Antiplatelet efficacy of xv459, a novel nonpeptide platelet gpiib/llla antagonist: comparative Platelet Binding Profiles with c7E3

Journal of Pharmacology and Experimental Therapeutics

Volumn 286, Issue 3, 1998, Pages 1277-1284

  Mousa, Shaker A ^a   Bozarth, Jeffrey M ^a   Lorelli, William ^a   Forsythe, Mark S ^a   Thoolen, Martin J M C ^a   Slee, Andrew M ^a   Reilly, Thomas M ^a   Friedman, Paul A ^a  

^a DUPONT COMPANY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3 [[[3 [4 (AMINOIMINOMETHYL)PHENYL] 4,5 DIHYDRO 5 ISOXAZOLYL]ACETYL]AMINO] N (BUTOXYCARBONYL)ALANINE; ABCIXIMAB; ANTITHROMBOCYTIC AGENT; CYCLO(DEXTRO 2 AMINOBUTYRYL 2 N METHYLARGINYLGLYCYLASPARTYL 3 AMINOMETHYLBENZOIC ACID) METHANESULFONATE; EPTIFIBATIDE; FIBRINOGEN RECEPTOR; ROXIFIBAN; TIROFIBAN; UNCLASSIFIED DRUG; AMINO ACID; FIBRINOGEN; ISOXAZOLE DERIVATIVE; MONOCLONAL ANTIBODY;

ARTICLE; BABOON; BINDING AFFINITY; BINDING KINETICS; CONTROLLED STUDY; DOG; DRUG EFFICACY; DRUG MECHANISM; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; DRUG SOLUBILITY; DRUG SPECIFICITY; DRUG STRUCTURE; HUMAN; NONHUMAN; PRIORITY JOURNAL; RECEPTOR OCCUPANCY; SWINE; THROMBOCYTE ADHESION; THROMBOCYTE AGGREGATION INHIBITION; ANIMAL; COMPARATIVE STUDY; DRUG ANTAGONISM; DRUG EFFECT; IMMUNOLOGY; METABOLISM; PAPIO; THROMBOCYTE; THROMBOCYTE AGGREGATION;

AMINO ACIDS; ANIMALS; ANTIBODIES, MONOCLONAL; BLOOD PLATELETS; DOGS; FIBRINOGEN; HUMANS; ISOXAZOLES; PAPIO; PLATELET AGGREGATION; PLATELET AGGREGATION INHIBITORS; PLATELET GLYCOPROTEIN GPIIB-IIIA COMPLEX;

EID: 0032160611     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (41)

