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Antimicrobial Agents and Chemotherapy, July 2002, p. 2284-2286, Vol. 46, No. 7
0066-4804/02/$04.00+0     DOI: 10.1128/AAC.46.7.2284-2286.2002
Copyright © 2002, American Society for Microbiology. All Rights Reserved.

GF120918, a P-Glycoprotein Modulator, Increases the Concentration of Unbound Amprenavir in the Central Nervous System in Rats

Jeffrey E. Edwards,1 Kenneth R. Brouwer,2 and Patrick J. McNamara1,3*

Graduate Center for Toxicology,1 Department of Pharmaceutical Sciences, University of Kentucky, Lexington, Kentucky,3 Bioanalysis and Drug Metabolism, Glaxo Wellcome, Inc., Research Triangle Park, North Carolina2

Received 31 August 2001/ Returned for modification 5 December 2001/ Accepted 19 March 2002

The goal of this study was to determine the distribution of unbound amprenavir in the central nervous system (CNS) of rats. The concentration of unbound amprenavir in the extracellular fluid of the brain and the blood was examined in the presence and absence of the MDR modulator GF120918 by microdialysis. The brain-to-blood ratio of amprenavir in the absence and presence of GF120918 was found to be significantly different (P < 0.003; 0.076 and 0.617, respectively). The use of the MDR modulator GF120918 could potentially increase the penetration of human immunodeficiency virus protease inhibitors into the CNS.

* Corresponding author. Mailing address: Rose Street, Room 410, College of Pharmacy, University of Kentucky, Lexington, KY 40536-0082. Phone: (859) 257-8656. Fax: (859) 257-7564. E-mail: pmcnamar{at}pop.uky.edu.

Antimicrobial Agents and Chemotherapy, July 2002, p. 2284-2286, Vol. 46, No. 7
0066-4804/02/$04.00+0     DOI: 10.1128/AAC.46.7.2284-2286.2002
Copyright © 2002, American Society for Microbiology. All Rights Reserved.



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