SR 121787, a new orally active fibrinogen receptor antagonist

Thrombosis and Haemostasis

Volumn 80, Issue 3, 1998, Pages 469-476

  Savi, Pierre ^a   Badorc, Alain ^a   Lalé, Alain ^a   Bordes, Marie Françoise ^a   Bornia, Josette ^a   Labouret, Catherine ^a   Bernat, André ^a   De Cointet, Paul ^a   Hoffmann, Peter ^a   Maffrand, Jean Pierre ^a   Herbert, Jean Marc ^a,b  

^a SANOFI   (France)

^b Haemobiology Research Department   (France)

Author keywords

[No Author keywords available]

Indexed keywords

3 [[4 [4 (AMINOIMINOMETHYL)PHENYL] 2 THIAZOLYL](1 CARBOXYMETHYL 4 PIPERIDINYL)AMINO]PROPIONIC ACID; 3 [[4 [4 [AMINO(ETHOXYCARBONYLIMINO)METHYL]PHENYL] 2 THIAZOLYL](1 ETHOXYCARBONYLMETHYL 4 PIPERIDINYL)AMINO]PROPIONIC ACID ETHYL ESTER; ADENOSINE DIPHOSPHATE; ANTICOAGULANT AGENT; ANTITHROMBOCYTIC AGENT; ARACHIDONIC ACID; COLLAGEN; DRUG METABOLITE; FIBRINOGEN; FIBRINOGEN RECEPTOR; FIBRINOGEN RECEPTOR ANTAGONIST; L 692884; THROMBIN; THROMBOCYTE ACTIVATING FACTOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BABOON; CONTROLLED STUDY; DOSE TIME EFFECT RELATION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG EFFICACY; DRUG POTENCY; DRUG STRUCTURE; DRUG TOLERABILITY; HEMATOLOGY; HEMODYNAMICS; HEMOSTASIS; INTRAVENOUS DRUG ADMINISTRATION; NONHUMAN; ORAL DRUG ADMINISTRATION; PRIORITY JOURNAL; RABBIT; THROMBOCYTE ACTIVATION; THROMBOCYTE ADHESION; THROMBOCYTE AGGREGATION; THROMBOCYTE AGGREGATION INHIBITION; THROMBOSIS;

EID: 0031726464     PISSN: 03406245     EISSN: None     Source Type: Journal    
DOI: 10.1055/s-0037-1615231     Document Type: Article

References (31)

