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Vertex
Pharmaceuticals Receives U.S. Patent Covering Assay Technology to Accelerate
Drug Discovery Targeting Hepatitis C Protease
CAMBRIDGE, Mass., Oct. 2 /PRNewswire/ -- Vertex Pharmaceuticals Incorporated
(Nasdaq: VRTX) announced today that it has received a patent from the
United States Patent and Trademark Office for a novel technology to screen
compounds for activity against hepatitis C virus (HCV) protease, using
a cell- based assay. The invention is a proprietary tool that can be used
to accelerate the discovery of HCV protease inhibitors for the treatment
of HCV infection, and is broadly applicable for drug discovery against
other protease enzyme targets as well. The Patent Number is 6,117,639.
To date, efforts to grow HCV robustly and reproducibly in cultured cells,
in the test tube or in an animal model have not been successful. This
has hampered efforts industry-wide to screen compounds for direct activity
against HCV, especially HCV protease inhibitors. HCV infection is recognized
as a major threat to public health, and no drugs exist that directly and
potently block HCV viral replication.
"Working together, our virology and cell biology groups developed
a way to measure HCV protease activity in a cell-based assay," said
Vicki Sato, Ph.D., Senior Vice President of Research and Development and
Chief Scientific Officer of Vertex. "Using recombinant DNA techniques,
our researchers have created a fusion protein that, when cut by the hepatitis
C NS3-4A serine protease, will alter expression of a reporter gene in
a highly quantifiable way. This new assay has made it possible to rapidly
screen for compounds that may have direct antiviral activity in a cellular
environment. Already, we have been able to advance several potent small
molecule HCV protease inhibitors into pharmacokinetic evaluation, and
we could select a drug development candidate as early as 2001."
The hepatitis C NS3-4A serine protease is a virally encoded enzyme generally
believed to be essential for replication of HCV. Vertex researchers solved
the three-dimensional atomic structure of HCV protease and reported the
results in the journal Cell in 1996. Vertex is collaborating with Eli
Lilly to discover, develop, and commercialize HCV protease inhibitors
for the treatment of HCV infection. As part of ongoing discovery efforts,
Vertex is focused on creating novel assays
and techniques to help evaluate potential HCV protease inhibitors.
HCV causes inflammation of the liver, which may lead to cirrhosis, liver
failure, and liver cancer. Approximately 2.7 million people in the United
States are chronically infected with the hepatitis C virus, although many
are currently undiagnosed. According to the Centers for Disease Control,
hospitalization and death rates due to HCV are projected to triple from
current levels over the next 10 to 15 years.
Broad Application of Patent For Protease Targets
Vertex's Patent No. 6,117,639 claims a novel method for determining activity
of inhibitory drug candidates against a protease. Vertex's method uses
a multi-domain fusion protein comprised of a protease cleavage site and
is used to monitor protease activity in a cell via a reporter gene expression
system. In the presence of a protease, such as the hepatitis C NS3-4A
serine protease, the expression of a reporter gene is significantly reduced.
As a result, Vertex can measure the activity of an HCV protease inhibitor
by the inhibitor's ability to increase the expression of the reporter
gene in the presence of that protease. The claimed method is applicable
to the discovery of chemical compounds targeting any protease.
Proteases function by cleaving and activating proteins, and play an important
role in the regulation of numerous biological processes, including viral
replication and activation of the immune response.
Proteases have been implicated as contributors to several diseases, including
Alzheimer's disease, hypertension, cancer and viral infections.
There are numerous examples of marketed drugs that achieve a therapeutic
effect by inhibiting protease activity, including HIV protease inhibitors
for the treatment of HIV and AIDS, and angiotensin converting enzyme (ACE)
inhibitors for the treatment of hypertension.
"In addition to the hepatitis C NS3-4A serine protease, this patent
broadly applies to other proteases, including those which may be the subject
of Vertex drug discovery efforts. As part of our chemogenomics approach
to drug discovery, we are seeking to develop proprietary technologies
that we can integrate into our drug discovery platform, with particular
emphasis on technologies that enhance our ability to pursue drug design
across families of related protein targets," said Sato.
Vertex's approach to drug discovery, termed "chemogenomics,"
seeks to capitalize on the emergence of large amounts of genomic information
by combining medicinal chemistry and molecular biology to identify and
describe many of the possible drug candidates for a drug target or group
of targets. As part of this approach, Vertex is pursuing a strategy of
parallel drug design in gene families, which are groups of genes with
similar sequences that code for structurally similar proteins. Vertex's
most advanced efforts in parallel drug design are in the caspase, kinase
and protease gene families. Proteases are of strong interest because of
the structural similarity among specific proteases, the proven medical
value of blocking protease activity with small molecule inhibitors, and
the role that proteases play in a range of diseases.
The inventors of the patent are Drs. Thomas Hoock, Ann Kwong, and Ursula
Germann, all of Vertex.
Vertex Pharmaceuticals Incorporated discovers, develops and markets small
molecule drugs that address major unmet medical needs. Vertex has seven
drug candidates in clinical development to treat viral diseases, inflammation,
cancer, autoimmune diseases and neurological disorders.
Vertex has created its pipeline using a proprietary, information-based
approach to drug design that integrates multiple technologies in biology,
chemistry and biophysics, aimed at increasing the speed and success rate
of drug discovery. Vertex's first approved product is Agenerase (TM) (amprenavir),
an HIV protease inhibitor, which Vertex co-promotes with Glaxo Wellcome.
This press release contains forward-looking statements about Vertex's
Patent No. 6,117,639, including statements about Vertex's ability to use
the patented technology to accelerate the discovery of HCV protease inhibitors
for the treatment of HCV infection, the patent's application for drug
discovery against other protease enzyme targets and Vertex's expectation
that it could select a drug development candidate targeting HCV protease
as early as 2001. While management makes its best efforts to be accurate
in making forward- looking statements, any such statements are subject
to risks and uncertainties that could cause Vertex's actual results to
vary materially. Risk factors include uncertainties relating to Vertex's
ability to use effectively the patented technology to discover protease
inhibitors for HCV and other diseases, Vertex's ability to successfully
develop, test and finance any new drug discovered using the patented technology,
Vertex's ability to protect its proprietary technologies, patent-infringement
claims, and competitive technologies and drugs.
Vertex's press releases are available at www.vpharm.com,
or by fax-on- demand at (800) 758-5804 - Code: 938395.
SOURCE Vertex Pharmaceuticals Incorporated
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