3rd IAS Conference on HIV Pathogenesis and Treatment
July 24 - 27, 2005, Rio de Janerio, Brazil
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GlaxoSmithKline Begins Phase III Trials of CCR5 Antagonist Aplaviroc GlaxoSmithKline (GSK) announced this week that Phase III trials have begun of the company’s experimental entry inhibitor aplaviroc (formerly 873140). Following is an edited version of the GSK announcement: Entry inhibitors like aplaviroc represent a new mechanism of action in this class of antiretrovirals. They work by binding to one of the chemokine co-receptors, CCR5, on the immune cell surface that is essential for HIV-1 entry and infection. “The availability of an orally administered entry inhibitor may provide an important treatment option for people infected with HIV-1,” commented Dr. Joseph Eron, Professor of Medicine at the University of North Carolina at Chapel Hill and Principal Director of the UNC AIDS Clinical Trials Unit. “It is imperative that companies like GSK continue with their research and development efforts to expand the number of antiretroviral drugs available with different modes of action or improved efficacy and toxicity profiles.” Aplaviroc selectively inhibits the binding of the HIV envelope to the CCR5 co-receptor on the cell surface by producing changes in the receptor conformation via an allosteric mechanism. Allosteric inhibition occurs when an interaction in one region of a protein prevents the function of another part of the protein. This affects the interaction of the virus with the cell, as HIV cannot use the antagonist-bound CCR5 pathway. The viral entry cascade and subsequent infection by CCR5-using HIV are therefore blocked. Aplaviroc is the proposed generic name for 873140, which was in-licensed for development from Ono Pharmaceutical Co., Ltd. in December 2002. Symposium at IAS Highlights GSK Progress in Development of New HIV Therapies GSK also hosted a satellite symposium at the 3rd International AIDS Society (IAS) Conference on HIV Pathogenesis and Treatment in Rio de Janeiro, Brazil highlighting the company’s progress in the development of new treatments for HIV. Antiretroviral drug resistance is a major cause of treatment failure in patients infected with HIV-1 and has been associated with increased mortality. To address the continued need for new anti-HIV drugs, GSK has a number of drugs in development that hope to demonstrate activity against viral strains that are resistant to existing agents. In addition to aplaviroc, the investigational compound 640385 is in Phase II development as a next-generation protease inhibitor (PI); and 695634, which was co-discovered with Vertex Pharmaceuticals, is in Phase II development as a next-generation non-nucleoside reverse transcriptase inhibitor (NNRTI). About GlaxoSmithKline GlaxoSmithKline is one of the world's leading pharmaceutical and healthcare companies and is committed to improving the quality of human life by enabling people to do more, feel better and live longer. GSK is a leader in bringing HIV/AIDS treatments to patients and provides its anti-retrovirals to 64 of the least developed countries and Sub-Saharan Africa at not-for-profit prices. For more information, visit GlaxoSmithKline on the World Wide Web at www.gsk.com Source |
