DMP 754. Antiplatelet/antithrombotic, glycoprotein IIb/IIIa antagonist

Drugs of the Future

Volumn 23, Issue 7, 1998, Pages 707-711

  Xue, Chu Biao ^a   Mousa, Shaker A ^a  

^a DUPONT COMPANY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANTICOAGULANT AGENT; ANTITHROMBOCYTIC AGENT; EPTIFIBATIDE; FIBRINOGEN RECEPTOR; FIBRINOGEN RECEPTOR ANTAGONIST; LAMIFIBAN; ROXIFIBAN; TIROFIBAN; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BABOON; CAROTID ARTERY THROMBOSIS; CONTROLLED STUDY; CORONARY ARTERY THROMBOSIS; DOG; DOSE TIME EFFECT RELATION; DRUG ABSORPTION; DRUG ELIMINATION; DRUG METABOLISM; DRUG STRUCTURE; DRUG SYNTHESIS; HUMAN; INTRAVENOUS DRUG ADMINISTRATION; NONHUMAN; ORAL DRUG ADMINISTRATION; RHESUS MONKEY; THROMBOCYTE AGGREGATION INHIBITION;

EID: 0031717647     PISSN: 03778282     EISSN: None     Source Type: Journal    
DOI: 10.1358/dof.1998.023.07.463750     Document Type: Article

References (43)

