Nonpeptide glycoprotein IIb/IIIa inhibitors. 8. Antiplatelet activity and oral antithrombotic efficacy of L-734,217

Journal of Pharmacology and Experimental Therapeutics

Volumn 278, Issue 1, 1996, Pages 62-73

  Cook, Jacquelynn J ^a   Holahan, Marie A ^a   Lyle, Elizabeth A ^a   Ramjit, Denise R ^a   Sitko, Gary R ^a   Stranieri, Maria T ^a   Stupienski III, Raymond F ^a   Wallace, Audrey A ^a   Hand, Elizabeth L ^a   Gehret, John R ^a   Kothstein, Theresa ^a   Drag, Marlene D ^a   McCormick, Gwendolynn Y ^a   Perkins, James J ^a   Ihle, Nathan C ^a   Duggan, Mark E ^a   Hartman, George D ^a   Gould, Robert J ^a   Lynch Jr , Joseph J ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ACETYLSALICYLIC ACID; ADENOSINE DIPHOSPHATE; ANTICOAGULANT AGENT; COLLAGEN; FIBRINOGEN RECEPTOR; FIBRINOGEN RECEPTOR ANTAGONIST; HEPARIN; L 734217; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BLEEDING TIME; CONTROLLED STUDY; CORONARY ARTERY CIRCUMFLEX BRANCH; CORONARY ARTERY THROMBOSIS; DOG; DOSE RESPONSE; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG EFFICACY; FEMALE; GUINEA PIG; HEART INFARCTION; HEART VENTRICLE EXTRASYSTOLE; HEMOSTASIS; INTRAVENOUS DRUG ADMINISTRATION; MALE; MESENTERIC ARTERY; NONHUMAN; ORAL DRUG ADMINISTRATION; PRIORITY JOURNAL; RAT; THROMBOCYTE AGGREGATION INHIBITION; THROMBOCYTE RICH PLASMA;

ANIMALS; BETA-ALANINE; DOGS; DOSE-RESPONSE RELATIONSHIP, DRUG; GLYCOPROTEINS; GUINEA PIGS; MALE; PIPERIDINES; PLATELET AGGREGATION; PLATELET AGGREGATION INHIBITORS; RATS; RATS, SPRAGUE-DAWLEY;

EID: 12644302208     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (50)

1. BARRETT, J. S., GOULD, R. J., ELLIS, J. D., HOLAHAN, M. A., STRANIERI, M. T., LYNCH, J. J., HARTMAN, G. D., IHLE, N., DUGGAN, M., MORENO, O. A. AND THEOHARIDES, A. D.: Pharmacokinetics and pharmacodynamics of L-703,104, a potent fibrinogen receptor antagonist, after intravenous and oral administration in the dog. Pharm. Res. 11: 426-431, 1994.
2. BRAUNWALD, E., JONES, R. H., MARK, D. B., BROWN, J., BROWN, L., CHEITLIN, M. D., CONCANNON, C. A., COWAN, M., EDWARDS, C., FUSTER, V., GOLDMAN, L., GREEN, L. A., GRINES, C. L., LYTLE, B. W., MCCAULEY, K. M., MUSHLIN, A. I., ROSE, G. C., SMITH III, E. E., SWAIN, J. A., TOPOL, E. J. AND WILLERSON, J. T.: Diagnosing and managing unstable angina. Circulation 80: 613-622, 1994.
3. BUSH, L. R. AND SHEBUSKI, R. J.; In vivo models of arterial thrombosis and thrombolysis. FASEB J. 4: 3087-3098, 1990.
4. COLLEN, D., Lu, H.-R., STASSEN, J.-M., YREYS, I., YASUDA, T., BUNTING, S. AND GOLD, H. K.: Antithrombotic effects and bleeding time prolongation with synthetic platelet GPIIb/IIIa inhibitors in animal models of platelet-mediated thrombosis. Thromb. Haemost. 71: 95-102, 1994.
5. COLLER, B. S., FOLTS, J. D., SMITH, S. R., SCUDDER, L. E. AND JORDAN, R.: Abolition of in vivo platelet thrombus formation in primates with monoclonal antibodies to the platelet GP IIb/IIIa receptor. Correlation with bleeding time, platelet aggregation, and blockade of GP IIb/IIIa receptors. Circulation 80:1766-1774, 1989.
