Influence of plasma cholesterol and triglyceride concentrations and eritoran (E5564) micelle size on its plasma pharmacokinetics and ex vivo activity following single intravenous bolus dose into healthy female rabbits

Pharmaceutical Research

Volumn 25, Issue 1, 2008, Pages 176-182

  Wasan, Kishor M ^a   Risovic, Verica ^a   Sivak, Olena ^a   Lee, Stephen D ^a   Mason, Douglas X ^d   Chiklis, Gregory R ^d   McShane, Jim ^b   Lynn, Melvyn ^b   Wong, Nancy ^c   Rossignol, Daniel P ^b  

^a UNIVERSITY OF BRITISH COLUMBIA   (Canada)

^b EISAI INC   (United States)

^c EISAI RESEARCH INSTITUTE   (United States)

^d ZeptoMetrix Corporation   (United States)

Author keywords

Cholesterol; E5564; Eritoran; Micelle particle size; Pharmacokinetics; Rabbits; TNF ; Triglycerides

Indexed keywords

CHOLESTEROL; ERITORAN; LIPOPOLYSACCHARIDE; TRIACYLGLYCEROL; TUMOR NECROSIS FACTOR ALPHA;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; BLOOD ANALYSIS; BLOOD SAMPLING; CHOLESTEROL BLOOD LEVEL; CHOLESTEROL DIET; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG ACTIVITY; DRUG FORMULATION; FEMALE; HYDRODYNAMICS; LIQUID CHROMATOGRAPHY; MASS SPECTROMETRY; MATHEMATICAL ANALYSIS; MICELLE; NONHUMAN; PLASMA CLEARANCE; PRIORITY JOURNAL; SINGLE DRUG DOSE; TRIACYLGLYCEROL BLOOD LEVEL;

ANIMALS; AREA UNDER CURVE; CHOLESTEROL; CHOLESTEROL, HDL; CHOLESTEROL, LDL; DISACCHARIDES; DOSE-RESPONSE RELATIONSHIP, DRUG; ENZYME-LINKED IMMUNOSORBENT ASSAY; FEMALE; INJECTIONS, INTRAVENOUS; MICELLES; PARTICLE SIZE; RABBITS; SUGAR PHOSPHATES; TRIGLYCERIDES; TUMOR NECROSIS FACTOR-ALPHA;

EID: 38049098060     PISSN: 07248741     EISSN: 1573904X     Source Type: Journal    
DOI: 10.1007/s11095-007-9428-8     Document Type: Article

References (24)

