Pharmacological effects of a novel recombinant hirudin, CX-397, in vivo and in vitro: Comparison with recombinant hirudin variant-1, heparin, and argatroban

Thrombosis and Haemostasis

Volumn 81, Issue 2, 1999, Pages 250-255

  Komatsu, Yasuhiko ^a   Inoue, Yoshifumi ^a   Goto, Yuso ^a   Fukazawa, Tominaga ^a   Hayashi, Hideya ^a  

^a JAPAN ENERGY CORPORATION   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

ANTITHROMBIN; ARGATROBAN; CX 397; FERRIC CHLORIDE; HEPARIN; LEPIRUDIN; THROMBIN; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTERIOVENOUS SHUNT; ARTERY THROMBOSIS; ARTICLE; BLEEDING; BLOOD CLOTTING TIME; CONTROLLED STUDY; DRUG EFFECT; DRUG EFFICACY; DRUG POTENCY; HEMOSTASIS; INTRAVENOUS DRUG ADMINISTRATION; MALE; NONHUMAN; PRIORITY JOURNAL; RAT; THROMBOCYTE AGGREGATION; VEIN THROMBOSIS;

EID: 0033023026     PISSN: 03406245     EISSN: None     Source Type: Journal    
DOI: 10.1055/s-0037-1614452     Document Type: Article

References (36)

