Oral antiplatelet, antithrombotic efficacy of DMP 728, a novel platelet GPIIb/IIIa antagonist

Circulation

Volumn 93, Issue 3, 1996, Pages 537-543

  Mousa, Shaker A ^a   DeGrado, William F ^a   Mu, Dun Xu ^a   Kapil, Ram P ^a   Lucchesi, Benedict R ^a   Reilly, Thomas M ^a  

^a DUPONT COMPANY   (United States)

Author keywords

platelet aggregation inhibitors; receptor antagonists; thrombosis

Indexed keywords

ACETYLSALICYLIC ACID; ANTITHROMBOCYTIC AGENT; CYCLO(DEXTRO 2 AMINOBUTYRYL 2 N METHYLARGINYLGLYCYLASPARTYL 3 AMINOMETHYLBENZOIC ACID) METHANESULFONATE; FIBRINOGEN RECEPTOR; TICLOPIDINE;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTERY THROMBOSIS; ARTICLE; BLEEDING TIME; CAROTID ARTERY THROMBOSIS; CORONARY ARTERY THROMBOSIS; DOG; DOSE RESPONSE; INTRAVENOUS DRUG ADMINISTRATION; NONHUMAN; ORAL DRUG ADMINISTRATION; PRIORITY JOURNAL; THROMBOCYTE AGGREGATION INHIBITION; THROMBOEMBOLISM; THROMBOSIS;

EID: 0030045279     PISSN: 00097322     EISSN: None     Source Type: Journal    
DOI: 10.1161/01.CIR.93.3.537     Document Type: Article

References (33)

