- 23.04.2012, 13:33:33
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- OTE0005
Resverlogix' RVX-208 is the First BET Bromodomain Inhibitor in Clinical Trials
Calgary, Alberta (ots/PRNewswire) -
This Novel Epigenetic Mechanism Defines an Entirely New Class of
Therapeutic
TSX Exchange Symbol: RVX
Resverlogix Corp. ("Resverlogix" or the "Company") 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:
Canada & USA Toll Free Dial In: 1-800-319-4610
Outside of Canada & USA call: +1-604-638-5340
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(TM)
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
. For further information please visit http://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 athttp://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: Company
Contacts: Donald J. McCaffrey President and CEO
Resverlogix Corp. Phone: +1-403-254-9252 Email:
[email protected] Sarah Zapotichny Director of
Investor Relations Resverlogix Corp. Phone:
+1-403-254-9252 Email: [email protected] US
Institutional Investors: Susan Noonan Managing
Partner S.A. Noonan Communications, LLC Phone:
+1-212-966-3650 Email: [email protected] Media:
Tony Russo, Ph.D. Matt Middleman, M.D. Russo
Partners, LLC Phone: +1-212-845-4251 Phone:
+1-212-845-4272 Email: [email protected]
Email: [email protected]
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