Clearance of rFVIIa and NN1731 after intravenous administration to Beagle dogs

European Journal of Pharmaceutical Sciences

Volumn 42, Issue 5, 2011, Pages 578-583

  Agersø, Henrik ^a   Kristensen, Niels Rode ^a   Østergaard, Henrik ^a   Karpf, Ditte Maria ^a   Hermit, Mette Brunsgaard ^a   Pelzer, Hermann ^a   Petersen, Lars Christian ^a   Ezban, Mirella ^a  

^a NOVO NORDISK A S   (Denmark)

Author keywords

Antithrombin; Clearance; Modelling; NN1731; Pharmacokinetics; rFVIIa

Indexed keywords

ANTIGEN; ANTITHROMBIN; BLOOD CLOTTING FACTOR 7A; BLOOD CLOTTING FACTOR 7A ANTIGEN; NN 1731; RECOMBINANT BLOOD CLOTTING FACTOR 7A; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANTIGEN ANTIBODY COMPLEX; ARTICLE; BLOOD CLOTTING; BLOOD SAMPLING; COMPLEX FORMATION; CONTROLLED STUDY; DOG; DRUG CLEARANCE; DRUG HALF LIFE; NONHUMAN; PRIORITY JOURNAL; SINGLE DRUG DOSE;

ANIMALS; ANTITHROMBIN PROTEINS; BLOOD COAGULATION; DATA INTERPRETATION, STATISTICAL; DOGS; FACTOR VII; FACTOR VIIA; HALF-LIFE; INJECTIONS, INTRAVENOUS; METABOLIC CLEARANCE RATE; MODELS, BIOLOGICAL; RECOMBINANT PROTEINS;

EID: 79954629839     PISSN: 09280987     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejps.2011.02.013     Document Type: Article

References (32)