1. X. Du, A. Poltorak, M. Silva, and B. Beutler. Analysis of Tlr4-mediated LPS signal transduction in macrophages by mutational modification of the receptor. Blood Cells Mol. Dis. 25:328-338 (1999).
2. S. K. Huang, K. D. Lee, K. Hong, D. S. Friend, and D. Papahadjopoulos Microscopic localization of sterically stabilized liposomes in colon-carcinoma-bearing mice. Cancer Res. 52:5135-5143 (1992).
3. K. Kaneko, R. Ueda, K. Kikuchi, Y. Sano, and T. Yoshimura. Quantitative determination of a potent lipopolysaccharide antagonist, E5564, in rat and dog plasma by high-performance liquid chromatography with fluorescence detection. J. Chromatogr. B Biomed. Sci. Appl. 736:67-75 (1999).
4. M. Lynn, D. P. Rossignol, J. L. Wheeler, R. J. Kao, C. A. Perdomo, R. Noveck, R. Vargas, T. D'Angelo, S. Gotzkowsky, and F. G. McMahon. Blocking of responses to endotoxin by E5564 in healthy volunteers with experimental endotoxemia. J. Infect. Dis. 187:631-639 (2003).
5. M. Mullarkey, J. R. Rose, J. Bristol, T. Kawata, A. Kimura, S. Kobayashi, M. Przetak, J. Chow, F. Gusovsky, W. J. Christ, and D. P. Rossignol. Inhibition of endotoxin response by E5564, a novel toll-like receptor 4-directed endotoxin antagonist. J. Pharmacol. Exp. Ther. 304:1093-1102 (2003).
6. F. Norido, A. Zatta, C. Fiorito, M. Prosdocimi, and G. Weber. Hematologic and biochemical analysis profiles of selectively bred WHHL rabbits. Lab. Anim. Sci. 43:319-323 (1993).
7. N. M. O'Meara, R. A. Devery, D. Owens, P. B. Collins, A. H. Johnson, and G. H. Tomkin. Serum lipoproteins and cholesterol metabolism in two hypercholesterolemic rabbit models. Diabetologia. 34:139-143 (1991).
8. S. M. Opal, P. J. Scannon, J. L. Vincent, et al. Relationship between plasma levels of lipopolysaccharide (LPS) and LPS-binding protein in patients with severe sepsis and septic shock. J. Infect. Dis. 180:1584-1589 (1999).
9. A. Poltorak, X. He, I. Smirnova, M. Y. Liu, C. V. Huffel, X. Du, D. Birdwell, E. Alejos, M. Silva, C. Galanos, M. Freudenberg, P. Ricciardi-Castagnoli, B. Layton, and B. Beutler. Defective LPS signaling in C3H/HeJ and C57BL/10ScCr mice: mutations in Tlr4 gene. Science. 282:2085-2088 (1998).
10. M. Ramaswamy, T. L. Wallace, P. A. Cossum, and K. M. Wasan. Species differences in the proportion of plasma lipoprotein lipid carried by high-density lipoproteins influence the distribution of free and liposomal nystatin in human, dog, and rat plasma. Antimicrob. Agents Chemother. 43:1424-1428 (1999).
11. J. R. Rose, W. J. Christ, J. R. Bristol, T. Kawata, and D. P. Rossignol. Agonistic and antagonistic activities of bacterially derived Rhodobacter sphaeroides lipid A: comparison with activities of synthetic material of the proposed structure and analogs. Infect. Immun. 63:833-839 (1995).
12. J. R. Rose, M. A. Mullarkey, W. J. Christ, L. D. Hawkins, M. Lynn, Y. Kishi, K. M. Wasan, K. Peteherych, and D. P. Rossignol. Consequences of interaction of a lipophilic endotoxin antagonist with plasma lipoproteins. Antimicrob. Agents Chemother. 44:504-510 (2000).
13. D. P. Rossignol, W. J. Christ, L. D. Hawkins, S. Kobayashi, T. Kawata, M. Lynn, I. Yamatsu, and Y. Kishi. Synthetic endotoxin antagonists. In H. Brade, S. M. Opal, S. N. Vogel, and D. C. Morrison (eds.), Endotoxin in Health and Disease. Marcel Dekker, New York, 1999, pp. 699-717.
14. D. P. Rossignol, and M. Lynn. Antagonism of in vivo and ex vivo response to endotoxin by E5564, a novel synthetic lipid A antagonist. J. Endotoxin Res. 8:483-488 (2003).
15. D. P. Rossignol, K. M. Wasan, E. Choo, E. Yau, N. Wong, J. Rose, J. Moran, and M. Lynn. Safety, pharmacokinetics, pharmacodynamics, and plasma lipoprotein distribution of eritoran (E5564) during continuous intravenous infusion into healthy volunteers. Antimicrob. Agents Chemother. 48:3233-3240 (2004).
16. A. Suganuma, D. P. Rossignol, K. Kaneko, A. W. LaRochelle, and W. D. Kerns. Clinical pharmacology of E5564, a lipid A antagonist, in a canine lipopolysaccharide challenge model. J. Endotoxin Res. 6:115 (2000).
17. T. J. Walsh, J. Bacher, and P. A. Pizzo. Chronic silastic central venous catherization for reduction, maintenance and support of persistent granulocytopenia in rabbits. Lab. Anim. Sci. 38:467-471 (1988).
18. K. M. Wasan, and S. M. Cassidy. Role of plasma lipoproteins in modifying the biological activity of hydrophobic drugs. J. Pharm. Sci. 87:411-424 (1998).
19. K. M. Wasan, S. M. Cassidy, M. Ramaswamy, A. Kennedy, F. W. Strobel, S. P. Ng, and T. Y. Lee. A comparison of step-gradient and sequential density ultracentrifugation and the use of lipoprotein deficient plasma controls in determining the plasma lipoprotein distribution of lipid-associated nystatin and cyclosporine. Pharm. Res. 16:165-169 (1999a).
20. K. M. Wasan, P. H. Pritchard, M. Ramaswamy, W. Wong, E. M. Donnachie, and L. J. Brunner. Differences in lipoprotein lipid concentration and composition modify the plasma distribution of cyclosporine. Pharm. Res. 14:1613-1620 (1997).
21. K. M. Wasan, O. Sivak, R. Cote, A. M. MacInnes, K. D. Boulanger, M. Lynn, W. J. Christ, L. D. Hawkins, and D. P. Rossignol. Association of E5564, an endotoxin antagonist, with high-density lipoproteins in vitro: dependence on low-density and triglyceride-rich lipoprotein concentration. Antimicrob. Agents Chemother. 47:2796-2803 (2003).
22. K. M. Wasan, F. W. Strobel, S. C. Parrott, M. Lynn, W. J. Christ, L. D. Hawkins, and D. P. Rossignol. Lipoprotein distribution of a novel endotoxin antagonist, E5531, in plasma from human subjects with various lipid levels. Antimicrob. Agents Chemother. 43:2562-2564 (1999b).
23. Y. N. Wong, D. Rossignol, J. R. Rose, R. Kao, A. Carter, and M. Lynn. Safety, pharmacokinetics and pharmacodynamics of E5564, a lipid A antagonist, during an ascending single-dose clinical study. J. Clin. Pharmacol. 43:735-742 (2003).
24. J. H. Zar. Multiple regression and correlation in biostatistical analysis. Prentice-Halls, Englewood, NJ, 1984.