Is thrombin generation the new rapid, reliable and relevant pharmacological tool for the development of anticoagulant drugs?

Pharmacological Research

Volumn 59, Issue 3, 2009, Pages 160-166

  Robert, Séverine ^a   Ghiotto, Jérémie ^b   Pirotte, Bernard ^b   David, Jean Louis ^c   Masereel, Bernard ^a   Pochet, Lionel ^a   Dogné, Jean Michel ^a  

^a UNIVERSITY OF NAMUR   (Belgium)

^b UNIVERSITY OF LIÈGE   (Belgium)

^c UNIVERSITY OF LIÈGE   (Belgium)

Author keywords

Anticoagulant drugs; Thrombin; Thrombin activity profile; Thrombin generation

Indexed keywords

ANTICOAGULANT AGENT; ARGATROBAN; BLOOD CLOTTING FACTOR 10A INHIBITOR; ENOXAPARIN; FONDAPARINUX; LEPIRUDIN; N [2 (5 AMIDINO 2 HYDROXYPHENOXY) 3,5 DIFLUORO 6 [3 (1 METHYL 1H 2 IMIDAZOLIN 2 YL)PHENOXY] 4 PYRIDINYL] N METHYLGLYCINE; THROMBIN INHIBITOR;

ANALYTIC METHOD; ANTICOAGULATION; ARTICLE; CALIBRATED AUTOMATED THROMBOGRAM; CATALYSIS; CONTROLLED STUDY; DOSE RESPONSE; DRUG MECHANISM; DRUG POTENCY; DRUG SCREENING; ENZYME ACTIVITY; EX VIVO STUDY; HUMAN; MALE; MAXIMUM PLASMA CONCENTRATION; NORMAL HUMAN; PARAMETER; PRIORITY JOURNAL; RELIABILITY; REPRODUCIBILITY; SCREENING TEST; TECHNIQUE; THROMBIN TIME; THROMBOCYTE POOR PLASMA; TIME TO MAXIMUM PLASMA CONCENTRATION; VALIDATION STUDY;

ANTICOAGULANTS; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DESIGN; HUMANS; MALE; THROMBIN;

EID: 59349093707     PISSN: 10436618     EISSN: 10961186     Source Type: Journal    
DOI: 10.1016/j.phrs.2008.12.003     Document Type: Article

References (36)