1. H. Agerso, D.F. Brophy, H. Pelzer, E.J. Martin, M. Carr, U. Hedner, and M. Ezban Recombinant human factor VIIa (rFVIIa) cleared principally by antithrombin following IV administration in haemophilia patients J. Thromb. Haemost. 9 Feb (2) 2011 333 338 10.1111/j.1538-7836.2010.04152.x
2. G.A. Allen, E. Persson, R.A. Campbell, M. Ezban, U. Hedner, and A.S. Wolberg A variant of recombinant factor VIIa with enhanced procoagulant and antifibrinolytic activities in an in vitro model of hemophilia Arterioscler. Thromb. Vasc. Biol. 27 March (3) 2007 683 689
3. T.L. Beeby, L.F. Chasseaud, T. Taylor, and M.K. Thomsen Distribution of the recombinant coagulation factor 125I-rFVIIa in rats Thromb. Haemost. 70 September (3) 1993 465 468 (Pubitemid 23254677)
4. H. Boxenbaum Interspecies scaling, allometry, physiological time, and the ground plan of pharmacokinetics J. Pharmacokinet. Biopharm. 10 April (2) 1982 201 227 (Pubitemid 12044187)
5. R. Gopalakrishnan, U. Hedner, S. Ghosh, R.C. Nayak, T.C. Allen, U.R. Pendurthi, and L.V. Rao Bio-distribution of pharmacologically administered recombinant factor VIIa (rFVIIa) J. Thromb. Haemost. 8 February (2) 2010 301 310
6. U. Hedner, and M. Ezban Tissue factor and factor VIIa as therapeutic targets in disorders of hemostasis Annu. Rev. Med. 59 2008 29 41 (Pubitemid 351287922)
7. M. Hoffman, and D.M. Monroe III. The action of high-dose factor VIIa (FVIIa) in a cell-based model of hemostasis Semin. Hematol. 38 October (4 Suppl. 12) 2001 6 9 (Pubitemid 33123950)
8. M. Hoffman, E. Persson, M. Ezban, and D.M. Monroe Platelet binding of NN1731, a Factor VIIa variant with enhanced tissue factor-independent activity. 2010 p. 37 Proceedings, Haemophilia World Congress Buenos Aires, Argentina 2010
9. H.L. Holmberg, B. Lauritzen, M. Tranholm, and M. Ezban Faster onset of effect and greater efficacy of NN1731 compared with rFVIIa, aPCC and FVIII in tail bleeding in hemophilic mice J. Thromb. Haemost. 7 September (9) 2009 1517 1522
10. P.B. Johansen, S.E. Bjorn, H. Agerso, I. Thorup, M.B. Hermit, B. Sorensen, H.R. Stennicke, M. Ezban, and M. Tranholm Prolonged effect of GlycoPEGylated rFVIIa (40 k-PEG-rFVIIa) in rabbits correlates to activity in plasma Thromb. Haemost. 104 April (1) 2010
11. T. Klitgaard, R. Palacios, K.D. Boffard, P.T. Iau, B. Warren, S. Rizoli, R. Rossaint, Y. Kluger, and B. Riou Pharmacokinetics of recombinant activated factor VII in trauma patients with severe bleeding Crit. Care 10 4 2006 R104
12. J.H. Lawson, S. Butenas, N. Ribarik, and K.G. Mann Complex-dependent inhibition of factor VIIa by antithrombin III and heparin J. Biol. Chem. 268 January (2) 1993 767 770 (Pubitemid 23019699)
13. D.E. Mager, and W.J. Jusko General pharmacokinetic model for drugs exhibiting target-mediated drug disposition J. Pharmacokinet. Pharmacodyn. 28 December (6) 2001 507 532 (Pubitemid 34289541)
14. D.M. Monroe, M. Hoffman, J.A. Oliver, and H.R. Roberts Platelet activity of high-dose factor VIIa is independent of tissue factor Br. J. Haematol. 99 December (3) 1997 542 547 (Pubitemid 27519853)
15. J.H. Morrissey, B.G. Macik, P.F. Neuenschwander, and P.C. Comp Quantitation of activated factor VII levels in plasma using a tissue factor mutant selectively deficient in promoting factor VII activation Blood 81 3 1993 734 744 (Pubitemid 23040866)
16. J. Moss, B. Scharling, M. Ezban, and S.T. Moller Evaluation of the safety and pharmacokinetics of a fast-acting recombinant FVIIa analogue, NN1731, in healthy male subjects J. Thromb. Haemost. 7 February (2) 2009 299 305
17. O.H. Olsen, K.D. Rand, H. Ostergaard, and E. Persson A combined structural dynamics approach identifies a putative switch in factor VIIa employed by tissue factor to initiate blood coagulation Protein Sci. 16 April (4) 2007 671 682 (Pubitemid 46506996)
18. S.T. Olson, P.E. Bock, J. Kvassman, J.D. Shore, D.A. Lawrence, D. Ginsburg, and I. Bjork Role of the catalytic serine in the interactions of serine proteinases with protein inhibitors of the serpin family. Contribution of a covalent interaction to the binding energy of serpin-proteinase complexes J. Biol. Chem. 270 December (50) 1995 30007 30017
19. S.T. Olson, R. Swanson, E. Raub-Segall, T. Bedsted, M. Sadri, M. Petitou, J.P. Herault, J.M. Herbert, and I. Bjork Accelerating ability of synthetic oligosaccharides on antithrombin inhibition of proteinases of the clotting and fibrinolytic systems. Comparison with heparin and low-molecular-weight heparin Thromb. Haemost. 92 November (5) 2004 929 939 (Pubitemid 39545514)
20. E. Persson, and L.S. Nielsen Site-directed mutagenesis but not gamma-carboxylation of Glu-35 in factor VIIa affects the association with tissue factor FEBS Lett. 385 May (3) 1996 241 243
21. E. Persson, M. Kjalke, and O.H. Olsen Rational design of coagulation factor VIIa variants with substantially increased intrinsic activity Proc. Natl. Acad. Sci. U.S.A. 98 November (24) 2001 13583 13588 (Pubitemid 33115941)
22. E. Persson, H. Bak, A. Ostergaard, and O.H. Olsen Augmented intrinsic activity of Factor VIIa by replacement of residues 305, 314, 337 and 374: evidence of two unique mutational mechanisms of activity enhancement Biochem. J. 379 April (Pt 2) 2004 497 503 (Pubitemid 38570123)
23. E. Persson, G. Bolt, T.D. Steenstrup, and M. Ezban Recombinant coagulation factor VIIa - from molecular to clinical aspects of a versatile haemostatic agent Thromb. Res. December 2009
24. L.C. Petersen, T. Elm, M. Ezban, T.N. Krogh, D.M. Karpf, A. Steino, E.H. Olsen, and B.B. Sorensen Plasma elimination kinetics for factor VII are independent of its activation to factor VIIa and complex formation with plasma inhibitors Thromb. Haemost. 101 May (5) 2009 818 826
25. L.C. Petersen, D.M. Karpf, H. Agerso, M.B. Hermit, H. Pelzer, E. Persson, T. Nichols, and M. Ezban Intravascular inhibition of factor VIIa and the analogue NN1731 by antithrombin Br. J. Haematol. 2010
26. R Development Core Team, 2009. R: A Language and Environment for Statistical Computing. R Foundation for Statistical Computing. Available from: http://www.R-project.org.
27. L.V. Rao, and U.R. Pendurthi Factor VIIa binding to endothelial cell protein C receptor Thromb. Res. 122 Suppl. 1 2008 S3 S6
28. T. Seested, H.M. Nielsen, E.I. Christensen, and R.S. Appa Cellular and intracellular distribution of recombinant activated factor VII in the rat liver Thromb. Haemost. 103 February (4) 2010
29. H. Tang, and M. Mayersohn A global examination of allometric scaling for predicting human drug clearance and the prediction of large vertical allometry J. Pharm. Sci. 95 August (8) 2006 1783 1799 (Pubitemid 44229585)
30. I. Tarnow, T. Falk, A. Tidholm, T. Martinussen, A.L. Jensen, L.H. Olsen, H.D. Pedersen, and A.T. Kristensen Hemostatic biomarkers in dogs with chronic congestive heart failure J. Vet. Intern. Med. 21 May (3) 2007 451 457 (Pubitemid 46814192)
31. P. Wildgoose, Y. Nemerson, L.L. Hansen, F.E. Nielsen, S. Glazer, and U. Hedner Measurement of basal levels of factor VIIa in hemophilia A and B patients Blood 80 1 1992 25 28
32. M. Zaar, N.H. Secher, P.I. Johansson, B. Vainer, M. Ezban, H. Agerso, P.L. Madsen, N. Lomholt, M.B. Hermit, and B. Lauritzen Effects of a recombinant FVIIa analogue, NN1731, on blood loss and survival after liver trauma in the pig Br. J. Anaesth. 103 December (6) 2009 840 847