NEW YORK (Reuters Health) - Findings from a new study provide evidence that an experimental integrase inhibitor, denoted L-870812, can suppress retroviral replication in vivo.
In an earlier study, Dr. Daria J. Hazuda and colleagues, from Merck Research Laboratories in West Point, Pennsylvania, had shown that inhibition of HIV integrase was an effective method of blocking viral replication in vitro (see Reuters Health report January 28, 2000).
As reported in the July 8th online issue of Science, Dr. Hazuda’s team tested the efficacy of L-870812 in rhesus macaques infected with simian-human immunodeficiency virus (SHIV).
When given before CD4+ cells were depleted, treatment with L-870812 effectively suppressed viral levels, allowing induction of SHIV-specific cell-mediated immunity, the investigators report. Although the agent also showed activity during chronic infection, the magnitude of effect depended on the viral load and the pretreatment immune response.
The new drug, which was given in an oral formulation, was well tolerated, and no toxic effects were observed in any of the animals, according to the report.
The current findings provide “the first evidence of in vivo efficacy for integrase inhibitors in retroviral infections, demonstrating integrase inhibitors can be engineered with the appropriate properties required for an effective therapy to treat chronic HIV-1 infection,” the authors state.
Source: Science 2004. [ Google search on this article ]
MeSH Headings:DNA Nucleotidyltransferases: Enzyme Inhibitors: Enzymes, Coenzymes, and Enzyme Inhibitors: Nucleotidyltransferases: Phosphotransferases: Retroviridae Proteins: Viral Core Proteins: Viral Proteins: Viral Structural Proteins: Gene Products, pol: Integrase: HIV Integrase: HIV Integrase Inhibitors: Integrase Inhibitors: Nucleocapsid Proteins: Chemical Actions and Uses: Chemical Actions: Polyproteins: Chemicals and DrugsCopyright © 2002 Reuters Limited. All rights reserved. Republication or redistribution of Reuters content, including by framing or similar means, is expressly prohibited without the prior written consent of Reuters. Reuters shall not be liable for any errors or delays in the content, or for any actions taken in reliance thereon. Reuters and the Reuters sphere logo are registered trademarks and trademarks of the Reuters group of companies around the world.