1. Gerotziafas G.T., and Samama M.M. Heterogeneity of synthetic factor Xa inhibitors. Curr Pharm Des 11 (2005) 3855-3876
2. Gross P.L., and Weitz J.I. New anticoagulants for treatment of venous thromboembolism. Arterioscler Thromb Vasc Biol 28 (2008) 380-386
3. Haas S. New oral Xa and IIa inhibitors: updates on clinical trial results. J Thromb Thrombolysis 25 (2008) 52-60
4. Leadley Jr. R.J., Chi L., Rebello S.S., and Gagnon A. Contribution of in vivo models of thrombosis to the discovery and development of novel antithrombotic agents. J Pharmacol Toxicol Methods 43 (2000) 101-116
5. Lin J., Deng H., Jin L., Pandey P., Quinn J., Cantin S., et al. Design, synthesis, and biological evaluation of peptidomimetic inhibitors of factor XIa as novel anticoagulants. J Med Chem 49 (2006) 7781-7791
6. Ye B., Arnaiz D.O., Chou Y.L., Griedel B.D., Karanjawala R., Lee W., et al. Thiophene-anthranilamides as highly potent and orally available factor xa inhibitors(1). J Med Chem 50 (2007) 2967-2980
7. Prasa D., Svendsen L., and Sturzebecher J. The ability of thrombin inhibitors to reduce the thrombin activity generated in plasma on extrinsic and intrinsic activation. Thromb Haemost 77 (1997) 498-503
8. Prasa D., Svendsen L., and Sturzebecher J. Inhibition of thrombin generation in plasma by inhibitors of factor Xa. Thromb Haemost 78 (1997) 1215-1220
9. Macfarlane R.G., and Biggs R. A thrombin generation test: the application in haemophilia and thrombocytopenia. J Clin Pathol 6 (1953) 3-8
10. Pitney W.R., and Dacie J.V. A simple method of studying the generation of thrombin in recalcified plasma: application in the investigation of haemophilia. J Clin Pathol 6 (1953) 9-14
11. Hemker H.C., and Beguin S. Endogenous thrombin potential. In: Jespersen J., Bertina R.M., and Havertake H. (Eds). Laboratory techniques in thrombosis: a manual (1999), Kluwer Academic Publishers, Dordrecht 63-78
12. Hemker H.C., Giesen P., AlDieri R., Regnault V., de Smed E., Wagenvoord R., et al. The calibrated automated thrombogram (CAT): a universal routine test for hyper- and hypocoagulability. Pathophysiol Haemost Thromb 32 (2002) 249-253
13. Kikumoto R., Tamao Y., Tezuka T., Tonomura S., Hara H., Ninomiya K., et al. Selective inhibition of thrombin by (2R,4R)-4-methyl-1-[N2-[(3-methyl-1,2,3,4-tetrahydro-8-quinolinyl+++) sulfonyl]-l-arginyl)]-2-piperidinecarboxylic acid. Biochemistry 23 (1984) 85-90
14. Stone S.R., and Hofsteenge J. Kinetics of the inhibition of thrombin by hirudin. Biochemistry 25 (1986) 4622-4628
15. 2Cl-A selective affinity label for thrombin. Thromb Res 14 (1979) 969-973
16. Weitz J.I. Low-molecular-weight heparins. N Engl J Med 337 (1997) 688-698
17. Adler M., Davey D.D., Phillips G.B., Kim S.H., Jancarik J., Rumennik G., et al. Preparation, characterization, and the crystal structure of the inhibitor ZK-807834 (CI-1031) complexed with factor Xa. Biochemistry 39 (2000) 12534-12542
18. Hemker H.C., Giesen P., Al Dieri R., Regnault V., de Smedt E., Wagenvoord R., et al. Calibrated automated thrombin generation measurement in clotting plasma. Pathophysiol Haemost Thromb 33 (2003) 4-15
19. Hoffman M., and Monroe D.M. A cell-based model of hemostasis. Thromb Haemost 85 (2001) 958-965
20. Mann K.G., Brummel K., and Butenas S. What is all that thrombin for?. J Thromb Haemost 1 (2003) 1504-1514
21. Mann K.G., Butenas S., and Brummel K. The dynamics of thrombin formation. Arterioscler Thromb Vasc Biol 23 (2003) 17-25
22. Collen D., Matsuo O., Stassen J.M., Kettner C., and Shaw E. In vivo studies of a synthetic inhibitor of thrombin. J Lab Clin Med 99 (1982) 76-83
23. Hauptmann J., and Markwardt F. Studies on the anticoagulant and antithrombotic action of an irreversible thrombin inhibitor. Thromb Res 20 (1980) 347-351
24. Markwardt F. Pharmacological approaches to thrombin regulation. Ann NY Acad Sci 485 (1986) 204-214
25. Post J.M., Sullivan M.E., Abendschein D., Ewing J., Hinchman J.W., and Light D.R. Human in vitro pharmacodynamic profile of the selective factor Xa inhibitor ZK-807834 (CI-1031). Thromb Res 105 (2002) 347-352
26. Vacca J.P. New advances in the discovery of thrombin and factor Xa inhibitors. Curr Opin Chem Biol 4 (2000) 394-400
27. Samama M.M., Gerotziafas G.T., Elalamy I., Horellou M.H., and Conard J. Biochemistry and clinical pharmacology of new anticoagulant agents. Pathophysiol Haemost Thromb 32 (2002) 218-224
28. Gerotziafas G.T., Elalamy I., Depasse F., Perzborn E., and Samama M.M. In vitro inhibition of thrombin generation, after tissue factor pathway activation, by the oral, direct factor Xa inhibitor rivaroxaban. J Thromb Haemost 5 (2007) 886-888
29. Hemker H.C., Choay J., and Beguin S. Free factor Xa is on the main pathway of thrombin generation in clotting plasma. Biochim Biophys Acta 992 (1989) 409-411
30. Herault J.P., Bernat A., Pflieger A.M., Lormeau J.C., and Herbert J.M. Comparative effects of two direct and indirect factor Xa inhibitors on free and clot-bound prothrombinase. J Pharmacol Exp Ther 283 (1997) 16-22
31. Gerotziafas G.T., Petropoulou A.D., Verdy E., Samama M.M., and Elalamy I. Effect of the anti-factor Xa and anti-factor IIa activities of low-molecular-weight heparins upon the phases of thrombin generation. J Thromb Haemost 5 (2007) 955-962
32. Petros S., Siegemund T., Siegemund A., and Engelmann L. The effect of different anticoagulants on thrombin generation. Blood Coagul Fibrinol 17 (2006) 131-137
33. Samama M.M., Le Flem L., Guinet C., Gerotziafas G., and Depasse F. Three different patterns of calibrated automated thrombogram obtained with six different anticoagulants. J Thromb Haemost 5 (2007) 2554-2556
34. Singh S.S. Preclinical pharmacokinetics: an approach towards safer and efficacious drugs. Curr Drug Metab 7 (2006) 165-182
35. Wu K.K., and Thiagarajan P. Role of endothelium in thrombosis and hemostasis. Annu Rev Med 47 (1996) 315-331
36. Dager W.E., and White R.H. Argatroban for heparin-induced thrombocytopenia in hepato-renal failure and CVVHD. Ann Pharmacother 37 (2003) 1232-1236