QUÉBEC CITY, Aug. 30, 2011
/PRNewswire/ - Aeterna Zentaris Inc. (NASDAQ: AEZS) (TSX: AEZ)
(the "Company") today announced that a poster on its novel
orally active anticancer Erk inhibitor, which includes AEZS-131,
was presented at the 242nd American Chemical Society
National Meeting held at the Colorado Convention Center in Denver, Colorado. The poster was presented by
Matthias Gerlach, Ph.D., Senior
Director of Medicinal Chemistry for Aeterna Zentaris Inc.
Focus on inhibition of downstream kinase Erk 1/2 activity as a
therapeutic target is attractive because the pharmacologic
inhibition of Erk 1/2 reverses the activation of the
Ras-Raf-Mek-Erk signal transduction pathway through many common
deregulated molecular lesions in cancer. This pathway controls a
number of fundamental cellular processes including cell survival,
proliferation, motility and differentiation. It is constitutively
activated in cancers of the lung, colon, pancreas, kidney, and
ovary. Erk is pivotal in the pathway downstream of Ras, Raf and
Mek, acting as central point where multiple signaling pathways
coalesce to drive transcription.
Poster #17068
Entitled, "Novel Pyrido[2,3-b]pyrazines as orally active ERK
inhibitors," M. Gerlach, I. Seipelt, G. Mueller, T.
Schuster, L. Blumenstein, B. Aicher, E. Guenther and M. Teifel.
Results
AEZS-131 is an orally active small molecular compound that
selectively inhibits Erk 1/2 with an IC50 of 4nM.
The in vitro antiproliferative efficacy proved to be
excellent in diverse human tumor cell lines. GI50 values
in the low nanomolar range were obtained. In vivo anti-tumor
activity was studied in a mouse xenograft experiment utilizing the
human HCT-116 colon cancer model. Up to 74% inhibition of tumor
growth was achieved with daily oral doses of 30 - 120 mg/kg. Our
medicinal chemistry programs are supported by X-ray crystallography
and modeling towards the optimization of pyrido[2,3-b]pyrazines as
novel series of kinase inhibitors.
Juergen Engel, Ph.D., Aeterna
Zentaris' President and Chief Executive Officer, commented: "As
part of our targeting strategy in cancer with perifosine, AEZS-108,
AEZS-112 and AEZS-120, we are proud to have identified the first in
class Erk 1/2 inhibitor with in vivo anticancer activity. In
parallel we are also developing AEZS-129 a pan PI3K inhibitor
without m-TOR activity as well as AEZS-132, a dual inhibitor of
PI3K and Erk."
About Erk 1/2 Inhibitor Compounds
Aeterna Zentaris has identified small molecular compounds that
selectively inhibit Erk 1/2, among them AEZS-131, which has
been shown to significantly inhibit tumor growth in in vivo
studies. Early development of the Erk inhibitor AEZS-131 is an
integral part based on our knowledge with perifosine of Aeterna
Zentaris' kinase research program comprising the investigation of
different compounds for single Erk inhibition, single PI3K
inhibition and dual Erk/PI3K kinase inhibition.
About Aeterna Zentaris Inc.
Aeterna Zentaris is a late-stage oncology drug development
company currently investigating potential treatments for various
cancers including colorectal, multiple myeloma, endometrial,
ovarian, prostate and bladder cancer. The Company's innovative
approach of "personalized medicine" means tailoring treatments to a
patient's specific condition and to unmet medical needs. Aeterna
Zentaris' deep pipeline is drawn from its proprietary discovery
unit providing the Company with constant and long-term access to
state-of-the-art therapeutic options. For more information please
visit www.aezsinc.com.
Forward-Looking Statements
This press release contains forward-looking statements made
pursuant to the safe harbour provisions of the U.S. Securities
Litigation Reform Act of 1995. Forward-looking statements involve
known and unknown risks and uncertainties that could cause the
Company's actual results to differ materially from those in the
forward-looking statements. Such risks and uncertainties include,
among others, the availability of funds and resources to pursue
R&D projects, the successful and timely completion of clinical
studies, the ability of the Company to take advantage of business
opportunities in the pharmaceutical industry, uncertainties related
to the regulatory process and general changes in economic
conditions. Investors should consult the Company's quarterly and
annual filings with the Canadian and U.S. securities commissions
for additional information on risks and uncertainties relating to
forward-looking statements. Investors are cautioned not to rely on
these forward-looking statements. The Company does not undertake to
update these forward-looking statements. We disclaim any obligation
to update any such factors or to publicly announce the result of
any revisions to any of the forward-looking statements contained
herein to reflect future results, events or developments, unless
required to do so by a governmental authority or by applicable
law.
SOURCE AETERNA ZENTARIS INC.