QUEBEC CITY, April 5 /CNW Telbec/ - Aeterna Zentaris Inc. (NASDAQ: AEZS)
(TSX: AEZ) (the "Company") today announced that a poster on its highly
selective Erk 1/2 inhibitor anticancer compound, AEZS-131, was
presented at the 102nd annual meeting of the American Association for Cancer Research
currently held at the Orange County Convention Center in Orlando,
Entitled, "A highly selective Erk 1/2 inhibitor with in-vivo anti tumor potency", Irene Seipelt, Eckhard Guenther, Lars Blumenstein, Gilbert Mueller,
Peter Schmidt, Babette Aicher, Michael Teifel and Matthias Gerlach
(Aeterna Zentaris GmbH).
AEZS-131 is an orally active small molecular compound that selectively
inhibits Erk 1/2 with an IC50 of 4nM, blocks cellular Rsk-1
phosphorylation, modulates downstream cellular substrate activation,
arrests tumor cells in G1 and inhibits the growth of multiple human
tumor cell lines in the nanomolar range. In in vivo pharmacokinetic studies, AEZS-131 showed a favorable PK profile.
Anti-tumor activity was studied in in vivo mouse xenograft experiments utilizing the HCT-116 colon cancer model.
AEZS-131 significantly inhibited tumor growth and was well tolerated at
daily doses up to 120 mg/kg.
Focus on inhibition of downstream kinase Erk 1/2 activity as a
therapeutic target may be attractive because the pharmacologic
inhibition of Erk 1/2 reverses Ras and Raf activation in cells which
also demonstrate resistance to common Raf inhibitors, such as
"Inhibition of Erk represents a novel approach of targeting the
Raf-Mek-Erk pathway which is frequently upregulated in cancer. AEZS-131
is a first-in-class Erk 1/2 inhibitor demonstrating proof-of-concept in vivo after oral administration." stated Juergen Engel, President and Chief
Executive Officer of Aeterna Zentaris. "The activity in cells resistant
to Raf inhibitors further underlines the potential of this approach in
patients that are refractory to current treatment regimens."
About Erk 1/2 Inhibitor Compound
Extracellular signal-regulated kinases ("Erks") act in the
Ras-Raf-Mek-Erk signaling cascade and regulate various cellular
processes such as cell growth, proliferation and survival in response
to a variety of extracellular or intrinsically mutated upstream
signals. 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 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, ovarian, endometrial cancer and multiple myeloma.
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.
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.
For further information:
Investor Relations Coordinator
(418) 652-8525 ext. 265
The Investor Relations Group
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(418) 652-8525 ext. 406