1. Sharf M, Engels J, Tripier D. Primary structure of new 'iso-hirudin'. FEBS Lett 1989; 255: 105-10.
2. Markwardt F. Pharmacology of hirudin: one hundred years after the first report of the anticoagulant agent in medicinal leeches. Biomed Biochim Acta 1985; 7/8: 1007-13.
3. Kaiser B. Anticoagulant and antithrombotic actions of recombinant hirudin. Semin Thromb Haemost 1991; 17: 130-6.
4. Markwardt F. Hirudin and derivatives as anticoagulant agents. Thromb Haemost 1991; 66: 141-52.
5. Lyle EM, Lewis SD, Lehman ED, Gardell SJ, Motzel SL, Lynch JJ Jr. Assessment of thrombin inhibitor efficacy in a novel rabbit model of simultaneous arterial and venous thrombosis. Thromb Haemost 1998; 79: 656-62.
6. Global Use of Strategies to Open Occluded Coronary Arteries (GUSTO) IIa Investigators. Randomized trial of intravenous heparin versus recombinant hirudin for acute coronary syndromes. Circulation 1994; 90: 1631-7.
7. Antman EM. for the TIMI 9A Investigators. Hirudin in acute myocardial infarction. Safety report from the Thrombolysis and Thrombin Inhibition in Myocardial Infarction (TIMI) 9A trial. Circulation 1994; 90: 1624-30.
8. Neuhaus K-L, Essen RV, Tebbe U, Jessel A, Heinrichs H, Mäurer W, Döring W, Harmjanz D, Kötter V, Kalhammer E, Simon H, Horacek T. Safely observations from the pilot phase of the randomized r-Hirudin for Improvement of Thrombolysis (HIT-III) study. A study of the Arbeitsgemeinschaft leitender kardiologischer Krankenhausärzte (ALKK). Circulation 1994; 90: 1638-42.
9. GUST-IIb Investigators. A comparison of recombinant hirudin with heparin for the treatment of acute coronary syndromes. N Engl J Med 1996; 335: 775-82.
10. Antman EM. for the TIMI-9B Investigators. Hirudin in acute myocardial infarction. Thrombolysis and thrombin inhibition in myocardial infarction (TIMI) 9B trial. Circulation 1996; 94: 911-21.
11. Braun P, Dennis S, Hofsteenge J, Stone SR. Use of site directed mutagenesis to investigate the basis for the specificity of hirudin. Biochemistry 1988; 27: 6517-22.
12. Wallace A, Dennis S, Hofsteenge J, Stone SR. Contribution of the N-terminal region of hirudin to its interaction with thrombin. Biochemistry 1989; 28: 10079-84.
13. Lazar, JB, Winant RC, Johnson PH. Hirudin: amino-terminal residues play a major role in the interaction with thrombin. J Biol Chem 1991; 266: 685-8.
14. Betz A, Hofsteenge J, Stone SR. Interaction of the N-terminal region of hirudin with the active-site cleft of thrombin. Biochemistry 1992; 31: 4557-62.
15. Komatsu Y, Misawa S, Sukesada A, Ohba Y, Hayashi H. CX-397, a novel recombinant hirudin analog having a hybrid sequence of hirudin variants-1 and -3. Biochem Biophys Res Commun 1993; 196: 773-9.
16. Takiguchi Y, Asai F, Wada K, Hayashi H, Nakashima M. Antithrombotic effect of a novel recombinant hirudin analogue. CX-397. in a rat arterial thrombosis model. Brit J Pharmacol 1995; 116: 3056-60.
17. Ohyama T, Hori T, Moriike M, Asano T, Hayashi H, Iwade K, Hosoda S. Anti-thrombotic effects of CX-397, a recombinant hirudin analog, in a canine model of coronary artery thrombosis. Thromb Haemost 1998; 79: 423-30.
18. Okamoto S, Hijikata A, Kikumoto R, Tonomura S, Hara H, Ninomiya K, Maruyama A, Sugano M, Tamao Y. Potent inhibition of thrombin by the newly synthesized arginine derivative No. 805. The importance of stereo-structure of its Hydrophobic carboxamide portion. Biochem Biophys Res Commun 1981; 101: 440-6.
19. Kikumoto R, Tamao Y, Tezuka T, Tonomura S, Hara H, Ninomiya K, Hijikata A, Okamoto S. Selective inhibition of thrombin by (2R,4R)-4-methyl-1-[N2-[(3-methyl-1,2,3,4-tetrahydro-8-quinolinyl) sulfonyl]-1-arginyl)]-2-piperidinecarboxylic acid. Biochemistry. 1984; 23: 85-90.
20. Misawa S, Furuya H, Matsuda H, Abe S, Hayashi H. High level expression and secretion of biologically active leech hirudin variant 1 (HV1) by Escherichia coli. In: Biochemical Engineering for 2001: Proceedings of Asia-Pacific Biochemical Engineering Conference 1992. Furusaki S, Endo I, Matsuno R, eds. Springer-Verlag, Tokyo 1992; pp 62-4.
21. Greißbach U, Stürzebecher J, Markwardt F. Assay of hirudin in plasma using a chromogenic thrombin substrate. Thromb Res 1985; 37: 347-50.
22. Muramatsu R, Sasaki M, Watanabe N, Goto Y, Okayama T, Nukui E, Morikawa T, Hayashi H. Antithrombotic effects of NF-6505. a novel anion-binding exosite inhibitor. Thromb Res 1997; 86: 453-60.
23. Smith GF, Neubauer BL, Sundboom JL, Best KL, Goode RL, Tanzer LR, Merriman RL, Frank JD, Herrmann RG. Correlation of the in vivo anticoagulant, antithrombotic, and antimetastatic efficacy of warfarin in the rat. Thromb Res 1988; 50: 163-74.
24. Mielke CH Jr. Kaneshiro MM, Maher IA, Weiner JM, Rapaport SI. The standardized normal Ivy bleeding time and its prolongation by aspirin. Blood 1969; 34: 204-15.
25. Stella L, Donati MB, de Gaetano G. Bleeding time in laboratory animals. I. Aspirin does not prolong bleeding time in rats. Thromb Res 1975; 7: 709-16.
26. Muramatsu R, Komatsu Y, Nukui E, Okayama T, Morikawa T, Kobashi K, Hayashi H. Structure-activity studies on C-terminal hirudin peptides containing sulfated tyrosine residues. Int J Peptide Protein Res 1996; 48: 167-73.
27. Mustard JF, Perry DW, Ardlie NG, Packam MA. Preparation of suspensions of washed platelets from humans. Brit J Haematol 1972; 22: 193-204.
28. Born GVR. Aggregation of blood platelets by adenosine diphosphate and its reversal. Nature 1962; 194: 827-929.
29. Moncada S, Gryglewski R, Bunting S, Vane JR. An enzyme isolated from arteries transforms prostaglandin endoperoxides to an unstable substance that inhibits platelet aggregation. Nature 1976; 263: 663-5.
30. Henderson PJF. A linear equation that describes the steady-state kinetics of enzymes and subcellular particles interacting with tightly bound inhibitors. Biochem J 1972; 127: 321-33.
31. Elg M, Gustafsson D, Deinum J. The importance of enzyme inhibition kinetics for the effect of thrombin inhibitors in a rat model of arterial thrombosis. Thromb Haemost 1997; 78: 1286-92.
32. Friedberg RC, Hagen PO, Pizzo SV. The role of endothelium in factor Xa regulation: the effect of plasma proteinase inhibitors and hirudin. Blood 1988; 71: 1321-8.
33. Pizzo SV, Friedberg RC, Sze P, Winant R, Hudson D, Lazar JM, Johnson PH. Recombinant hirudin displaces human factor Xa from its endothelial binding sites. Thromb Res 1990; 57: 803-6.
34. Walenga JM, Bakhos M, Messmore HL, Koza M, Wallock M, Orfei E, Fareed J, Pifarre R. Comparison of recombinant hirudin and heparin as an anticoagulant in a cardiopulmonary bypass model. Blood Coagul Fibrinolysis 1991; 2: 105-11.
35. Riess FC, Potzsch B, Behr I, Jager K, Rossing R, Bleese N, Schaper W, Muller-Berghaus G. Recombinant hirudin as an anticoagulant during cardiac operations: experiments in a pig model. Eur J Cardiothorac Surg 1997; 11: 739-45.
36. Rucinski B, Niewiarowski S, James P, Walz DA, Budzynski AZ. Anti-heparin proteins secreted by human platelets: Purification and characterization and radioimmunoassay. Blood 1979; 53: 47-62.