1. Zhang, L.-H., Anzalone, L., Ma, P., Kauffman, G.S., Storace, L. Ward, R. The chiral specific synthesis of DMP 754, a platelet GPIIb/IIIa antagonist. Tetrahedron Lett 1996, 37: 4455-8.
2. Xue, C.-B., Wityak, J., Sielecki, T.M. et al. Discovery of an orally active series of isoxazoline glycoprotein IIIb/IIIa antagonists. J Med Chem 1997, 40: 2064-84.
3. Leonard, E.F., Turitto, V.T., Vroman, L. Blood in contact with natural and artificial surfaces. Ann NY Acad Sci 1987, 516: 1-688.
4. Phillips, D.R., Charo, I.F., Parise, L.V., Fitzgerald, L.A. The platelet membrane glycoprotein IIb/IIIa complex. Blood 1988, 71: 831-43.
5. Ashby, B., Daniel, J.L., Smith, J.B. Mechanisms of platelet activation and inhibition. Platelet Health Dis 1990, 4: 1-26.
6. Nachman, R.L., Leung, L.L.K. Complex formation of platelet membrane glycoproteins IIb and IIIa with fibrinogen. J Clin Invest 1982, 69: 263-9.
7. Ruggeri, Z.M., DeMarlo, L., Garth, L., Boder, R., Montgomery, R.R. Platelets have more than one binding site for von Willebrand factor. J Clin Invest 1983, 72: 1-12.
8. Gardner, J.M., Hynes, H.D. Interaction of fibronectin with its receptor on platelets. Cell 1985, 42: 438-49.
9. Pytela, R.M., Pierschbacher, M.D., Rouslahti, E. A 125/115-kDa cell surface receptor specific for vitronectin interacts with the arginine-glycine-aspartic acid adhesion sequence derived from fibronectin. Proc Natl Acad Sci USA 1985, 82: 5766-70.
10. Cook, N.S., Ubben, D. Fibrinogen as a major risk factor in cardiovascular disease. Trends Pharmacol Sci 1991, 11: 444-51.
11. Davies, M.J., Thomas, A.C. Plaque fissuring - The cause of acute myocardial infarction, sudden ischemic death, and crescendo angina. Brit Heart J 1985, 53: 363-73.
12. Fuster, V., Steele, P.M., Chesebro, J.H. Role of platelets and thrombosis in coronary atherosclerotic disease and sudden death. J Amer Coll Cardiol 1985, 5: 175B-84B.
13. Maseri, A., Chierchia, S., Davies, G. Pathophysiology of coronary occlusion in acute infarction. Circulation 1986, 73: 233-9.
14. Haerem, J.W. Platelet aggregates in intramyocardial vessels in patients dying suddenly and unexpectedly from coronary artery disease. Atherosclerosis 1972, 15: 199-213.
15. Coller, B.S. Platelets and thrombolytic therapy. New Engl J Med 1990, 322: 33-42.
16. Ezratty, A.M., Loscalzo, J. New approaches to antiplatelet therapy. Blood Coagul Fibrinolysis 1991, 2: 317-27.
17. Das, J., Hall, S.E. Platelet aggregation inhibitors. Curr Opin Ther Patent 1991, 1: 221-40.
18. Jakubowski, J.A., Smith, D.F., Sall, D.J. Future antithrombotic therapy. Ann Rep Med Chem 1992, 27: 99-108.
19. Mousa, S.A., Topol, E. Novel antiplatelet therapies: Recent advances in the development of platelet GPIIb/IIIa receptor antagonists. In: Current Review of Interventional Cardiology, Third Edition, P.W. Serruys and D. Holmes (Eds.), Current Medicine, Philadelphia, 1997, 13: 114-29.
20. Philips, D.R., Charo, I.R, Scarborough, R.M. GPIIb/IIIa: The responsive integrin. Cell 1991, 65: 359-62.
21. Pytela, R., Pierschbacher, M.S., Ginsberg, M.H., Plow, E.F., Ruoslahti, E. Platelet membrane glycoprotein IIIb/IIIa: Member of a family of RGD specific adhesion receptors. Science 1986, 231: 1559-62.
22. Ojima, I., Chakravarty, S., Dong, Q. Antithrombotic agents: From RGD to peptide mimetics. Bioorg Med Chem 1995, 3: 337-60.
23. Mousa, S.A., Bennett, J.S. Platelets in health and disease. Platelet GPIIb/IIIa structure and function: Recent advances in antiplatelet therapy. Drugs Fut 1996, 21: 1141-54.
24. Topol, E.J., Plow, E.F. Clinical trials of platelet receptor inhibitors. Thromb Haemost 1993, 70: 94-8.
25. The EPIC Investigators. Use of monoclonal antibody directed against the platelet glycoprotein IIb/IIIa receptor in high-risk coronary angioplasty. New Engl J Med 1994, 330: 956-61.
26. Tcheng, J.E., Harrington, R.A., Kottke-Marchant, K. et al. Multicenter, randomized, double-blind, placebo-controlled trial of the platelet integrin glycoprotein IIb/IIIa blocker integrelin in elective coronary intervention. Circulation 1995, 91: 215-7.
27. Hartman, G.D., Egbertson, M.S., Halczenko, W. et al. Nonpeptide fibrinogen receptor antagonists. 1. Discovery and design of exosite inhibitors. J Med 1992, 35: 4640-2.
28. Peerlinck, K., DeLepeleire, I., Goldberg, M., Farrell, D., Barrett, J., Hand, E., Panebianco, D., Deckmyn, H., Vermylen, J., Arnout, J. MK383 (L-700462), a selective nonpeptide platelet glycoprotein IIb/IIIa antagonist, is active in man. Circulation 1993, 88: 1512-7.
29. Alig, L., Edenhofer, A., Hadvary, P. et al. Low molecular weight, non-peptide fibrinogen receptor antagonist. J Med Chem 1992, 35: 4393-407.
30. Theroux, P., Kouz, S., Knudtson, M.L., Kells, C., Nasmith, J., Roy, L., DalleAve, S., Steiner, B., Xiao, Z., Rapold, H.J. A randomized, double-blind controlled trial with the non-peptidic platelet GP IIb/IIIa antagonist Ro 44-9883 in unstable angina. Circulation 1994, 90: Abst 1243.
31. Zablocki, J.A., Rico, J.G., Garland, R.B. et al. Potent in vitro and in vivo inhibitors of platelet aggregation based upon the Arg-Gly-Asp sequence of fibrinogen. (Aminobenzamido)succinyl (ABAS) series of orally active fibrinogen receptor antagonists. J Med 1995, 38: 2378-94.
32. Zablocki, J., Nicholson, N., Taite, B. et al. Selection of an orally active glycoprotein IIb/IIIa receptor antagonist for clinical trials. Thromb Haemost 1993, 69: Abst 2503.
33. Kottke-Marchant, K., Simpfendorfer, C., Lowrie, M., Burns, D., Anders, R.J. Sustained but variable inhibition of platelet aggregation with xemilofiban, an oral GPIIb/IIIa receptor antagonist, in patients with unstable angina. Circulation 1995, 92(8, Suppl.): Abst 2331.
34. Narjes, H., Weisenberger, H., Muller, T.H. et al. Tolerability and platelet fibrinogen receptor occupancy (FRO) after oral treatment with BIBU 104 xx in healthy volunteers. Thromb Haemost 1995, 73: 1315-592.
35. Cannon, C.P., McCabe, C.H., Borzak, S. et al. Randomized trial of an oral platelet glycoprotein IIb/IIIa antagonist, sibrafiban, in patients after acute coronary syndrome. Results of the TIMI 12 trial. Circulation 1998, 97: 340-9.
36. Topol, E.J. Toward a new frontier in myocardial reperfusion therapy: Emerging. Circulation 1998, 97: 211-8.
37. Xue, C.-B., Wityak, J., Sielecki, T.M. et al. Synthesis and pharmacology of orally active isoxazoline glycoprotein IIb-IIIa receptor antagonists. 211th ACS Natl Meet (March 24-28, New Orleans) 1996, Abst MEDI 132.
38. Olson, R.E., Wityak, J., Xue, C.-B. et al. The discovery of DMP 754, an orally active isoxazoline GPIIb/IIIa antagonist. 211th ACS Natl Meet (March 24-28, New Orleans) 1996, Abst MEDI 250.
39. Mousa, S.A., Forsythe, M., Lorelli, W. et al. Novel nonpeptide antiplatelet glycoprotein IIb/IIIa receptor antagonist, DMP 754: Receptor binding affinity and specificity. Coron Artery Dis 1996, 7: 767-74.
40. Mousa, S.A., Borzath, J.M., Forsythe, M.S., Lorelly, W., Ramachandran, N., Jackson, S., DeGrado, W.F., Reilly, T.M. Antiplatelet efficacy and specificity of DMP 728, a novel platelet GPIIb/IIIa receptor antagonist. Cardiology 1993, 83: 374-82.
41. Mousa, S.A., Bozarth, J., Forsythe, M., Xue, C.-B., Wityak, J., Olson, R., Thoolen, M., Reilly, T. Discovery of novel orally active non-peptide antiplatelet GPIIb/IIIa antagonist, DMP 754: Comparative platelet binding affinity profiles with DMP 728 and c7E3. Thromb Haemost 1997, Suppl.: Abst PS-2707.
42. Kapil, R.P., Padovani, P.K., Garner, D.M., Chien, B.M., Quon, C.Y., Lam, G.N. Nonlinear pharmacokinetics of a novel platelet glycoprotein IIb/IIIa receptor antagonist, XV459, in beagle dogs. Pharm Res 1996, 13(9, Suppl.): Abst PPDM 8417.
43. Kapil, R.P., Emm, T.A., Mousa, S.A., Padovani, P.K., Quon, C.Y., Lam, G.N. Biological matrix-dependent pharmacokinetic and pharmacodynamic parameters of a novel glycoprotein IIb/IIIa receptor antagonist, XU063, in beagle dogs. Thromb Res 1997, 86: 221-32.