1. Ashby B, Daniel JL and Smith JB (1990) Mechanisms of platelet activation and inhibition. Platelet In Health & Disease 4(l):l-26.
2. Bennett JS, Vilaire GO (1979) Exposure of platelet fibrinogen receptors by ADP and epinephrine. J Clin Invest 64:1393-1401.
3. Coller BS (1985) A new marine monoclonal antibody reports an activation-dependent change in the conformation and/or microenvironment of the platelet GPIIbAIIa complex. J Clin Invest 76:101-108.
4. Coller BS, Folts JD, Scudder LE, Smith SR (1986) Antithrombotic effect of a monoclonal antibody to the platelet glycoprotein Ilb/IIIa receptor in an experimental animal model. Blood 68:783-786.
5. Cook NS, Kottirsch G, Zerwes H-G (1994) Platelet glycoprotein Ilb/IIIa antagonists. Drugs of the Future 19:135-159.
6. Davies MJ (1990) A macro and micro view of coronary vascular insult in ischémie heart disease. Circulation 82:suppl II, 1138-1146.
7. Davies MJ, Thomas AC (1985) Plaque fissuring-the cause of acute myocardial infarction, sudden ischémie death, and cresendo angina. Br Heart J 53:363-373.
8. D'Souza SE, Ginsberg MH, Burke TA, Plow EF (1990) The ligand binding site of the platelet I integrin receptor GPIIb/IIIa is proximal to the second calcium binding domain of its a subunit. Biol Chem 265:3440-3446.
9. The EPIC Investigators (1994) Use of a monoclonal antibody directed against the glycoprotein Ilb/IIIa receptor in high-risk coronary angioplasty. N Engl J Med 330:956-961.
10. Fitzgerald DJ, Roy L, Catella F, Fitzgerald GA (1986) Platelet activation in unstable coronary disease. N Eng J Med 315:983-989.
11. Fuster V (1994) Mechanisms leading to myocardial infarction: Insights from studies of vascular biology. Circulation 90:2126-2148.
12. Fuster V, Steele PM, Chesebro JH (1985) Role of platelets and thrombosis in coronary atherosclerotic disease and sudden death. J Am Coll Cardiol 5:175B184B.
13. Hamm CW, Bliefield W, Kupper W, Lorenz RL, Weber PC, Wober W (1987) Biochemical evidence of platelet activation in patients with persistent unstable angina. J Am Coll Cardiol 10:998-1004.
14. Heiman NS, Ohman EM, Califf RM, George BS, Kereiakes D, Aguirre FV, Weisman H, Schaible T, Topol EJ (1993) Profound inhibition of platelet aggregation with monoclonal antibody c7E3 after thrombolytic therapy: Results of the thrombolysis and angioplasty in myocardial infarction (TAMI) 8 pilot study. J Am Coll Cardiol 22:381-389.
15. Kottke-Marchant K, Simpfendorfer C, Lowrie M, Burns D, Anders RJ (1995) Sustained but variable inhibition of platelet aggregation with Xemlofiban, an oral GPIIb/IIIa receptor antagonist, in patients with unstable angina. Circulation 92:(8 Suppl.):! 488.
16. Kruithof EKO, Tran-Thang C, Bachman F (1986) Studies on the release of a plasminogen activator inhibitor by human platelets. Thromb Haemostas 55:201-205.
17. Mousa S, Bozarth J, Forsythe M, Jackson S, Leamy A, Diemer M, Kapil, Knabb R, Mayo M, Pierce S, De Grado W, Thoolen M, Reilly T (1994) Antiplatelet, antithrombotic efficacy of DMP 728, a novel platelet GPIIb/IIIa receptor antagonist. Circulation 89:3-12.
18. Mousa S, Bozarth J, Forsythe M, Lorelli W, Jackson S, Ramachandran N, De Grado W, Thoolen M, Reilly T (1993) Antiplatelet efficacy and specificity of a novel platelet GPIIb/IIIa receptor antagonist, DMP728. Cardiology 83 (5-6):374-382.
19. Mousa S and Reilly TM (1995) Antiplatelet effects of direct thrombin inhibitors us. GPIIb/IIIa receptor antagonists: Comparative analysis, in Cardiovascular Disease: Cellular & Molecular Mechanisms, Prevention, Treatment, (Gallo LL ed) Plenum Press, New York, pp 255-267.
20. Mousa SA, Bennett JS (1996) Platelets in health and disease: Platelet GPIIb/IHa structure and function: Recent advances in antiplatelet therapy. Drugs of the future 21(11):1141-1154.
21. Mousa SA, Forsythe M, Lorelli W, Bozarth J, Xue C-B, Wityak J, Sielecki TM, Olson R, Degrade W, Kapil R, Hussain M, Wexler R, Thoolen M, Reilly TM (1996) Novel nonpeptide antiplatelet GPIIb/IIIa receptor antagonist, DMP 754: Receptor binding affinity and specificity. Coronary Artery Disease 7(10):767-774.
22. Mousa SA and Topol E (1997) Novel antiplatelet therapies: Recent advances in the development of platelet GPIIb/IIIa receptor antagonists, in Current Review of Interventional Cardiology 3rd ed (Serruys PW and Holmes D eds) pp 114-129, Current Medicine, Philadelphia.
