AEZS-136 shows synergy and efficacy in human tumor cells
QUÉBEC CITY, April 3, 2012
/PRNewswire/ - Aeterna Zentaris Inc. (NASDAQ: AEZS) (TSX: AEZ)
(the "Company") today announced that a poster on its novel
orally active anticancer PI3K/Erk 1/2 inhibitor, AEZS-136, showed
the compound's unique inhibition and excellent activity against
PI3K and Erk signaling pathways, as well as being well tolerated.
The poster titled, "Dual inhibition of PI3K and Erk1/2 shows
synergy and efficacy in human tumor cells, either by using drug
combinations or novel dual PI3K/Erk inhibitors", I.
Seipelt, M. Gerlach, L. Blumenstein, G. Mueller, E. Guenther,
J. Engel and M. Teifel, was presented by Irene Seipelt, PhD, Director, Preclinical
Development at Aeterna Zentaris, at the American Association for
Cancer Research Annual Meeting currently held in Chicago.
Results
The anti-proliferative efficacy of AEZS-136 was evaluated in
more than 40 human tumor cell lines including breast, ovary,
endometrium, multiple myeloma, lung, melanoma, colon, leukemia and
prostate cancer cells. In vitro ADMET properties were also
widely assessed, while in vivo pharmacokinetics (PK) and
anti-tumor efficacy was explored. AEZS-136 was well tolerated and
showed dose-dependent inhibition of human colon tumor growth of up
to 72% in a Hct116 mouse model.
Conclusions
- Effective dual targeting of Raf-Mek-Erk and PI3K-Akt
pathway
- Unique inhibitor with excellent activity against PI3K and
Erk
- Induction of G1 arrest and apoptosis
- Broad anti-proliferative activity in vitro
- Favorable in vitro ADMET and in vivo PK
profile
- Well tolerated up to daily doses of 90mg/kg for 4 weeks
- In vivo anti-tumor efficacy after oral
administration
Juergen Engel, Ph.D., Aeterna
Zentaris' President and CEO, commented, "The preclinical data
presented yesterday, confirms that AEZS-136 has a unique
advantageous dual PI3K /Erk kinase inhibition profile which could
prove to be more efficient than single pathway inhibition.
Furthermore, AEZS-136 has shown to be well tolerated. Following
these encouraging preclinical data, we are currently moving this
promising compound into the clinical development stage."
To consult a copy of the poster, please click here.
About AEZS-136
AEZS-136 is an integral part of the Company's kinase research
program comprising the investigation of different compounds for
single Erk inhibition, single PI3K inhibition and
dual Erk/PI3K kinase inhibition. AEZS-136 selectively inhibits
the kinase activity of Erk 1/2 and class 1 PI3Ks, enabling
simultaneous inhibition of the Raf-Mek-Erk and the PI3K-Akt
signaling cascades. AEZS-136 was discovered using our proprietary
compound library and high throughput screening technology.
About Aeterna Zentaris Inc.
Aeterna Zentaris is a late-stage oncology drug development
company currently investigating potential treatments for various
cancers. 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 risk that safety and efficacy data from any of our
Phase 3 trials may not coincide with the data analyses from
previously reported Phase 1 and/or Phase 2 clinical trials, 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.