The antithrombotic and anti-inflammatory effects of BCX-3607, a small molecule tissue factor/factor VIIa inhibitor

Thrombosis Research

Volumn 117, Issue 3, 2006, Pages 343-349

  Arnold, C Shane ^a   Parker, Cynthia ^a   Upshaw, Ramanda ^a   Prydz, Hans ^b   Chand, Pooran ^a   Kotian, Pravin ^a   Bantia, Shanta ^a   Babu, Y Sudhakar ^a  

^a BIOCRYST PHARMACEUTICALS INC   (United States)

^b UNIVERSITY OF OSLO   (Norway)

Author keywords

C reactive protein; Factor VII; Interleukin 6; Interleukin 8; Thrombosis; Tissue factor

Indexed keywords

2' [(5 CARBAMIMIDOYLPYRIDIN 2 YLAMINO)METHYL] 4 ISOBUTYLCARBAMOYL 4' VINYLBIPHENYL 2 CARBOXYLIC ACID; ANTICOAGULANT AGENT; ANTIINFLAMMATORY AGENT; BCX 3607; BLOOD CLOTTING FACTOR 7A INHIBITOR; INTERLEUKIN 6; INTERLEUKIN 8; LIPOPOLYSACCHARIDE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIINFLAMMATORY ACTIVITY; ARTICLE; CONTROLLED STUDY; CYTOKINE PRODUCTION; DEEP VEIN THROMBOSIS; DRUG EFFECT; DRUG POTENCY; ENDOTHELIUM CELL; ENDOTOXEMIA; HUMAN; HUMAN CELL; IN VITRO STUDY; KERATINOCYTE; MALE; NONHUMAN; PRIORITY JOURNAL; RAT; THROMBUS; UMBILICAL VEIN;

ANIMALS; ANTI-INFLAMMATORY AGENTS; ATHEROSCLEROSIS; BLOTTING, NORTHERN; CELLS, CULTURED; DISEASE MODELS, ANIMAL; DOSE-RESPONSE RELATIONSHIP, DRUG; ENDOTHELIUM, VASCULAR; ENDOTOXEMIA; FACTOR VIIA; FIBRINOLYTIC AGENTS; HUMANS; INFLAMMATION; INTERLEUKIN-6; INTERLEUKIN-8; KERATINOCYTES; LIPOPOLYSACCHARIDES; MALE; MICE; MODELS, BIOLOGICAL; MODELS, CHEMICAL; PROTHROMBIN TIME; PYRIDINES; RATS; RATS, SPRAGUE-DAWLEY; RNA, MESSENGER; SEPSIS; THROMBOPLASTIN; TIME FACTORS;

EID: 29244487521     PISSN: 00493848     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.thromres.2005.03.015     Document Type: Article

References (32)