23. Mousa SA, Mu D-X, Reilly T (1997) Intravenous and oral antithrombotic efficacy of a novel nonpeptide antiplatelet GPIIb/IIIa antagonist, DMP 754, as compared to other antiplatelet and anticoagulant strategies (Abstract). Thrombosis Hemostasis, Suppl., 1600:392.
24. Narjes H, Weisenberger H, Muller TH, Deichsel G, Krause J (1995) Tolerability and platelet fibrinogen receptor occupancy (FRO) after oral treatment with BIBU 104 xx in healthy volunteers (Abstract). Thromb Haemostasis 73(6):1592.
25. Nichols AJ, Ruffolo RR, Huffman WF, Poste G, Samanen J (1992) Development of GPIIb/IIIa antagonists as antithrombotic drugs. Trends Pharmacol Sei 13(11): 413-417.
26. O'Neil K, De Grado W, Mousa S, Ramachandran N, Hoess R (1994) Identificatior. of recognition sequences of adhesion molecules using phage display technology. M'dh Enzymol 245:370-386.
27. Peerlinck K, De Lepeleire I, Goldberg M, Farrell D, Barrett J, Hand E, Arnout J, Panebianco D, Deckmyn H, Vermylen J (1993) MK383 (L-700462), a selective nonpeptide platelet glycoprotein Ilb/IIIa antagonist, is active in man. Circulât, on 88, (4 pt 1):1512-1517.
28. Philips DR, Charo IF, Scarborough RM (1991) GPIIb/IIIa: The responsive integrin. Cell 65:359-362.
29. Pytela R, Pierschbacher MS, Ginsberg MH, Plow EF, Ruoslahti E (1986) Platelet membrane glycoprotein Ilb/IIIa: Member of a family of RGD specific adhesion receptors. Science (Wash DC) 231:1559-1562.
30. Rubenstein MD, Wall RT, Bain DS, Harrison DC (1981) Platelet activation in clini ;al coronary artery disease and spasm. Am Heart J 102:363-367.
31. Smitherman TC, Milam M, Woo J, Willerson JT, Frenkel EP (1981) Elevated buta thromboglobulin in peripheral venous blood of patients with acute myocardial ischemia: Direct evidence for enhanced platelet reactivity in vivo. Am J Cardiol 48:395-402.
32. Simoons ML, Jan de Boer M, Van den Brand MJMB, van Miltenburg AJM, Hoorntje JCA, Heyndrickx GR, van der Weiken LR, De Bono D, Rutsch W, Schaible TF, Weisman HF, Klootwijk P, Nijssen KM, Stibbe J, de Feyter PJ, European Cooperative Group. Randomized trial of a GPIIb/IIIa platelet receptor blocker in -efarctory unstable angina. Circulation 89:596-603.
33. Simpfendorfer C, Kottke-Marchant K, Lowrie M, Anders RJ, Burns DM, Miller E'P, Cove CS, DeFranco AC, Ellis SG, Moliterno DJ, Raymond RE, Button JM, Topol .IJ (1997) First chronic platelet glycoprotein Ilb/IIIa integrin blockade: A randomized, placebo-controlled pilot study of Xemilofiban in unstable angina with percutaneous coronary interventions. Circulation 96:76-81.
34. Tcheng JE, Harrington RA, Kottke-Marchant K, Kleiman NS, Ellis SG, Kereiakes DJ, Mick MJ, Navetta FI, Smith JE, Worley SJ, Miller JA, Joseph DM, Sigmon KN, Kitt MM, du Mee CP, Califf RM, Topol EJ (1995) Multicenter, randomized, double-blind, placebo-controlled trial of the platelet integrin glycoprotein Ilb/IIIa blocker Integrilin in elective coronary intervention. IMPACT Investigators. Circulation 91(8):2151-2157.
35. Tcheng JE (1997) Platelet glycoprotein Ilb/IIIa integrin blockade: Recent clinical trials in interventional cardiology. Thrombosis Haemostsis 78(1):205-209.
36. Topol EJ (1995) Novel antithrombotic approaches to coronary artery diseases. Am J Cardiol 75(6):27b-33b.
37. Topol EJ (1997) Targeted approaches to thrombus inhibition: An end to the shotgun approach. Clinical Cardiol 20 (Suppl. I):22-26.
38. Topol EJ and Plow EF (1993) Clinical trials of platelet receptor inhibitors. Thromb Haemost 70:94-98.
39. Willerson JT, Golino P, Eidt J, Campbell WB, Buja LM (1989) Specific platelet mediators and unstable coronary artery lesions. Experimental evidence and potential clinical implications. Circulation 80:198-205.
40. Yasuda T, Gold HK, Yaoita H, Leinbach RC, Guerrero JL, Jang I-K, Holt R, Fallon JT, Collen D (1990) Comparison effects of aspirin, a synthetic thrombin inhibitor and a monoclonal antiplatelet glycoprotein Ilb/IIIa antibody on coronary artery reperfusion, reocclusion and bleeding with recombinant tissue-type plasminogcn activator in a canine preparation. J Am Coll Cardiol 16:714-722.
41. Send reprint requests to: Shaker A. Mousa, Ph.D., MBA, FACC, Du Pont Pharmaceutical Company, Exp. Station, E400/3470, Wilmington, DE 198800400. Email: shaker.a.mousa@dupontpharma.com