1995; 270: 11947– 11954. 33 Kereiakes DJ, Kleiman NS, Ambrose J, et al. Randomized, double-blind, placebo-controlled dose-ranging study of tirofiban (MK-383) platelet IIb/IIIa blockade in high risk patients undergoing coronary angioplasty. J Am Coll Cardiol 1996; 27: 536– 542. 34 Keularts IMLW, Beguin S, de Zwaan C, Hemker HC. Treatment with a GPIIb/IIIa antagonist inhibits thrombin generation in platelet rich plasma from patients. Thromb Haemost 1998; 80: 370– 371. 35 Kong DF, Califf RM, Miller DP, et al. Clinical outcomes of therapeutic agents that block the platelet glycoprotein IIb/IIIa integrin in ischemic heart disease. Circulation 1998; 98: 2829– 2835. 36 Kouns WC, Wall DC, White MM, Fox CF, Jennings LK. A conformation-dependent epitope of human platelet glycoprotein IIIa. J Biol Chem 1990; 265: 20594– 20604. 37 Lynch JJ, Cook JJ, Sitko GR, et al. Non-peptide glycoprotein IIb/IIIa inhibitors. 5. Antithrombotic effects of MK-0383. J Pharmacol Exp Ther 1995; 272: 20– 32. 38 Mark DB, Talley D, Topol EJ, et al. Economic assessment of platelet glycoprotein IIb/IIIa inhibition for prevention of ischemic complications of high-risk coronary angioplasty. Circulation 1996; 94: 629– 635. 39 McQueney PA, Bollag DM, Hartman GD, Gould RJ, Bednar B. Characterization of ligand binding sites on GPIIb/IIIa upon binding of GPIIb/IIIa antagonists using monoclonal antibodies. Circulation 1996; 94: 1– 99. 40 Merck Research Laboratories clinical study report—protocol 005. West Point , PA : Merck Research Laboratories, 1996. 41 Merck Research Laboratories clinical study report—protocol 008. West Point , PA : Merck Research Laboratories, 1996. 42 Merck Research Laboratories clinical study report—protocol 009. West Point , PA : Merck Research Laboratories, 1997. 43 Merck Research Laboratories clinical study report—protocol 014. West Point , PA : Merck Research Laboratories, 1997. 44 Nable S, Peters DH, Goa KL. Enoxaparin: a reappraisal of its pharmacology and clinical applications in the prevention and treatment of thromboembolic disease. Drugs 1995; 49: 388– 401. 45 Nobiletti J, Morse EE, Sophia P, Kiraly T, Azrin M. Inhibition of platelet aggregation and release in vitro by GP IIb/IIIa receptor antagonists. Circulation 1997; 96: 1– 721. 46 Pedicord DL, Thomas BE, Mousa SA, Dicker IB. Glycoprotein IIb/IIIa receptor antagonists inhibit the development of platelet procoagulant activity. Thromb Res 1998; 90: 247– 258. 47 Peerlinck K, De Lepeleire I, Goldberg M, et al. MK-0383 (L-700,462), a selective non-peptide platelet glycoprotein IIb/IIIa antagonist, is active in man. Circulation 1993; 88: 1512– 1517. 48 Phillips DR, Charo IF, Parise LV, Fitzgerald LA. The platelet membrane glycoprotein IIb/IIIa complex. Blood 1988; 71: 831– 843. 49 Rao AK, Sun L, Hiramatsu Y, et al. Glycoprotein IIb/IIIa antagonist tirofiban (Aggrastat) inhibits thrombin generation during cardiopulmonary bypass in baboons. Thromb Haemost Abstr Suppl 1997; 78: 578. 50 Reverter JC, Beguin S, Kessels H, Kumar R, Hemker HC, Coller BS. Inhibition of platelet mediated, tissue-induced thrombin generation by mouse/human chimeric 7E3 antibody. Potential implications for the effect of c7E3 treatment on acute thrombosis and "clinical restenosis." J Clin Invest 1996; 98: 863– 874. 51 Ross R. The pathogenesis of atherosclerosis: a perspective for the 1990s. Nature 1993; 362: 801– 809. 52 The EPILOG Investigators. Platelet glycoprotein IIb/IIIa receptor blockade and low-dose heparin during percutaneous coronary revascularization. N Engl J Med 1997; 336: 1689– 1696. 53 The Platelet Receptor Inhibition in Ischemic Syndrome Management (PRISM) Study Investigators. A comparison of aspirin plus tirofiban with aspirin plus heparin for unstable angina. N Engl J Med 1998; 338: 1498– 1505. 54 The Platelet Receptor Inhibition in Ischémie Syndrome Management in Patients Limited by Unstable Signs and Symptoms (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– 1497. 55 The RESTORE Investigators. 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– 1453. 56 The RESTORE Investigators. Six month angiographie and clinical folllow-up of patients prospectively randomized to either tirofiban or placebo during angioplasty in the RESTORE trial. J Am Coll Cardiol 1998; 32: 28– 34. 57 Topol EJ. Novel antithrombotic approaches to coronary artery disease. Am J Cardiol 1995; 75: 27B– 33B. 58 Topol EJ, Byzova TV, Plow EF. Platelet GPIIb/IIIa blockers. Lancet 1999; 353: 227– 231. 59 Weitz JI. Low molecular weight heparins. N Engl J Med 1997; 337: 688– 698. 60 White BP, Sumner MJ, Pike NB, Lumley P. Antithrombotic efficacy of fibrinogen receptor (GPIIb/IIIa) antagonists in a canine coronary thrombosis model: relation to bleeding. (Abstract). Thromb Haemost 1995; 73: 1339. 61 Xiao Z, Theroux P, Lu Y, Ghitescu M, Frojmovic MM. Modulation of platelet neutrophil interaction with pharmacological inhibition of fibrinogen binding to platelet GPIIb/IIIa receptor. J Am Coll Cardiol 1997; 29: 154A. Citing Literature Volume17, Issue3September 1999Pages 199-224 ReferencesRelatedInformation

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