1. W. Ruf, and T.S. Edgington Structural biology of tissue factor, the initiator of thrombogenesis in vivo FASEB J 8 1994 385 390
2. W. Konigsberg, D. Kirchofer, M.A. Riederer, and Y. Nemerson The TF:FVIIa complex: clinical significance, structure-function relationships and its role in signaling and metastasis Thromb Haemost 86 2001 757 771
3. E. Camerer, W. Huang, and S.R. Coughlin Tissue factor-and factor X-dependent activation of protease-activated receptor 2 by factor VIIa Proc Natl Acad Sci U S A 97 2000 5255 5260
4. F.B. Taylor, A.C. Chang, G. Peer, A. Li, M. Ezban, and U. Hedner Active site inhibited factor VIIa (DEGR VIIa) attenuates the coagulant and interleukin-6 and-8, but not tumor necrosis factor, responses of the baboon to LD100 Escherichia coli Blood 91 1998 1609 1615
5. A.H.M. Moons, M. Levi, and R.J.G. Peters Tissue factor and coronary artery disease Cardiovasc Res 53 2000 313 325
6. B.H. Annex, S.M. Denning, K.M. Channon, M.H. Sketch Jr., R.S. Stack, and J.H. Morrissey Differential expression of tissue factor protein in directional atherectomy specimens from patients with stable and unstable coronary syndromes Circulation 91 1995 619 622
7. H. Suefuji, H. Ogawa, H. Yasue, K. Kaikita, H. Soejima, and T. Motoyama Increased plasma tissue factor levels in acute myocardial infarction Am Heart J 134 1997 253 259
8. K. Misumi, H. Ogawa, H. Yasue, H. Soejima, H. Suefuji, and K. Nishiyama Comparison of plasma tissue factor levels in unstable and stable angina pectoris Am J Cardiol 81 1998 22 26
9. J.J. Badimon, M. Lettino, V. Toschi, V. Fuster, M. Berrozpe, and J.H. Chesebro Local inhibition of tissue factor reduces the thrombogenicity of disrupted human atherosclerotic plaques: effects of tissue factor pathway inhibitor on plaque thrombogenicity under flow conditions Circulation 14 1999 1780 1787
10. R.A. Santucci, J. Erlich, J. Labriola, M. Wilson, K.J. Kao, and T.S. Kickler Measurement of tissue factor activity in whole blood Thromb Haemost 83 2000 445 554
11. U. Ganter, R. Arcone, C. Toniatti, G. Morrone, and G. Ciliberto Dual control of C-reactive protein gene expression by interleukin-1 and interleukin-6 EMBO J 8 1989 3773 3779
12. B. Weinhold, and U. Ruther Interleukin-6-dependent and independent regulation of the human C-reactive protein gene Biochem J 327 1997 425 429
13. P.M. Ridker, C.H. Hennekens, J.E. Buring, and N. Rifai C-reactive reactive protein and other markers of inflammation in the prediction of cardiovascular cardiovascular disease in women N Engl J Med 342 2000 836 843
14. M.A. Albert, and P.M. Ridker The role of C-reactive protein in cardiovascular disease risk Curr Cardiol Rep 2 1999 99 104
15. K.O. Pietila, A.P. Harmoinen, J. Jokiniitty, and A.I. Pasternack Serum C-reactive protein concentration in acute myocardial infarction and its relationship to mortality during 24 months of follow-up in patients under thrombolytic treatment Eur Heart J 9 1996 1345 1349
16. H. Danenberg, A. Szalai, R. Swaminathan, L. Peng, Z. Chen, and P. Siefert Increased arterial thrombosis in human C-reactive protein transgenic mice Circulation 108 5 2003 512 515
17. P. Kotian, P. Chand, Y.S. Babu, S. Bantia, S.N. Gupta, and R. Krishnan Drugs Future 29 2004 (SA) 179: XVIIIth Symp. on MEDICINAL CHEMISTRY
18. D.P. Thomas Venous thrombosis and the "Wessler test" Thromb Haemost 76 1996 1 4
19. E. Camerer, E. Gjernes, M. Wiiger, S. Pringle, and H. Prydz Binding of factor VIIa to tissue factor on keratinocytes induces gene expression J Biol Chem 275 2000 6580 6585
20. X. Wang, E. Gjernes, and H. Prydz Factor VIIa induces tissue factor-dependent up-regulation of interleukin-8 in a human keratinocyte line J Biol Chem 277 2002 23620 23626
21. A.K. Salyers, J.A. Szalony, O.D. Suleymanov, J.J. Parlow, R.S. Wood, and M.S. South Assessment of bleeding propensity in non-human primates by combination of selective tissue factor/factor/VIIa inhibition and aspirin compared to warfarin and aspirin treatment Pharmacology 70 2004 100 106
22. K. Malm, B. Dahlback, and B. Arnljots Low-molecular-weight heparin (Dalteparin) effectively prevents thrombosis in a rat model of deep arterial injury Plastic and Reconstructive Surgery 111 2003 1659 1666
23. O.D. Suleymanov, J.A. Szalony, A.K. Salyers, R.M. LaChance, J.J. Parlow, and M.S. South Pharmacological interruption of acute thrombus formation with minimal hemorrhagic complications by a small molecule tissue factor/factor VIIa inhibitor: comparison to factor Xa and thrombin inhibition in a nonhuman primate thrombosis model J Pharmacol Exp Ther 306 3 2003 1115 1121
24. E. De Jonge, P.W. Friederich, G.P. Vlasuk, W.E. Rote, M.B. Vroom, and M. Levi Activation of coagulation of recombinant factor VIIa elicits interleukin 6 (IL-6) and IL-8 release in healthy human volunteers Clin Diagn Lab Immunol 10 2003 495 497
25. L.M. Biasucci, G. Liuzzo, G. Fantuzzi, G. Caligiuri, A.G. Rebuzzi, and F. Ginnetti Increasing levels of interleukin (IL)-1Ra and IL-6 during the first 2 days of hospitalization in unstable angina are associated with increased risk of in-hospital coronary events Circulation 99 16 1999 2079 2084
26. A. Scholin, A. Siegbahn, L. Lind, C. Berne, G. Sundkvist, and E. Bjork CRP and IL-6 concentrations are associated with poor glycemic control despite preserved beta-cell function during the first year after diagnosis of type 1 diabetes Diabetes Metab Res Rev 20 3 2000 205 210
27. J.A. DiVietro, M.J. Smith, B.R. Smith, L. Petruzzelli, R.S. Larson, and M.B. Lawrence Immobilized IL-8 triggers progressive activation of neutrophils rolling in vitro on P-selectin and intercellular adhesion molecule-1 J Immunol 167 2001 4017 4025
28. E.M. Boyle Jr., J.C. Kovacich, C.A. Hebert, T.G. Canty Jr., E. Chi, and E.N. Morgan Inhibition of interleukin-8 blocks myocardial ischemia-reperfusion injury J Thorac Cardiovasc Surg 116 1998 114 121
29. P. Libby, P.M. Ridker, and A. Maseri Inflammation and atheosclerosis Circulation 105 2002 1135 1143
30. G. Liuzzo, L.M. Biasucci, J.R. Gallimore, R.L. Grillo, A.G. Rebuzzi, and M.B. Pepys N Engl J Med 331 1994 417 424
31. X. Han, T.J. Girard, P. Baum, D.R. Abendschein, and G.J. Broze Jr. Structural requirements for the TFPI-mediated inhibition of neointimal thickening after balloon injury in the rat Arterioscler Thromb Vasc Biol 19 1999 2563 2567
32. R.L. Whisler, V.K. Proctor, E.C. Downs, and R.F. Mortensen Modulation of human monocyte chemotaxis and procoagulant activity by human C-reactive protein (CRP) Lymphokine Res 5 1986 223 228