Investigating clearance mechanisms for recombinant activated factor VII in a perfused liver model

Thrombosis and Haemostasis

Volumn 104, Issue 2, 2010, Pages 243-251

  Appa, Rupa S ^a   Theill, Charlotte ^a   Hansen, Lene ^a   Møss, Judi ^a   Behrens, Carsten ^a   Nicolaisen, Else Marie ^a   Klausen, Niels K ^a   Christensen, Michael S ^a  

^a NOVO NORDISK A S   (Denmark)

Author keywords

Asialo orosomucoid; Asialo rFVIIa; Asialoglycoprotein receptor (ASGPR); In situ rat liver perfusion; Recombinant activated factor VII (rFVIIa)

Indexed keywords

RECOMBINANT BLOOD CLOTTING FACTOR 7A;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; DOSE TIME EFFECT RELATION; DRUG CLEARANCE; DRUG HALF LIFE; DRUG METABOLISM; ISOLATED LIVER; LIVER METABOLISM; LIVER PERFUSION; NONHUMAN; PRIORITY JOURNAL; RAT; SIALYLATION;

ANIMALS; ASIALOGLYCOPROTEIN RECEPTOR; ASIALOGLYCOPROTEINS; COAGULANTS; FACTOR VIIA; GLYCOSYLATION; HALF-LIFE; HUMANS; INJECTIONS, INTRAVENOUS; LIVER; MALE; METABOLIC CLEARANCE RATE; OROSOMUCOID; PEPTIDE FRAGMENTS; PERFUSION; RATS; RATS, SPRAGUE-DAWLEY; RECOMBINANT PROTEINS;

EID: 77955453031     PISSN: 03406245     EISSN: None     Source Type: Journal    
DOI: 10.1160/TH09-10-0723     Document Type: Article

References (49)

