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Aeterna Zentaris Presents Preclinical Data for Its Anti-Cancer PI3K/ Erk 1/2 Inhibitor, AEZS-136, at AACR Meeting
AEZS-136 shows synergy and efficacy in human tumor cells QUÉBEC CITY, April 3, 201...
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[{"type":"text","content":"\n\n\n\n\n\nAEZS-136 shows synergy and efficacy in human tumor cells\n\n\nQUÉBEC CITY, April 3, 2012 /CNW Telbec/ - Aeterna Zentaris Inc. (NASDAQ:\n AEZS) (TSX: AEZ) (the \"Company\") today announced that a poster on its\n novel orally active anticancer PI3K/Erk 1/2 inhibitor, AEZS-136, showed\n the compound's unique inhibition and excellent activity against PI3K\n and Erk signaling pathways, as well as being well tolerated. The poster\n titled, \"Dual inhibition of PI3K and Erk1/2 shows synergy and efficacy in human\n tumor cells, either by using drug combinations or novel dual PI3K/Erk\n inhibitors\", I. Seipelt, M. Gerlach, L. Blumenstein, G. Mueller, E. Guenther, J.\n Engel and M. Teifel, was presented by Irene Seipelt, PhD, Director, Preclinical Development\n at Aeterna Zentaris, at the American Association for Cancer Research\n Annual Meeting currently held in Chicago.\n\n\nResults\n\n\nThe anti-proliferative efficacy of AEZS-136 was evaluated in more than\n 40 human tumor cell lines including breast, ovary, endometrium,\n multiple myeloma, lung, melanoma, colon, leukemia and prostate cancer\n cells. In vitro ADMET properties were also widely assessed, while in vivo pharmacokinetics (PK) and anti-tumor efficacy was explored. AEZS-136\n was well tolerated and showed dose-dependent inhibition of human colon\n tumor growth of up to 72% in a Hct116 mouse model.\n\n\nConclusions\n\n\nEffective dual targeting of Raf-Mek-Erk and PI3K-Akt pathway\n\n\nUnique inhibitor with excellent activity against PI3K and Erk\n\n\nInduction of G1 arrest and apoptosis\n\n\nBroad anti-proliferative activity in vitro\n\n\nFavorable in vitro ADMET and in vivo PK profile\n\n\nWell tolerated up to daily doses of 90mg/kg for 4 weeks\n\n\nIn vivo anti-tumor efficacy after oral administration\n\n\nJuergen Engel, Ph.D., Aeterna Zentaris' President and CEO, commented,\n \"The preclinical data presented yesterday, confirms that AEZS-136 has a\n unique advantageous dual PI3K /Erk kinase inhibition profile which\n could prove to be more efficient than single pathway inhibition.\n Furthermore, AEZS-136 has shown to be well tolerated. Following these\n encouraging preclinical data, we are currently moving this promising\n compound into the clinical development stage.\"\n\n\nTo consult a copy of the poster, please click here.\n\n\nAbout AEZS...