Effects of aprosulate, a novel synthetic glycosaminoglycan, on coagulation and platelet function parameters: A prospective, randomized phase I study

Clinical and Applied Thrombosis/Hemostasis

Volumn 5, Issue 3, 1999, Pages 192-197

  Schenk, Joachim F ^d   Radziwon, Piotr ^a   Mörsdorf, Stefan ^e   Eckenberger, Peter ^b   Breddin, Hans K ^c  

^a MEDICAL UNIVERSITY OF BIALYSTOK   (Poland)

^b Div R and D Luitpold Pharma   (Germany)

^c Intl Inst Thromb and Vasc Dis   (Germany)

^d SAARLAND UNIVERSITY   (Germany)

^e NONE

Author keywords

Anticoagulation; Aprosulate; Platelet function; Thrombin generation; UFH

Indexed keywords

APROSULATE; FIBRINOGEN; HEPARIN CALCIUM; RISTOCETIN; VON WILLEBRAND FACTOR;

ADULT; ANTICOAGULATION; ARTICLE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DOSE RESPONSE; DRUG TOLERABILITY; ERYTHEMA; GLYCOSAMINOGLYCAN METABOLISM; HUMAN; HUMAN CELL; HUMAN EXPERIMENT; HUMAN TISSUE; NORMAL HUMAN; PARTIAL THROMBOPLASTIN TIME; PHASE 1 CLINICAL TRIAL; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; SULFATION; THROMBOCYTE ADHESION; THROMBOCYTE FUNCTION;

EID: 0033044129     PISSN: 10760296     EISSN: None     Source Type: Journal    
DOI: 10.1177/107602969900500311     Document Type: Article

References (39)

