BUSINESS WIRE
CGEN-25017 Previously Demonstrated Significant Anti-Angiogenic
Activity
Peptide Was Predicted Using Compugen’s DAC Blockers Discovery
Platform
TEL AVIV, Israel--(BUSINESS WIRE)--Compugen Ltd. (NASDAQ:CGEN) announced today that CGEN-25017, a novel
peptide antagonist of the Angiopoietin/Tie-2 pathway, has shown positive
therapeutic effects in an animal model of retinopathy, a very serious
eye condition characterized by over-growth of blood vessels. CGEN-25017,
which was initially discovered using Compugen’s Disease-Associated
Conformation (DAC) Blockers discovery platform, had previously
demonstrated significant inhibitory activity in two other models of
angiogenesis, an in vitro multi-cellular assay and the widely
recognized chorioallantoic membrane (CAM) model.
In the recently completed study utilizing a rodent model of
oxygen-induced retinopathy, administration of CGEN-25017 resulted in a
dramatic decrease in the extent of pathological neovascularization,
outperforming the positive control, soluble Tie-2. These results provide
evidence for the potential use of this novel peptide in the treatment of
angiogenic ocular diseases, such as diabetic retinopathy, age-related
macular degeneration and retinopathy of prematurity. Furthermore, since
this animal model is well accepted for assessing anti-angiogenic
activity in general, the profound dose-dependent anti-angiogenic potency
of CGEN-25017 seen in this and earlier studies indicate potential
therapeutic utility for other diseases involving pathological
angiogenesis such as cancer and inflammatory conditions, including
psoriasis and rheumatoid arthritis.
Professor John S. Penn, from the Department of Ophthalmology and Visual
Sciences at the Vanderbilt University School of Medicine, who supervised
the study and is a recognized world expert in this field stated, “The
efficacy achieved with CGEN-25017 is a fairly rare finding in this
model. Based upon our past experience conducting efficacy trials of this
type, CGEN-25017 falls within the top 10% of all test compounds that
have passed through our hands. Thus, in my opinion, CGEN-25017 warrants
further development and study as a potential therapy for
angiogenesis-related diseases."
Dr. Anat Cohen-Dayag, Compugen co-CEO added, “Angiogenesis is a field of
intense research interest worldwide both by academia and industry.
CGEN-25017 is a novel peptide that has not only demonstrated very potent
anti-angiogenic activity, but it also most likely does so by a different
mechanism than known VEGF inhibitors, thus offering the possibility for
increased efficacy and fewer side effects. The discovery of CGEN-25017
was made through the use of Compugen’s DAC Blockers platform, which
predicts the sequences of novel peptides that may block the folding of
certain proteins into their disease-associated states. Peptide blockers
predicted by this platform have now been validated experimentally in
functional assays for 11 out of 12 protein targets selected for
screening. In addition to CGEN-25017, two other predicted peptides to
date have also demonstrated therapeutic potential and several others are
now undergoing experimental validation. The DAC Blockers platform itself
is one of ten product candidate discovery platforms that have been
developed and validated to date by the Company. Thus, the discovery and
validation of CGEN-25017 provides an excellent perspective on the power
and potential of Compugen’s unique discovery capabilities.”
About Retinopathy
Retinopathy is a pathologic condition of the retina, the light-sensitive
nerve tissue that sends visual images to the brain, in which abnormal
retinal neovascularization (angiogenesis) can lead to progressive and
severe vision loss as a result of vitreal bleeding and retinal
detachment. Diabetic retinopathy is the leading cause of visual
disability and blindness among adults in the developed world, affecting
an estimated 20 million people.
About Angiogenesis and
Angiopoietin/Tie-2
Angiogenesis, the growth of new capillary blood vessels, is an important
natural process for healing and reproduction. However, abnormal blood
vessel growth is now recognized as a common denominator underlying an
increasing list of deadly and debilitating conditions, such as tumor
development, retinopathy and inflammation. Angiopoietins are naturally
occurring secreted angiogenic factors. Their receptor, Tie2, which
belongs to the family of tyrosine kinase receptors, is almost
exclusively expressed by endothelial cells. Modulation of Tie2 activity
by angiopoietins is crucial for angiogenesis, blood vessel maturation,
and vascular endothelium integrity. In view of the critical role that
angiopoietins and their receptor play in angiogenesis, various
inhibitory strategies have been employed to therapeutically target the
angiopoietin/Tie2 pathway.
About the DAC Blockers Discovery
Platform
The DAC Blockers Platform is designed for the prediction and selection
of peptides that block proteins from adopting their disease-associated
conformations. This is accomplished through the use of a series of
proprietary algorithms to identify segments in proteins of interest
that, if introduced as synthetic peptides, would prevent the proteins
from adopting disease-associated conformations and related activities
and thus could have therapeutic benefits. In addition, a key benefit of
the platform is its ability to predict, select and implement
proteome-wide searches for such peptides in proteins of interest within
human, viral and bacterial proteomes.
About Compugen
Compugen is a leading drug and diagnostic product candidate discovery
company. Unlike traditional high throughput trial and error experimental
based discovery, Compugen’s discovery efforts are based on in-silico
(by computer) prediction and selection utilizing a growing number of
field focused proprietary discovery platforms accurately modeling
biological processes at the molecular level. The resulting product
candidates are then validated through in vitro and in vivo
experimental studies and out-licensed for further development and
commercialization under various forms of revenue sharing agreements.
Compugen’s current collaborations include Biosite, Medarex, Inc., Merck
& Co., Inc., Merck Serono, Ortho-Clinical Diagnostics (a Johnson &
Johnson company), Roche, Siemens Healthcare Diagnostics, Inc., and Teva
Pharmaceutical Industries. In 2002, Compugen established an affiliate,
Evogene Ltd. www.evogene.com
(TASE: EVGN.TA), to utilize certain of the Company’s in-silico
predictive discovery capabilities in agricultural biotechnology. For
additional information about Compugen, please visit the Company’s
corporate Web site at www.cgen.com.
This press release may contain "forward-looking statements" within the
meaning of the Private Securities Litigation Reform Act of 1995. These
statements include words such as “may,” “expects,” “anticipates,”
“believes,” and “intends,” and describe opinions about future events.
These forward-looking statements involve known and unknown risks and
uncertainties that may cause the actual results, performance or
achievements of Compugen to be materially different from any future
results, performance or achievements expressed or implied by such
forward-looking statements. Some of these risks are: changes in
relationships with collaborators; the impact of competitive products and
technological changes; risks relating to the development of new
products; and the ability to implement technological improvements. These
and other factors are identified and more fully explained under the
heading "Risk Factors" in Compugen's annual reports filed with the
Securities and Exchange Commission.