6. COOK, J. J., HUANG, T-F., RUCINSKI, B., STRZYZEWSKI, M., TUMA, R. F., WILLIAMS, J. A. AND NIEWIAROWSKI, S.; Inhibition of platelet hemostatic plug formation by trigramin, a novel RGD-peptide. Am. J. Physiol. 256: H1038-H1043, 1989.
7. COOK, N. S., BRUTTGER, O., PALLY AND 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. 70: 838-847, 1993a.
8. COOK, N. S., ZERWES, H-G., TAPPARELLI, C., FOWLING M., SINGH, J., METTERNICH, R. AND HAGENBACH, A.: Platelet aggregation and fibrinogen binding in human rhesus monkey, guinea-pig, hamster and rat blood: activation by ADP and a thrombin receptor peptide and inhibition by glycoprotein IIb/IIIa antagonists. Thromb. Haemost. 70: 531-539, 1993b.
9. COUTRE, S. AND LEUNG, L.: Novel antithrombotic therapeutics targeted against platelet glycoprotein IIb/IIIa. Annu. Rev. Med. 46: 257-265, 1995.
10. COX, D., MOTOYAMA, Y., SEKI, J., AOKI, T., DOHI M. AND YOSHIDA, K.: Pentamidine: A non-peptide GPIIb/IIIa antagonist-in vitro studies on platelets from humans and other species. Thromb. Haemost. 68: 731-736, 1992.
11. DEMROW, H., BATLEY, C. AND FOLTS, J. D.: SDZ GPI562, an oral peptidomimetic inhibitor of the platelet GPIIb/IIIa abolishes epinephrine and shear induced cyclic flow reductions in stenosed monkey carotid arteries. J. Am Coll Cardiol 25: 70A, 1995.
12. DUGGAN, M. E., NAYLOR-OLSEN, A. M., PERKINS, J. J., ANDERSON, P. S., CHANG, C. T.-C., COOK, J. J., GOULD, R. J., IHLE, N. C., HARTMAN, G. D., LYNCH, J. J., LYNCH, R. J., MANNO, P. D., SCHAFFER, L. W. AND SMITH, R. L.: Nonpeptide fibrinogen receptor antagonists. 7. Design and synthesis of the potent, orally active fibrinogen receptor antagonist L-734,217. J. Med. Chem. 38: 3332-3341, 1995.
13. EPIC INVESTIGATORS: Use of a monoclonal antibody directed against the platelet glycoprotein IIb/IIIa receptor in high risk coronary angioplasty. N. Engl. J. Med. 330: 956-961, 1994.
14. FEIGEN, L. P., NICHOLSON, N. S., KING, L. W., CAMPION, J. G., TJOENG, F. S. AND PANZER-KNODLE, S. G.: SC-49992, a mimetic of the peptide arginine-glycineaspartic acid-phenylalanine that blocks platelet aggregation, enhances recombinant tissue plasminogen activator-induced thrombolysis and prevents reocclusion in a canine model of coronary artery thrombosis. J. Pharmacol. Exp. Ther. 267:1191-1197, 1993.
15. FISHBEIN, M. C., MEERBAUM, S., RIT, J., LANDO, U., KANMATSUSE, K., MERCIER, J. C., CORDAY, E. AND GANZ, W.: Early phase acute myocardial infarct size quantitation. Validation of the triphenyltetrazolium chloride tissue enzyme staining technique. Am. Heart J. 101: 593-600, 1981.
16. 2-protaglandin endoperoxide receptor activation in vivo. J. Clin. Invest. 77: 496-502, 1986.
17. GILBERT, J. D., HAND, E. L., MCLOUGHLIN, D. A., ELLIS, J. D., OLAH, T. V., YUAN, A. S. AND FERNANDEZ-METZLER, C.: The development and cross-validation of methods based on RIA and LC/MS/MS for the quantitation of the fibrinogen receptor antagonist L-734,217 in plasma. In Methodological Surveys in Bioanalysis of Drugs, Vol. 24, ed. by E. Reid, H. M. Hill and I. D. Wilson, Royal Society of Chemistry, Cambridge, 1996, in press.