1. Raake W, Klauser RJ, Elling H, Meinetsberger E. Anticoagulant and antithrombotic properties of synthetic sulfated bis-lactobiomacid amides. Thromb Res 1989;56:719.
2. Raake W, Klauser RJ, Meinetsberger E, et al. Pharmacologic profile of the antithrombotic and bleeding actions of sulfated lactobionic acid amides. Semin Thromb Hemost 1991;17(Suppl):129.
3. Raake W, Elling H. Rat jugular vein hemostasis - A new model for testing antithrombotic agents. Thromb Res 1989;53:73.
4. Klauser RJ, Meinetsberger E, Raake W. Biochemical studies on sulfated lactobionic acid amides. Semin Thromb Hemost 1991;17(Suppl):118.
5. Klauser RJ, Raake W, Meinetsberger E, Zeiller P. Antithrombotic and anticoagulant properties of synthetic polyanions: sulfated bis lactobionic acid amides. J Pharmacol Exp Ther 1991;259:8.
6. Klauser RJ. Interaction of the sulfated lactobionic acid amide I.W 10 082 with thrombin and its endogenous inhibitors. Thromb Res 1991;62:557.
7. Sugidachi A, Asai F, Koike H. In vivo pharmacology of aprosulate. a new synthetic polyanion with anticoagulant activity. Thromb Res 1993;69:71.
8. Raake W, Klauser RJ, Elling H, et al. Derivates of bis-aldonic acid amides and their anticoagulant and antithrombotic properties. Semin Thromb Hemost 1994;20:176.
9. Ofosu FA. Mechanisms for the anticoagulant effects of synthetic antithrombins. Adv Exp Med Biol 1993;340:213.
10. Sugidachi A, Asai F, Koike H. Anticoagulant and antiprotease activities of aprosulate sodium, a new synthetic polyanion, in human plasma and purified systems. Blood Coagul Fibrinolysis 1994;5:773.
11. Ofosu FA, Fareed J, Smith LM, et al. Inhibition of factor X, factor V and prothrombin activation by the bis-lactobionic acid amide LW 10 082. Eur J Biochem 1992;203:121.
12. Kijowski R, Hoppensteadt D, Jeske W, Fareed J. Protamine sulfate neutralization of the anticoagulant activity of Aprosulate, a synthetic sulfated lactobionic acid amide. Thromb Res 1994;73:349.
13. Pinhal MA, Walenga JM, Jeske W, et al. Antithrombotic agents stimulate the synthesis and modify the sulfation pattern of a heparan sulfate proteoglycan from endothelial cells. Thromb Res 1994; 74:143.
14. Klauser RJ, Meinetsberger E, Raake W, Zeiller P. New synthetic heparinoids: chemistry, anticoagulatory and antithrombotic properties of bis-lactobionic acid amides. Thromb Haemorrh Disorders 1990;2:75.
15. Sugidachi A, Asai F, Tany Y, et al. Occlusive thrombosis in the femoral artery of the rabbit: a pharmacological model for evaluating antiplatelet and anticoagulant agents. Blood Coagul Fibrinolysis 1996;7:57.
16. Raake W, Klauser RJ, Meinetsberger E. Antithrombotic activities of aprosulate sodium (LW 10 082) and its neutralization by protamine. Semin Thromb Hemost 1993;19:183.
17. Giedrojc J, Krupinski K, Breddin HK, Bielawiec M. Interaction between the sulfated lactobionic acid (LW 10 082) and other antithrombotic agents in animal thrombosis model. Pol J Pharmacol 1996;48:317.
18. Giedrojc J, Weichert W, Breddin HK. Antithrombotic effects of molsidomine alone and in combination with other antithrombotic agents in a thrombosis model of the microcirculation of the rat Antithrombotische Wirkungen von Molsidomin allein und in Kombination mit anderen Antithrombotika an einem Thrombose-modell in der Mikrozirkulation der Ratte. Z Kardiol 1991;80:35.
19. Papoulias UE, Wyld PJ, Haas S, et al. Phase-I study with aprosulate, a new synthetic anticoagulant. Thromb Res 1993;72:99.
20. Yin E, Wessler S, Butler J. Plasma heparin. A unique practical submicrogram sensitive assay. J Lab Clin Med 1973;81:298.
21. Clauss A. Gerinnungsphysiologische Schnellmethode zur Bestimmung des Fibrinogens. Acta Haematol 1957;17:237.
22. Macfarlane DE, Stibbe J, Kirby EP. A method for assaying von Willebrand factor (Ristocetin cofactor). Thromb Diath Haemorrh 1975;34:306.
23. Basic-Micic M, Roman C, Herpel U, et al. Platelet-induced thrombin generation time: a new sensitive global assay for platelet function and coagulation. Haemostasis 1992;22:309.
24. Basic-Micic M, Breddin HK, Effects of unfractionated and low molecular weight heparins on platelet-induced thrombin generation time and platelet adhesion. Semin Thromb Hemost 1993;19: 22.
25. Radziwon P, Boczkowska-Radziwon B, Schenk JF, Breddin HK. PITT sensitivity to heparin and heparin like compounds. Ann Hematol 1994;68(Suppl):A89.
26. Schenk JE. Plättcheninduzierte Thrombinbildungszeit und Tagesrhythmik. Infusionstherapie und Transfusionsmedizin 1994;348: 109.
27. Schenk JF, Breddin HK, Radziwon P, et al. Influence of hemostatic abnormalities on platelet induced thrombin generation time. Int Angiol 1994;14:340.
28. Breddin HK. Zur Messung der Thrombozytenadhäsivität. Thromb Diath Haemorrh 1964;12:269.
29. Hoppensteadt D, Ahsan A, Walenga JM, Fareed J. Activation of heparin cofactor II by sulfated lactobionic acid. Blood 1988;72: 298.
30. Hoppensteadt DA, Jeske W, Fareed J, Nicolaides AN. Physical and pharmacologic manipulation of the vascular system as measured by the release of TFPI and other mediators of antithrombotic actions. Int Angiol 1996;15:39.
31. Jeske W, Fareed J. Antithrombin III and heparin cofactor II mediated anticoagulant and antiprotease actions of heparin and its synthetic analogues. Semin Thromb Hemost 1993;19:241.
32. Hoppensteadt D, Walenga JM, Fareed J. Protamine sulfate neutralization of lactobionic acid amides. Semin Thromb Hemost 1991;17:153.
33. Fareed J, Coker S, Iqbal O, et al. Pharmacodynamics of a sulfated lactobionic acid amide-derived antithrombotic agent (Aprosulate) in primates. Semin Thromb Hemost 1991;17:147.
34. Sugidachi A, Breiter N, Ogawa T, et al. In vitro effects of aprosulate sodium, a novel anticoagulant, on platelet activation: possible mechanism for antiplatelet action. Thromb Haemost 1996;76:786.
35. Christiansen HM, Lassen MR, Borris LC, et al. Biologic tolerance of two different low molecular weight heparins. Semin Thromb Hemost 1991;17:450.
36. Lambert M, Laterre P-F, Leroy CH, et al. Modifications of liver enzymes during heparin therapy. Acta Clin Belg 1986;41:307.
37. Schwartz KA, Royer G, Kaufman DB, Penner JA. Complications of heparin administration in normal individuals. Am J Hematol 1985;19:355.
38. Dukes GE, Sanders SW, Russo J, et al. Transaminase elevations in patients receiving bovine or porcine heparin. Ann Intern Med 1984; 100:646.
39. Shilo S, Abraham AS, Breuer R, Sonnenblick M. Hypertransaminasemia with subcutaneous heparin therapy. Isr J Med Sci 1981; 17:1133.