1. Herbert JM, Frehel D, Vallée E, Kieffer G, Gouy D, Berger Y, Necciari J, Defreyn G, Maffrand JP. Clopidogrel: a novel antiplatelet and antithrombotic agent. Cardiovasc Drug Rev 1993; 11: 180-98.
2. Antiplatelet Trialists' Collaboration. Secondary prevention of vascular disease by prolonged antiplatelet therapy. Br. Med. J. 1994; 308: 81-106.
3. CAPRIE Steering committee : A randomized, blinded, trial of clopidogrel versus aspirin in patients at risk of ischaemic events (CAPRIE), Lancet, 1996; 348: 1329-39.
4. Phillips DR, Fitzgerald LA, Charo IF, Parise LV. The platelet membrane glycoprotein IIb-IIIa complex; structure, function, and relationship to adhesive protein receptors in nucleated cells. Ann. NY Acad. Sci. 1987: 509: 177-87.
5. Kieffer N, Phillips DR. Platelet membrane glycoproteins: functions in cellular interactions. Annu. Rev. Cell. Biol. 1990: 6: 329-57.
6. Coller BS. Antiplatelet agents in the prevention and therapy of thrombosis. Annu. Rev. Med. 1992; 43: 171-80.
7. Cadroy Y, Houghten RA, Hanson SR. RGDV peptide selectively inhibits platelet-dependent thrombus formation in vivo. Studies using a baboon model. J. Clin. Invest. 1989; 84: 939-44.
8. Dennis MS, Henzel WJ, Pitti RM, Lipari MT, Napier MA, Deisher TA, Bunting S, Lazarus RA. Platelet Gp IIb/IIIa from snake venoms; evidence for a family of platelet aggregation inhibitors. Proc Natl Acad Sci USA 1990; 87: 2471-5.
9. Tschopp JF, Driscoll EM, MU DX, Black SC, Pierschbacher MD, Lueehesi BR. Inhibition of coronary artery reocclusion after thrombolysis with an RGD-containing peptide with no significant effect on bleeding time. Coronary Art Dis 1993; 4: 809-17.
10. Mickelson JK, Simpson PJ, Cronin M, Homeiser JW, Laywell E, Kitzen J, Lucchesi BR. Antiplatelet antibody [7E3 F(ab')2] prevents rethrombosis after recombibinant tissue-type plasminogen activator-induced coronary artery thrombolysis in a canine model. Circulation 1990 ; 81: 617-27.
11. Mickelson JK, Simpson PJ, Lucchesi BR. Antiplatelet monoclonal F(ab') 2 antibody directed against the platelet Gp IIb/IIIa receptor complex prevent coronary artery thrombosis in the canine heart. J Mol Cell Cardiol 1989; 21: 393-405.
12. Bates ER, Walsh DG, Mu DX, Abrams GD, Lueehesi BR. Sustained inhibition of the vessel wall-platelet interaction after deep coronary artery injurj by temporary inhibition of the platelet glycoprotein IIb/IIIa receptor. Coronary Artery Dis. 1992; 3: 67-76.
13. Coller BS. Platelets and thrombolytic therapy. N Engl J Med 1990; 322: 33-42.
14. Gold HK, Gimple LW, Yasuda T, Leinbach RC, Werner W, Holt R, Jordan 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: 651-9.
15. Kleiman NS, Ohman EM, Califf RM, George BS, Kereiakes D, Aguirre FV, Weisman H; Schaible T, Topol EJ. Profound inhibition of platelet aggregation with monoclonal antibody 7E3 Fab after thrombolytic therapy. Results of the Thrombolysis and angioplasty in myocardial infarction (TAMI) 8 pilot study. J Am Coll Cardiol 1993; 22: 381-9.
16. 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: 956-61.
17. Winkelmann BR, Zahn R, Stilz HU, Overview of clinical trials with glycoprotein IIb-IIIa receptor antagonists in the prevention and management of coronary thrombosis, Exp. Opin Invest Drugs 1997, 6: 1623-42.
18. Cox D. Integrins and cardiovascular disease. Exp Opin Invest Drugs 1995; 4: 413-23.
19. Nicholson NS, Panzer-Knodle SG, King LW, Taite BB, Keller BT, Tjoeng FS, Engleman VW, Giorgio TD, Feigen LP. SC-49992 . A potent and specific inhibitor of platelet aggregation. Thromb Res 1994; 74: 523-35.
20. 3 integrins: comparison of Gp IIb/IIIa and the vitronectin receptor individually expressed in human melanoma cells. J Cell Biol 1991; 113: 451-61.
21. Foster MR, Hornby EJ, Brown S, Kitchin J, Hann M, Ward P. Improved potency and specificity of Arg-Gly-Asp (RGD) containing peptides as fibrinogen receptor blocking drugs. Thromb Res 1993; 72: 231-45.
22. Born GVR. Aggregation of blood platelets by adenosine diphosphate and its reversal. Nature (Lond) 1962; 194: 927-9.
23. 2 receptor antagonist. Thromb Haemost 1993; 69: 262-7.
24. Ratkowsky DA, Reedy TJ, Choosing near-linear parameters in the four-parameters logistic model for radioligands and related assays. Biometrics 1986; 42: 575-82.
25. Marquardt DW. An algorythm for least square estimation of non linear parameters. J Soc Indust Appl Mat 1963; 11: 431-41.
26. 3 (platelet Gp IIb/IIIa). Cell 1991; 65: 409-16.
27. Harfenist EJ, Packham MA, Mustard JF. Effects of the cell adhesion peptide, Arg-Gly-Asp-Ser, on responses of washed platelets from humans, rabbits and rats. Blood 1988; 71: 132-6.
28. Verhallen PFJ, Barth M, Species comparison of anti-aggregatory properties of three fibrinogen receptor antagonists: RGDS, echistatin and the carboxyterminal dodecapeptide of the fibrinogen gamma chain. Thromb Haemost 1991; 65: 1144.
29. Hoffmann P, Bernat A, Savi P, Herbert JM. Antiplatelet and antithrombotic efficacy of SR 121787, a novel orally active Gp IIb/IIIa antagonist in rabbits - comparison to clopidogrel and aspirin, J. Cardiovasc. Pharmacol 1997; 30: 360-6.
30. Kawamura M, Imura Y, Moriya N, Kita S, Fukushi H, Sugihara H, Nishikawa K, Terashita Z. Antithrombotic effects of TAK-029, a novel GP IIb/IIIa antagonist, in guinea pigs: Comparative studies with ticlopidine, clopidogrel, aspirin prostaglandin E1 and argatropan. J Pharmac Exp Ther 1996; 277: 502-10.
31. Vogel GMT, Meuleman DG, Bourgondiën FGM, Hobbelen PM. Comparison of two experimental thrombosis models in rats. Effects of four glycosaminoglycans. Thromb Res 1989; 54: 399-410.