This Novel Epigenetic Mechanism Defines an Entirely New Class of
Therapeutic
TSX Exchange Symbol: RVX
CALGARY, April 23, 2012 /PRNewswire/ - Resverlogix Corp. ("Resverlogix" or the
"Company") (TSX:RVX) today announces the "Mechanism of Action" (MoA) by
which RVX-208 increases apolipoprotein A-I (ApoA-I) production. Our
data shows RVX-208 to be an inhibitor of the Bromodomain and
Extraterminal Domain (BET) proteins. RVX-208 acts on BET proteins,
including BRD4, a member of the BET-protein family, leading to
increased transcription of the ApoA-I gene followed by production of
more ApoA-I protein.
ApoA-I is the major protein component of HDL, a class of lipoproteins
believed to reduce atherosclerosis through reverse cholesterol
transport (RCT). The ability of RVX-208 to increase ApoA-I makes it
the lead candidate in Resverlogix' pipeline for treating
atherosclerotic cardiovascular disease. RVX-208 is an orally active
small molecule, the first in a new class of compounds to enter into
human clinical trials more than 4 years ago. Clinical benefits of
RVX-208 are currently being explored in two concurrent Phase 2b
clinical trials (SUSTAIN and ASSURE), led by Cleveland Clinic.
"The finding that RVX-208 inhibits BET proteins is an important
discovery for a wide scientific and medical audience," stated Dr.
Norman Wong, Chief Scientific Officer of Resverlogix. "This discovery
is important because BET proteins are key players in 'epigenetics', a
critical mechanism for regulating the expression of genes. Epigenetic
processes are mediated by proteins, including the BET-proteins, that
act in concert with the DNA to make it transcriptionally active or
dormant. This epigenetic control of gene expression plays a key role in
the development and progression of many human diseases. The knowledge
gained from studies of RVX-208 will guide Resverlogix in its search for
additional compounds to treat some of these diseases," added Dr. Wong.
"The MoA of RVX-208 has allowed the company to expand the scope of its
technology and the potential of its pipeline significantly," stated
Donald McCaffrey, President and Chief Executive Officer of Resverlogix.
"We have been generating and filing new intellectual property since our
discovery, and see the opportunity to initiate licensing and partnering
discussions in the areas of atherosclerosis, oncology, autoimmune
and Alzheimer's diseases where the MoA plays a pivotal role." Mr.
McCaffrey added that, "the value of this discovery was further
validated when Dr. James Watson, in his first solo scientific
publication since 1972, highlighted the promise of BRD4 as a
therapeutic target and in particular, against untreatable cancers."
As previously announced, Resverlogix will be hosting a Conference Call
and Webcast today, April 23, 2012, commencing at 11 am EDT to present
in further detail the Mechanism of Action of RVX-208.
Link to access the Webcast:
http://services.choruscall.com/links/resverlogix120423.html
| Conference call dial-in numbers: |
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Canada & USA Toll Free Dial In:
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1-800-319-4610
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Outside of Canada & USA call:
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+1-604-638-5340
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Epigenetics
Epigenetics is the study of processes that enable information encoded in
DNA to be expressed. Although DNA encodes the genes, by itself DNA
cannot use this data. To use the data within DNA, it must work in
concert with proteins. An essential aspect in this collaborative
process is that both DNA and proteins are packaged together into
chromosomes that reside within the cell's nucleus. There are thousands
of different genes encoded within DNA and to enable expression of these
genes when called upon by the cell requires epigenetic processes. One
of the key epigenetic processes involves modification of chromosomal
proteins by acetylation, methylation or phosphorylation, each of which
is regulated by specific enzymes. These modified entities serve as
bait for other proteins including BET proteins to bind to or so called
"read" these modifications ("the epigenetic code"). As the BET
proteins bind, they recruit additional proteins to regulate gene
activity. When the gene becomes active, it leads to synthesis of
messenger ribonucleic acid (mRNA) followed by translation of mRNA into
a specific protein. In the past decade, tremendous progress has been
made in understanding the role of epigenetics in human disease. This
in depth understanding has led to the development of medicines directed
toward cancer, such as DNA methylation inhibitors and HDAC inhibitors.
The discovery that RVX-208 is a BET bromodomain inhibitor adds new
momentum to the promise of epigenetic mechanisms as a rich source of
new medicines.
RVX-208
RVX-208 is a novel small molecule that stimulates endogenous ApoA-I
production to trigger the synthesis of HDL. The use of this approach
will enhance the functionality of HDL. ApoA-I is the major protein
component of HDL. The main role of these particles is to act as the
body's natural defense system against atherosclerosis by mediating a
normal physiologic process called reverse cholesterol transport (RCT).
This pathway enables cholesterol, including that within atherosclerotic
plaques of vessel walls, to be transported to the liver for further
processing and elimination from the body. Enhanced RCT clearance of
cholesterol from vessel walls is expected to reduce or prevent
atherosclerosis. The ability of RVX-208 to increase ApoA-I production
and thereby augment RCT differentiates it from other HDL therapies.
RVX-208 is positioned to be one of the most promising drugs in
development for the treatment of atherosclerosis.
Resverlogix Corp.
Resverlogix Corp. is a leading biotechnology company engaged in the
development of novel therapies for important global medical markets
with significant unmet medical needs. The NexVas technology platform
is the Company's primary focus, developing novel small molecules that
enhance ApoA-I production. These vital therapies are focused on
addressing the burden of Atherosclerosis and other important diseases
such as Acute Coronary Syndrome, Alzheimer's disease, Peripheral Artery
Disease, Oncology and Autoimmune diseases. Resverlogix Corp.'s common
shares trade on the Toronto Stock Exchange (TSX:RVX). For further
information please visit www.resverlogix.com.
This news release may contain certain forward-looking information as
defined under applicable Canadian securities legislation, that are not
based on historical fact, including without limitation statements
containing the words "believes", "anticipates", "plans", "intends",
"will", "should", "expects", "continue", "estimate", "forecasts" and
other similar expressions. In particular, this news release includes
forward looking information relating to research and development
activities and the potential role of RVX-208 in the treatment of
atherosclerosis. Our actual results, events or developments could be
materially different from those expressed or implied by these
forward-looking statements. We can give no assurance that any of the
events or expectations will occur or be realized. By their nature,
forward-looking statements are subject to numerous assumptions and risk
factors including but not limited to those associated with the success
of research and development programs, clinical trial programs including
possible delays in patient recruitment, the regulatory approval
process, competition, securing and maintaining corporate alliances,
market acceptance of the Company's products, the availability of
government and insurance reimbursements for the Company's products, the
strength of intellectual property, financing capability, the potential
dilutive effects of any financing, reliance on subcontractors and key
personnel and additional assumptions and risk factors discussed in our
Annual Information Form and most recent MD&A which are incorporated
herein by reference and are available through SEDAR at www.sedar.com. The forward-looking statements contained in this news release are
expressly qualified by this cautionary statement and are made as of the
date hereof. The Company disclaims any intention and has no obligation
or responsibility, except as required by law, to update or revise any
forward-looking statements, whether as a result of new information,
future events or otherwise.
For further information, please contact:
SOURCE Resverlogix Corp.