1. Pytela R, Pierschbacher MS, Ginsberg MH, Plow EF, Ruoslahti E. Platelet membrane glycoprotein IIb/IIIa: member of a family of RGD specific adhesion receptors. Science. 1986;231:1559-1562.
2. Philips DR, Charo IF, Scarborough RM. GPIIb/IIIa: the responsive integrin. Cell. 1991;65:359-362.
3. D'Souza SE, Ginsberg MH, Burke TA, Plow EF. The ligand binding site of the platelet integrin receptor GPIIb-IIIa is proximal to the second calcium binding domain of its a subunit. J Biol Chem. 1990;265:3440-3446.
4. Hirsh PD, Hillis LD, Campbell WB, Firth BG, Willerson JT. Release of prostaglandins and thromboxane into the coronary circulation in patients with ischemic heart disease. N Engl J Med. 1981; 304:685-691.
5. Rubenstein MD, Wall RT, Bain DS, Harrison DC. Platelet activation in clinical coronary artery disease and spasm. Am Heart J. 1981;102:363-367.
6. Smitherman TC, Milam M, Woo J, Willerson JT, Frenkel EP. Elevated beta thromboglobulin in peripheral venous blood of patients with acute myocardial ischemia: direct evidence for enhanced platelet reactivity in vivo. Am J Cardiol. 1981;48:395-402.
7. Fitzgerald DJ, Roy L, Catella F, Fitzgerald GA. Platelet activation in unstable coronary disease. N Engl J Med. 1986;315:983-989.
8. Fuster V, Steele PM, Chesebro JH. Role of platelets and thrombosis in coronary atherosclerotic disease and sudden death. J Am Coll Cardiol. 1985;5:175B-184B.
9. Willerson JT, Golino P, Eidt J, Campbell WB, Buja LM. Specific platelet mediators and unstable coronary artery lesions: experimental evidence and potential clinical implications. Circulation. 1989;81:198-205.
10. Davies MJ, Thomas AC. Plaque fissuring - the cause of acute myocardial infarction, sudden ischemic death, and cresendo angina. Br Heart J. 1985;53:363-373.
11. Hamm CW, Bliefield W, Kupper W, Lorenz RL, Weber PC, Wober W. Biochemical evidence of platelet activation in patients with persistent unstable angina. J Am Coll Cardiol. 1987;10:998-1004.
12. Coller BS, Folts JD, Scudder LE, Smith SR. Antithrombotic effect of a monoclonal antibody to the platelet glycoprotein IIb/IIIa receptor in an experimental animal model. Blood. 1986;68:783-786.
13. Gold HK, Gimple LW, Yasuda T, Leinbach RC, Werner W, Holt R, Jordon R, Berger H, Collen D, Coller BS. Pharmacodynamic study of F(ab′)2 fragments of murine monoclonal antibody 7E3 directed against human platelet glycoprotein IIb/IIIa in patients with unstable angina pectoris. J Clin Invest. 1990;86:651-659.
14. Ruggeri ZM, Houghton RA, Russel SR, Zimmerman TS. Inhibition of platelet function with synthetic peptide designed to be a high affinity antagonist of fibrinogen binding to platelets. Proc Natl Acad Sci USA. 1986;83:5708-5712.
15. Nicholson NS, Panzer-Knodle SG, Salyers AK, Taite BB, King LW, Miyano M, Gorczynski RJ, Williams MH, Zupec ME, Tjoenge FS. In vitro and in vivo effects of a peptide mimetic (SC-47643) of RGD as an antiplatelet and antithrombotic agent. Thromb Res. 1991;62:567-578.
16. Nichols AJ, Ruffolo RR, Huffman WF, Poste G, Samanen J. Development of GPIIb/IIIa antagonists as antithrombotic drugs. Trends Pharmacol Sci. 1992;13:413-417.
17. Theroux P, White H, David D, Van de Werf F, Nienaber CA, Charbonnier B, Erhardt L, Gill J, Hillis WS, Jennings G, Tam L-B, Deschenes N, Fitzpatrick V, Sax FL. A heparin-controlled study of MK383 in unstable angina. Circulation. 1994;90:1231-1242.
18. Austel V, Himmelsbach F, Muller T. Non-peptide fibrinogen antagonists. Drugs Future. 1994;19:757-769.
19. Shebuski RJ, Berry DE, Bennett DB, Romoff T, Storer BL, Ali F, Samanen J. Demonstration of Ac-Arg-Gly-Asp-Ser-NH2 as an antiaggregatory agent in the dog by intracoronary administration. Thromb Haemost. 1989;61:183-188.
20. Ashby B, Daniel JL, Smith JB. Mechanisms of platelet activation and inhibition. Platelets Health Dis. 1990;4:1-26.
21. Chesebro JH, Knatterud G, Roberts R, Borer J, Cohen LS, Dalen J, Dodge HT, Francis CK, Hillis D, Ludbrook P, Markis JE, Muller H, Passamani ER, Power ER, Rao AK, Robertson T, Ross A, Ryan TJ, Sobel BE, Willerson J, Williams DO, Zaret BL, Braunwald E. Thrombolysis in Myocardial Infarction (TIMI) trial, phase I: a comparison between intravenous tissue plasminogen activator and intravenous streptokinase. Circulation. 1987;76:142-154.
22. Golino P, Ashton JH, Glas-Greenwalt P, McNatt J, Buja LM, Willerson JT. Mediation of reocclusion by thromboxane A2 and serotonin after thrombolysis with t-PA in a canine preparation of coronary thrombosis. Circulation. 1988;77:678-684.
23. John JA, Gold HK, Leinbach RC, Yasuda T, Gimple LW, Werner W, Finkelstein D, Newell J, Ziskind AA, Collen D. Prevention of coronary artery reocclusion and reduction in late coronary artery stenosis after thrombolytic therapy in patients with acute myocardial infarction. Circulation. 1988;78:546-556.
24. Weller T, Alig L, Muller MH, Kouns WC, Steiner B. Fibrinogen receptor antagonists - a novel class of promising antithrombotics. Drues Future. 1994;19:461-476.
25. Nicholson NS, Panzer-Knodle SG, Salyers AK, Taite BB, Szalony JA, Haas NF, King LW, Zablocki JA, Keller BT, Broschat K, Engleman VW, Herin M, Jacqmin P, Feigen LP. SC-5468A: an orally active inhibitor of platelet aggregation. Circulation. 1995;91: 403-410
26. Mousa SA, Flint S, Lorelli W, Hassell S, Bozarth JM, DeGrado WF Reilly TM. Intravenous antiplatelet efficacy and safety of the platelet GPIIb/IIIa receptor antagonists, DMP728 in anesthetized dogs. Thromb Res. 1994;76:109-119.
27. Wu ST, Stampfli HF, Banks CM, Emm TA, Kapil RP, Padovani PK Lee WM, Huang S-M. Determination of DMP 728, a IIb/IIIa receptor antagonist, in rat and dog plasma by high-performance liquid chromatography with ftuorimetric method. J Chromatogr Sci. 1994;657:254-260.
28. Folts JD. Experimental arterial platelet thrombosis, platelet inhibitors, and their possible clinical relevance. Cardiovasc Rev Rep. 1982;3:370-382.
29. Folts JD, Gallagher K, Rowe GG. Blood flow reduction in stenosed coronary arteries: vasospasm or platelet aggregation? Circulation. 1982;65:248-255.
30. Romson JL, Haack DW, Lucchesi BR. Electrical induction of coronary artery thrombosis in the ambulatory canine: a model for in vivo evaluation of antithrombotic agents. Thromb Res. 1980;17: 841-853.
31. Mickelson JK, Simpson PJ, Cronin M, Homeister JW, Laywell E, Kitzen J, Lucchesi BR. Antiplatelet antibody [7E3 F(ab′)2] prevents rethrombosis after recombinant tissue-plasminogen activator-induced coronary thrombolysis in a canine model. Circulation. 1990;81:617-627.
32. Mousa SA, Bozarth JM, Forsythe MS, Lorelli W, Ramachandran N, Jackson S, De Grado W, Reilly TM. Antiplatelet efficacy and specificity of DMP 728, a novel platelet GPIIb/IIIa receptor antagonist. Cardiology. 1993;83:374-382.
33. Mousa SA, Bozarth JM, Forsythe MS, Jackson SM, Leamy A, Diemer MM, Kapil RP, Knabb RM, Mayo MC, Pierce SK, DeGrado WF, Thoolen MJ, Reilly TM. Antiplatelet and antithrombotic efficacy of DMP 728, a novel platelet GPIIb/IIIa receptor antagonist. Circulation. 1994;89:3-12.