18. GOLD, H. K., COLLER, B. S., YASUDA, T., SAITO, T., FALLON, J. T., GUERRERO, J. L., LEINBACH, R. C., ZISKIND, A. A. AND COLLEN, D.: Rapid and sustained coronary artery recanalization with combined bolus injection of recombinant tissue-type plasminogen activator and monoclonal antiplatelet GF IIb/IIIa in a canine preparation. Circulation 77: 670-677, 1988.
19. JERGENS, A. E., TURRENTINE, M. A., KRAVE, K. H. AND JOHNSON, G. S.: Buccal mucosa bleeding times of healthy dogs and of dogs in various pathologic states, including thombocytopenia, uremia, and von Willebrand's disease. Am. J. Vet. Res. 48: 1337-1342, 1987.
20. JONES, C. R., AMBROS, R. J., RAPOLD, H. J., STEINER, B., WELLER, T., VAN HEIN-INOEN, P., CRIJINS, H. J. M. J., JONKMAN, J. H. G. AND HADVARY, P.: RO 44-9883: a novel non-peptide GP IIb/IIIa antagonist in man. Thromb. Haemost. 69: 560, 1993.
21. KEREIAKES D., KLEIMAN N., AMBROSE J., COHEN M., RODRIGUEZ S., PALABRICA T., HERRMANN H. C., SUTTON J., WEAER S. W., MCKEE D. AND SAX F. L.: A dosing study in high-risk PTCA of MK-383, a platelet IIb/IIIa antagonist. Circulation 90: I-21, 1994.
22. KLEIMAN, N. S., OHMAN, E. M., CALIFF, R. M., GEORGE, B. S., KEREIAKES, D., AGUIRRE, F. V., WEISMAN, H., SCHAIBLE, T. AND TOPOL, E. J.: Profound inhibition of platelet aggregation with monoclonal antibody 7E3 after thrombolytic therapy. Results of the thrombolysis and angioplasty in myocardial infarction (TAMI) 8 pilot study. J. Am. Coll. Cardiol. 22: 381-389, 1993.
23. KOTTKE-MARCHANT, K. SIMPFENDORFER, C., LOWRIE, M., BURNS, D. AND ANDERS, R. J.: Sustained but variable inhibition of platelet aggregation with Xemlofiban, an oral GPIIb/IIIa receptor antagonist, in patients with unstable angina. Circulation 92:1-488, 1995.
24. LEFKOVITS, J., PLOW, E. F. AND TOPOL, E. J.: Platelet glycoprotein IIb/IIIa receptors in cardiovascular medicine. N. Engl. J. Med. 332: 1553-1559, 1995.
25. LIND, S. E.: The bleeding time does not predict surgical bleeding. Blood 77: 2547-2552, 1991.
26. LUCCHESI, B. R., ROTE, W. E., DRISCOLL, E. M. AND Mu, D-X.: Prevention of thrombosis and rethrombosis and enhancement of the thrombolytic actions of recombinant tissue-type plasminogen activator in the canine heart by DMP728, a glycoprotein IIb/IIIa antagonist. Br. J. Pharmacol. 113: 1333-1343, 1994.
27. LYNCH, J. J., COOK, J. J., SITKO, G. R., HOLAHAN, M. A., RAMJIT, D. R., MELLOTT, M. J., STRANIERI, M. T., STABILITO, I. I., ZHANG, G., LYNCH, R. J., MANNO, P. D., CHANG, C. T.-C., EGBERTSON, M. S., HALCZENKO, W., DUGGAN, M. E., LASWELL, W. L., VASSALLO, L. M., SHAFER, J. A., ANDERSON, P. S., FRIEDMAN, P. A., HARTMAN, G. D. AND GOULD, R. J.: Non-peptide glycoprotein IIb/IIIa inhibitors. 5. Antithrombotic effects of MK-0383. J. Pharmacol. Exp. Ther. 272: 20-32, 1995.
28. MAZUR C., TSCHOPP J. F., FALAIKOU E. C., GOULD K. E., DIEHL J. T., PIERSCHBACHER M. D. AND CONNOLLY R. J.: Selective αiibβ3 receptor blockade with peptide TP9201 prevents platelet uptake on Dacron vascular grafts without significant effect on bleeding time. J. Lab. Clin. Invest. 124: 589-599, 1994.
