US drugmaker AEterna Zentaris presented strong in vivo data on ZEN-012, its novel, oral anticancer compound, at the 7th Joint Conference of the American Association for Cancer Research, held in Waikoloa, Hawaii.
AEterna's poster at the conference reviewed results of a preclinical development program which studied the drug's antiproliferative effects in a panel of 32 established human tumor cell lines including multi-drug resistant phenotypes. Mode-of-action studies revealed that ZEN-012 effectively inhibited tubulin polymerization and topoisomerase II activity. Results also showed that ZEN-012 induced apoptosis in U937 cells (human leukemic lymphoma cell line), as well as exerting anti-angiogenic properties at nanomolar concentrations far below anti-proliferative activity.
Given orally once or twice weekly, ZEN-012 proved to be a potent inhibitor of tumor growth in mammary, lung, renal, colon and melanoma xenograft models, as well as in leukemia cancer models at well-tolerated doses (16-40mg/kg), the firm noted, adding that it also showed good safety and toxicity profiles in a series of rodent and non-rodent studies.
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