AACR: New Inhibitor Shows Broad Anti-Tumor Activity

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(Chemotherapy Advisor) – Data presented at the annual meeting of the American Association for Cancer Research shows that AEZS-136 has synergy and efficacy in human tumor cells. The drug's manufacturer Aeterna Zentaris, Québec City, Canada, presented preclinical data on the PI3K/ Erk 1/2 inhibitor that demonstrated the compound's unique inhibition and activity against PI3K and Erk signaling pathways, as well as its safety. The poster entitled, "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 Annual Meeting currently held in Chicago.

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. The authors presented data on endometrial, lung, colon, multiple myeloma, and melanoma cell lines and AEZS-136 showed broad dose-dependent, anti-proliferative activity in all of them. AEZS-136 also resulted in a 72% dose-dependent reduction in tumor volume in a mouse model of colon cancer. AEZS-136 had favorable in vitro ADMET properties and in vivo pharmacokinetics (PK). AEZS-136 was well tolerated.

Juergen Engel, PhD, Aeterna Zentaris' president and CEO, commented: "The preclinical data presented 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." 

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