29. MICKELSON, J. K., SIMPSON, P. J. AND LUCCHESI, B. R.: Antiplatelet monoclonal F(ab')2 antibody directed against the platelet GPIIb/IIIa receptor complex prevents coronary artery thrombosis in the canine heart. J. Mol. Cell Cardiol. 21: 393-405, 1989.
30. MOUSA, S. A., BOZARTH, J. M., FORSYTHE, M. S., JACKSON, S. A., LEAMY, A., DIEMER, M. J., KAPIL, R. P., KNABB, R. M., MAYP, M. C., PIERCE, S. K., DEGRADO, W. F., THOOLEN, M. J. AND REILLY, T. M.: Antiplatelet, antithrombotic efficacy of DMP 728, a novel platelet GP IIb/IIIa receptor antagonist. Circulation 89: 3-12, 1994,
31. MULLER T. H., SCHURER H., WALDMANN L., BAUER E., HIMMELSBACH F., BINDER K.: Oral activity of BIBU 104, a prodrug of the non-peptide fibrinogen receptor antagonist BIBU 52, in mice and monkeys. Thromb. Haemost. 69:975, 1993.
32. NICHOLS, A. J., VASKO, J. A., KOSTER, P. F., VALOCIK, R. E., RHODES, G. R., MILLER-STEIN, C., BOPPANO, V. AND SAMANEN, J. M.: The in vivo pharmacological profile of the novel glycoprotein IIb/IIIa antagonist, SK&F 106760. J. Pharmacol. Exp. Ther. 270: 614-621, 1994.
33. NICHOLSON, N. S., PANZER-KNODLE, S. G., SALYERS, A. K., TAITE, B. B., SZALONY, J. A., HAAS, N. F., KING, L. W., ZABLOCKI, J. A., KELLER, B. T., BROSCHAT, K., ENGLEMAN, V. W., HERIN, M., JACQMIN, P. AND FEIGEN, L. P. SC-54684A: An orally active inhibitor of platelet aggregation. Circulation 91:403-410, 1995.
34. OHMAN, E. M., KIEIMAN, N. S., TALLEY, J. D., GACIOCH, G., NAVETTA, F. I., CARNEY, R. J., WORLEY, S., ANDERSON, H. V., COHEN, M., KEREIAKES, D., JOSEPH, D., SIGMON, K. N. AND TOPOL, E. J.: Simultaneous platelet glycoprotein IIb/IIIa integrin blockade with accelerated tissue plaaminogen activator in acute myocardial infarction. Circulation 90: I-564, 1994.
35. PEERLINCK, K., ARNOUT, J., DE LEPELEIRE, I., GOLDBERG, M., FITZPATRICK, V. AND VERMYLEN, J.: Combined effect of aspirin and MK-383 (L-700,462), a selective GPIIb/IIIa antagonist, in healthy volunteers. Thromb. Haemost. 69: 560, 1993.
36. PIKE N. B., FOSTER M. R., HORNBY E. J. AND LUMLEY P.: Effect of the fibrinogen receptor antagonist GR144053 upon platelet aggregation ex. vivo following intravenous and oral administration to the marmoset and cynomolgus monkey. Thromb. Haemost. 69: 1701, 1993.
37. RAMJIT, D. R., LYNCH, J. J., SITKO, G. R., MELLOTT, M. J., HOLAHAN, M. A., STABILITO, I. I., STRANIERI, M. T., ZHANG, G., LYNCH, R. J., MANNO, P. D., CHANG, C. T.-C., NUTT, R. F., BRADY, S. F., VEBER, D. F., ANDERSON, P. S., SHEBUSKI, R. J., FRIEDMAN, P. A. AND GOULD, R. J.: Antithrombotic effects of MK-0852, a novel platelet fibrinogen receptor antagonist, in canine models of thrombosis. J. Pharmacol. Exp. Ther. 266: 1501-1511, 1993.
38. RODGERS, R. P. C. AND LEVIN, J.: A critical reappraisal of the bleeding time. Semin. Thromb. Hemost. 16: 1-20, 1990.
39. ROMSON, J. L., HAACK, D. W. AND LUCCHESI, B. R.: Electrical induction of coronary artery thrombosis in the ambulatory canine: A model for in vivo evaluation of antithrombotic agents. Thromb. Res. 17: 841-853, 1980.
