L-chicoric acid, an inhibitor of human immunodeficiency virus type 1 (HIV-1) integrase, improves on the in vitro anti-HIV-1 effect of Zidovudine plus a protease inhibitor (AG1350).

Important note: Information in this article was accurate in 1999. The state of the art may have changed since the publication date.

L-chicoric acid, an inhibitor of human immunodeficiency virus type 1 (HIV-1) integrase, improves on the in vitro anti-HIV-1 effect of Zidovudine plus a protease inhibitor (AG1350).

Antiviral Res. 1998 Aug;39(2):101-11. Unique Identifier : AIDSLINE MED/99021324
Robinson WE Jr; Department of Pathology, University of California, Irvine,; 92697-4800, USA. ewrobins@uci.edu

Abstract: Combinations of anti-human immunodeficiency virus (HIV) drugs, including reverse transcriptase inhibitors and protease inhibitors, have proven immensely potent in the therapy of acquired immune deficiency syndrome (AIDS). To determine whether HIV integrase is a suitable target for combination therapy, the ability of an HIV integrase inhibitor, L-chicoric acid, to work in combination with a protease inhibitor and Zidovudine was tested in vitro. The addition of L-chicoric acid to either Zidovudine or protease inhibitor improved upon the observed anti-HIV activity of either compound alone. When all three drugs were combined, the anti-HIV activity was substantially better than either of the three compounds alone or any combination of two inhibitors. Doses of both Zidovudine and protease inhibitor could be reduced by more than 33% for an equivalent anti-HIV effect if L-chicoric acid was added. The improved anti-HIV activity was observed with a tissue culture adapted strain of HIV (HIV(LAI)) and with limited passage clinical isolates of HIV (HIV(R19) and HIV(R45)). These data demonstrate that a first generation HIV integrase inhibitor, L-chicoric acid, is at least additive in combination with existing multi-drug regimens and suggest that HIV integrase will be an excellent target for combination therapy of HIV infection.

Keywords: JOURNAL ARTICLE Anti-HIV Agents/*PHARMACOLOGY Drug Synergism HIV Integrase Inhibitors/*PHARMACOLOGY HIV Protease Inhibitors/*PHARMACOLOGY HIV-1/*DRUG EFFECTS Reverse Transcriptase Inhibitors/PHARMACOLOGY Succinates/*PHARMACOLOGY Support, Non-U.S. Gov't Support, U.S. Gov't, P.H.S. Zidovudine/*PHARMACOLOGY
990330
A9930490

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