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BY OUR PHARMA CORRESPONDENT 13th
August,2005:GlaxoSmithKline (GSK) announced
that phase III clinical studies with its entry
inhibitor aplaviroc (873140) have commenced in HIV
treatment-experienced patients.
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, the company
said in an official release.
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.
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, investigational compound
640385 is in phase II development as a
next-generation protease inhibitor (PI); and
695634 is in phase II development as a
next-generation non-nucleoside reverse
transcriptase inhibitor (NNRTI). Both compounds
are being evaluated for treatment of those
patients whose virus has become resistant to
multiple antiretroviral drugs.
Aplaviroc is the proposed generic name for 873140.
It was in-licensed for development from Ono
Pharmaceutical Co., Ltd. in December 2002. 640385
was co-discovered with Vertex Pharmaceuticals,
Inc, the GSK release added.
GlaxoSmithKline is one of the world's leading
pharmaceutical and healthcare companies The
company is a leader in 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.
BY OUR PHARMA CORRESPONDENT |
