Aeterna Zentaris: Poster Presentation at AACR Meeting Provides Rationale for New Therapeutic Opportunities in Oncology with Erk Inhibitors
QUÉBEC CITY, April 9, 2014 /PRNewswire/ - Aeterna Zentaris Inc. (NASDAQ: AEZS) (TSX: AEZ) (the "Company") today announced that a poster on AEZS-134, a highly potent and selective ATP competitive Erk inhibitor, provides rationale for new therapeutic opportunities in oncology with this compound. The poster, titled, "Erk Inhibition as a Therapeutic Option for the Treatment of Raf- and Mek- Inhibitor Resistant Tumors", I. Seipelt, P. Schmidt, H. Märzhäuser, M. Gerlach, K. Jung, T. Schuster and M. Teifel, was presented yesterday by Irene Seipelt, Ph. D., Director, Preclinical Development at Aeterna Zentaris, during a poster session at the American Association for Cancer Research Annual Meeting in San Diego, California.
Richard Sachse, MD, Aeterna Zentaris' CSO/CMO, commented, "Our abstract on AEZS-134 drew a high level of attention at AACR, as participants of a session on the most exciting recent developments in RAS/RAF/EGFR research, placed it among 11 high-impact abstracts out of the hundreds on this topic. The preclinical data presented yesterday, suggests that Erk inhibitors such as AEZS-134 may provide a treatment option for patients suffering from tumors which are resistant to currently established therapies such as B-Raf and Mek inhibitors. Following these encouraging preclinical data, we are currently evaluating further development of this compound class."
The MAPK pathway represents a prime target for therapeutic intervention in cancer. Recent approvals demonstrate significant antitumor activities and survival benefits for B-Raf and Mek inhibitors. However the observation of resistance to such Raf and Mek inhibitors has been documented in both clinical and preclinical trials. These phenomena led to the suggestion to target the downstream kinase Erk to overcome such resistance.
Results and Conclusions
Data demonstrate that Erk inhibitors result in efficient growth inhibition of tumor cells that are resistant to Raf and Mek inhibitors. AEZS-134, a highly potent and selective ATP competitive Erk inhibitor, overcomes the Raf inhibitor-induced paradoxical cell activation and the acquired resistance to Mek inhibitors in various tumor cell lines.
The data provide a rationale for new therapeutic opportunities by using Erk inhibitors in oncology. In order to maximize therapeutic benefit for patients, targeting Erk may be more effective than targeting Raf or Mek in a variety of MAPK resistance settings. AEZS-134 and related compounds provide potent and selective tools to help address this question.
To consult a copy of the poster, please click here.
AEZS-134 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-134 selectively inhibits the kinase activity of Erk. AEZS-134 was discovered using the Company's proprietary compound library and high throughput screening technology. AEZS-134 is available for partnering.
About Aeterna Zentaris Inc.
Aeterna Zentaris is a specialty biopharmaceutical company engaged in developing novel treatments in oncology and endocrinology. The Company's pipeline encompasses compounds at various stages of development. For more information, visit www.aezsinc.com.
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SOURCE Aeterna Zentaris Inc.