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Antimicrobial Agents and Chemotherapy, October 1999, p. 2562-2564, Vol. 43, No. 10
0066-4804/99/$04.00+0
Copyright © 1999, American Society for Microbiology. All rights reserved.

Lipoprotein Distribution of a Novel Endotoxin Antagonist, E5531, in Plasma from Human Subjects with Various Lipid Levels

Kishor M. Wasan,1,* Frank W. Strobel,1 Steven C. Parrott,1 Melvyn Lynn,2 William J. Christ,3 Lynn D. Hawkins,4 and Daniel P. Rossignol4

Faculty of Pharmaceutical Sciences, The University of British Columbia, Vancouver, British Columbia, Canada V6T 1Z31; Eisai, Inc., Teaneck, New Jersey 076662; and Eisai Merrimack Valley3 and Eisai Research Institute, Andover, Massachusetts 018104

Received 4 November 1998/Returned for modification 4 April 1999/Accepted 20 July 1999

The purpose of this study was to determine the distribution profile of a novel endotoxin antagonist, [14C]E5531, at 1 µg/ml in plasma samples obtained from fasted human subjects with various lipid and protein concentrations. Our findings suggest that the majority of E5531 binds with high-density lipoproteins (HDLs) independently of plasma lipid and protein levels tested. Furthermore, it appears that an increase in triglyceride-rich lipoprotein (TRL) lipid and protein levels and an increase in low-density lipoprotein (LDL) lipid levels significantly increase TRL plus LDL binding of E5531. However, only an increase in HDL protein levels significantly increases HDL binding of E5531.

* Corresponding author. Mailing address: Faculty of Pharmaceutical Sciences, The University of British Columbia, 2146 East Mall Ave., Vancouver, B.C., Canada V6T 1Z3. Phone: (604) 822-4889. Fax: (604) 822-3035. E-mail: Kwasan{at}unixg.ubc.ca.

Antimicrobial Agents and Chemotherapy, October 1999, p. 2562-2564, Vol. 43, No. 10
0066-4804/99/$04.00+0
Copyright © 1999, American Society for Microbiology. All rights reserved.


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