In Vitro Synergy and Enhanced Murine Brain Penetration of Saquinavir Coadministered with Mefloquine

• Published in: The Journal of pharmacology and experimental therapeutics Vol. 314; no. 3; pp. 1202 - 1209
• Main Authors: Owen, Andrew, Janneh, Omar, Hartkoorn, Ruben C, Chandler, Becky, Bray, Patrick G, Martin, Phillip, Ward, Stephen A, Hart, C Anthony, Khoo, Saye H, Back, David J
• Format: Journal Article
• Language: English
• Published: United States American Society for Pharmacology and Experimental Therapeutics 01.09.2005
• Subjects: Antimalarials; ATP-Binding Cassette, Sub-Family B, Member 1 - genetics; Brain - metabolism; Drug Synergism; HIV Protease Inhibitors - pharmacology; HIV-1 - drug effects; Humans; Mefloquine - pharmacology; Membrane Transport Proteins - genetics; Multidrug Resistance-Associated Proteins - genetics; Protein Binding; RNA, Messenger - analysis; Saquinavir - pharmacology; U937 Cells

Highly active antiretroviral therapy has substantially improved prognosis in human immunodeficiency virus (HIV). However, the integration of proviral DNA, development of viral resistance, and lack of permeability of drugs into sanctuary sites (e.g., brain and lymphocyte) are major limitations to cur...