40. SCHROR, K.: Antiplatelet drugs. A comparative review. Drugs 50: 7-28, 1995.
41. SCHULMAN, S. P., GOLDSCHMIDT-CLERMONT, P. J., NAVETTA, F. I., CHANDRA, N. C., GUERCI, A. D., CALIFF, R. M., FERGUSON, J. J., WILLERSON, J. T., WOLFE, C. L., BAHR, R., YAKUBOV, S. J., NYGAARD, T. W., MASON, S. J., BRASHEAHS, L., CHARO, I., DE MEE, C., KITT, M. M. AND GERSTENBLITH, G.: Integrelin in unstable angina: a doule-blind randomized trial. Circulation 88: I-608, 1993.
42. SIETSEMA, W. K.: The absolute oral bioavailability of selected drugs. J Clin. Pharm. 27: 179-211, 1989.
43. SIMOONS M. L., JAN DE BOER M., VAN DEN BRAND MJBM, VAN MILTENBURG AJM, HOORNTJE JCA, HEYNDRICKX G. R., VAN DER WIEKEN L. R., DE BONO D., RUTSCH W., SCHAIBLET. F., WEISMAN H. F., KLOOTWIJK P., NIJSSEN K M., STIBBE J. AND DE FEYTER P. J.: European Cooperative Study Group. Randomized trial of a GPIIb/IIIa platelet receptor blocker in refractory unstable angina. Circulation 89: 596-603, 1994.
44. TCHENG, J. E., HARRINGTON, R. A., KOTTKE-MARCHANT, K., KLEIMAN, N. S., ELLIS, S. G., KEREIAKES, D. J., MICK, M. J., NAVETTA, F. I., SMITH, J. E., WORLEY, S. J., MILLER, J. A., JOSEPH, D. M., SIGMON, K. N., KITT, M. M., DUMEE, C. P., CALIFF, R. M. AND TOPOL, E. J.: Multicenter randomized double-blind placebo controlled trail of the platelet integrin glycoprotein IIb/IIIa blocker Integrelin in elective coronary intervention. Circulation 91: 2151-2157, 1995.
45. THEROUX, P., KOUZ, S., KNUDTSON, M. L., KELLS, C., NASMITH, J., ROY, L., DALLE AVE, S., STEINER, B., XIAO, Z. AND RAPOLD, H. J.: A randomized double-blind controlled trial with the non-peptide platelet GPIIb/IIIa antagonist Ro 44-9883 in unstable angina. Circulation 90: I-246, 1994a.
46. THEROUX, P., WHITE, H., DAVID, D., VAN DE WERF, F., NIENABER, C. A., CHARBONNIER, B., ERHARDT, L., GILL, J., HILLIS, W. S., JENNINGS, G., TAN, L-B., DESCHENES, N., FITZPATRICK, V. AND SAX, F. L.: A heparin-controlled study of MK-383 in unstable angina. Circulation 90: I-231, 1994b.
47. TOPOL, E. J., CALIFF, R. M., WEISMAN, H. F., ELLIS, S. G., TCHENG, J. E., WORLEY, S., IVANHOE, R., GEORGE, B. S., FINTEL, D., WESTON, M., SIGMON, K., ANDERSON, K. M., LEE, K. L., WILLERSON, J. T. AND EPIC INVESTIGATORS.: Randomised trial of coronary intervention with antibody against platelet IIb/IIIa integrin for reduction of clinical restenosis. Results at six months. Lancet 1: 881-886, 1994.
48. TOPOL, E. J.: Prevention of cardiovascular ischemic complications with new platelet glycoprotein IIb/IIIa inhibitors. Am. Heart J. 130: 666-672, 1995.
49. TSCHOPP, J. F., DRISCOLL, E. M., MU, D-X., BLACK, S. C., PIERSCHBACHER, M. D. AND LUCCHESI, B. R.: Inhibition of coronary artery reocclusion after thrombolysis with an RGD-containing peptide with no significant effect on bleeding time. Coronary Artery Dis. 4: 809-817, 1993.
50. VIVALDI, M. T., KLONER, R. A. AND SCHOEN, F. J.: Triphenyltetrazolium staining of irreversible ischemic injury following coronary artery occlusion in rats. Am. J. Pathol. 121: 522-530, 1985.