1. Neuenschwander PF, Morrissey JH. Roles of the membrane-interactive regions of factor VIIa and tissue factor. The factor VIIa Gla domain is dispensable for binding to tissue factor but important for activation of factor X. J Biol Chem 1994; 269: 8007-8013.
2. Tranholm M, Kristensen K, Kristensen AT, et al. Improved hemostasis with superactive analogs of factor VIIa in a mouse model of hemophilia A. Blood 2003; 102: 3615-3620.
3. Fuchs HE, Trapp HG, Griffith MJ, et al. Regulation of factor IXa in vitro in human and mouse plasma and in vivo in the mouse. Role of the endothelium and the plasma proteinase inhibitors. J Clin Invest 1984; 73: 1696-1703.
4. Narita M, Rudolph AE, Miletich JP, et al. The low-density lipoprotein receptor-related protein (LRP) mediates clearance of coagulation factor Xa in vivo. Blood 1998; 91: 555-560.
5. Chang GT, Kisiel W. Internalization and degradation of recombinant human coagulation factor VIIa by the human hepatoma cell line HuH7. Thromb Haemost 1995; 73: 231-238.
6. Hjortoe G, Sorensen BB, Petersen LC, et al. Factor VIIa binding and internalization in hepatocytes. Thromb Haemost 2005; 3: 2264-2273.
7. Rao LV, Pendurthi UR. Regulation of tissue factor-factor VIIa expression on cell surfaces: a role for tissue factor-factor VIIa endocytosis. Mol Cell Biochem 2003; 253: 131-140.
8. Rao LV, Pendurthi UR. Factor VIIa binding to endothelial cell protein C receptor. Thromb Res 2008; 122 (Suppl 1): S3-S6.
9. Weeterings C, de Groot PG, Adelmeijer J, et al. The glycoprotein Ib-IX-V complex contributes to tissue factor-independent thrombin generation by recombinant factor VIIa on the activated platelet surface. Blood 2008; 112: 3227-3233.
10. Beeby TL, Chasseaud LF, Taylor T, et al. Distribution of the recombinant coagulation factor 125I-rFVIIa in rats. Thromb Haemost 1993; 70: 465-468.
11. Thomsen MK, Diness V, Nilsson P, et al. Pharmacokinetics of recombinant factor VIIa in the rat--a comparison of bio-, immuno- and isotope assays, Thromb Haemost 1993; 70: 458-464.
12. Seested T, Nielsen HM, Christensen EI, et al. Cellular and intracellular distribution of recombinant activated factor VII in the rat liver. Thromb Haemost 2010; 103: 860-862.
13. Skogh T, Blomhoff R, Eskild W, Berg T. Hepatic uptake of circulating IgG immune complexes. Immunology 1985; 55: 585-594.
14. Moestrup SK, Gliemann J, Pallesen G. Distribution of the alpha 2-macroglobulin receptor/low density lipoprotein receptor-related protein in human tissues. Cell Tissue Res 1992; 269: 375-382.
15. Smedsrod B, Pertoft H, Gustafson S, et al. Scavenger functions of the liver endothelial cell. Biochem J 1990; 266: 313-327.
16. Appa R, Christensen MS. Investigation of human recombinant FVIIa metabolism in a perfused rat liver model. Thromb Haemost 2007; 5 (Suppl 2): P-T-054 Abstract.
17. Nicolaisen EM, Petersen LC, Thim L, et al. Generation of Gla-domainless FVIIa by cathepsin G-mediated cleavage. FEBS Lett 1992; 306: 157-160.
18. Eap CB, Baumann P. Isoelectric focusing of alpha-1 acid glycoprotein (orosomucoid) in immobilized pH-gradients with 8M urea: detection of its desialylated variants using an alkaline phosphatase-linked secondary antibody system. Electrophoresis 1988; 9: 650-654.
19. Behrens C, Garibay PW, Zundel M. Use of galactose oxidase for selective chemical conjugation of protractor molecules to proteins of therapeutic interest. 2005; International Patent application number WO200501435.
20. Meijer DK, Keulemans K, Mulder GJ. Isolated perfused rat liver technique. Meth Enzymol 1981; 77: 81-94.
21. Wolkoff AW, Johansen KL, Goeser T. The isolated perfused rat liver: preparation and application. Anal Biochem 1987; 167: 1-14.
22. Wildgoose P, Nemerson Y, Hansen LL, et al. Measurement of basal levels of factor VIIa in hemophilia A and B patients. Blood 1992; 80: 25-28.
23. Morrissey JH, Macik BG, Neuenschwander PF, et al. Quantitation of activated factor VII levels in plasma using a tissue factor mutant selectively deficient in promoting factor VII activation. Blood 1993; 81: 734-744.
24. Klausen NK, Bayne S, Palm L. Analysis of the site-specific asparagine-linked glycosylation of recombinant human coagulation factor VIIa by glycosidase digestions, liquid chromatography, and mass spectrometry. Mol Biotechnol1998; 9: 195-204.
