ZEN-012

ZEN-012 (also known as AEZS-112) is an orally active small molecule anticancer agent developed by Aeterna Zentaris. It is characterized by a dual mechanism of action, functioning as both a tubulin polymerization inhibitor and a catalytic inhibitor of topoisomerase II. Specifically, ZEN-012 binds to the colchicine binding site on beta-tubulin at low micromolar concentrations and inhibits the catalytic activity of topoisomerase II without inducing DNA strand breaks typical of topoisomerase poisons. The compound also demonstrates pro-apoptotic and anti-angiogenic properties. Preclinical evaluations have shown nanomolar anti-proliferative activity against a broad spectrum of human cancer cell lines, including ovarian, endometrial, lung, and colon cancers, as well as efficacy in various xenograft models.

Other names

9-Acridinyl[4-(3-methoxyphenyl)-1-piperazinyl]methanone