25. Klausen NK, Kornfelt T. Analysis of the glycoforms of human recombinant factor VIIa by capillary electrophoresis and high-performance liquid chromatography. J Chromatogr A 1995; 718: 195-202.
26. Ashwell G, Harford J. Carbohydrate-specific receptors of the liver. Annu Rev Biochem 1982; 51: 531-554.
27. Baenziger JU, Fiete D. Galactose and N-acetylgalactosamine-specific endocytosis of glycopeptides by isolated rat hepatocytes. Cell 1980; 22: 611-620.
28. Schwartz AL. The hepatic asialoglycoprotein receptor. CRC Crit Rev Biochem 1984; 16: 207-233.
29. Schiff JM, Huling SL, Jones AL. Receptor-mediated uptake of asialoglycoprotein by the primate liver initiates both lysosomal and transcellular pathways. Hepatology 1986; 6: 837-847.
30. Ashwell G, Morell AG. The role of surface carbohydrates in the hepatic recognition and transport of circulating glycoproteins. Adv Enzymol Relat Areas Mol Biol 1974; 41: 99-128.
31. Wall DA , Wilson G, Hubbard AL. The galactose-specific recognition system of mammalian liver: the route of ligand internalization in rat hepatocytes. Cell 1980; 21: 79-93.
32. Wall DA, Hubbard AL. Receptor-mediated endocytosis of asialoglycoproteins by rat liver hepatocytes: biochemical characterization of the endosomal compartments. J Cell Biol 1985; 101: 2104-2112.
33. Morell AG, Gregoriadis G, Scheinberg IH, et al. The role of sialic acid in determining the survival of glycoproteins in the circulation. J Biol Chem 1971; 246:1461-1467.
34. Townsend RR, Wall DA, Hubbard AL, et al. Rapid release of galactose-terminated ligands after endocytosis by hepatic parenchymal cells: Evidence for a role of carbohydrate structure in the release of internalized ligand from receptor. PNAS 1984; 81: 466-470.
35. Pricer Jr. WE, Ashwell G. The binding of desialylated glycoproteins by plasma membranes of rat liver. J Biol Chem 1971; 246: 4825-4833.
36. Jones AJ, Papac DI, Chin EH, et al. Selective clearance of glycoforms of a complex glycoprotein pharmaceutical caused by terminal N-acetylglucosamine is similar in humans and cynomolgus monkeys. Glycobiology 2007; 17: 529-540.
37. Webster R, Taberner J, Edgington A, et al. Role of sialylation in determining the pharmacokinetics of neutrophil inhibitory factor (NIF) in the Fischer 344 rat. Xenobiotica 1999; 29: 1141-1155.
38. Thim L, Bjoern S, Christensen M, et al. Amino acid sequence and posttranslational modifications of human factor VIIa from plasma and transfected baby hamster kidney cells. Biochemistry 1988; 27: 7785-7793.
39. Jurlander B, Thim L, Klausen NK, et al. Recombinant activated factor VII (rFVIIa): Characterization, manufacturing, and clinical development. Semin Thromb Hemost 2001; 27: 373-383.
40. Weigel PH. Endocytosis and function of the hepatic asialoglycoprotein receptor. Subcell Biochem 1993; 19: 125-161.
41. Zeng FY, Oka JA, Weigel PH. A specific antibody to the carbohydrate recognition domain of the asialoglycoprotein receptor RHL1 subunit does not react with RHL2/3 but blocks ligand binding. Bichem Biophys Res Commun 1998; 249: 236-240.
42. Townsend R, Stahl P. Isolation and characterization of a mannose/N-acetylglucosamine/fucose-binding protein from rat liver. Biochem J 1981; 194: 209-214.
43. Pricer Jr. WE, Hudgin RL, Ashwell G, et al. A membrane receptor protein for asialoglycoproteins. Meth Enzymol 1974; 34: 688-691.
44. Thomas P, Summer JW. The biliary excretion of circulating asialoglycoproteins in the rat. Biochem Biophys Res Commun 2009; 80: 335-339.
45. Schiff JM, Fisher MM, Underdown BJ. Receptor-mediated biliary transport of immunoglobulin A and asialoglycoprotein: Sorting and missorting of ligands revealed by two radiolabeling methods. J Cell Biol 1984; 98: 79-89.
46. Thomas P, Toth CA, Zamcheck N. The mechanism of bilary excretion of alpha-1 acid glyco protein in the rat. Gastroenterology 1981; 80: 1302.
47. Iakhiaev A, Pendurthi UR, Voigt J, et al. Catabolism of factor VIIa bound to tissue factor in fibroblasts in the presence and absence of tissue factor pathway inhibitor. J Biol Chem 1999; 274: 36995-37003.
48. Ghosh S, Pendurthi UR, Steinoe A, et al. Endothelial cell protein C receptor acts as a cellular receptor for factor VIIa on endothelium. J Biol Chem 2007; 282: 11849-11857.
49. Fleck RA, Rao LV, Rapaport SI, et al. Localization of human tissue factor antigen by immunostaining with monospecific, polyclonal anti-human tissue factor antibody. Thromb Res 1990; 59: 421-437.