Back to products

Browse products

Approved anticancer agents

Anticancer agents in trials

Anticancer agents in preclinical trials

Anticancer molecular libraries

MedKoo product information:

AEZS-112

Description of AEZS 112: AEZS 112 is an orally active small mol. anti-cancer drug which inhibits the polymn. of tubulin at low micromolar concns. AEZS 112 dose-dependently increased non-vital hypodiploid cells and the cytotoxic effect was least pronounced in G2 phase of the cell cycle, indicating cell death during mitosis, as detd. by FACS anal. AEZS 112 showed anti-tumor activity in human ovarian and endometrial cancer cell lines at low micromolar concns., which could not be abrogated by caspase inhibition and is therefore a good candidate for in vivo studies in these tumors.

Current developer:    Æterna Zentaris Inc.

AEZS-112 is currently developed by Æterna Zentaris Inc. AEZS-112 is the first anticancer drug in development involving two mechanisms of action, tubulin and topoisomerase II inhibition. AEZS-112 expresses different modes of action such as, pro-apoptotic and anti-angiogenic properties.

Mode of action studies revealed that the compound AEZS-112 inhibits the polymerization of ß-tubulin in low micromolar concentrations. Competition studies suggest that AEZS-112 interacts with the same binding site on microtubules as colchicine. AEZS-112 destroys the mitotic spindles of the cancer cells, arrests the cancer cells in G2/M phase at low concentrations, mediates DNA fragmentation via inhibition of topoisomerase II and induces apoptosis via various mechanisms. See  Æterna Zentaris Inc's website.

1. Engel, Joerg B.; Schoenhals, Tanja; Weidler, Claudia; Haeusler, Sebastian; Krockenberger, Mathias; Rieger, Lorenz; Dietl, Johannes; Wischhusen, Joerg; Honig, Arnd. (Universitaetsfrauenklinik Wuerzburg, Wuerzburg, Germany.) Tubulin inhibitor AEZS 112 inhibits the growth of experimental human ovarian and endometrial cancers irrespective of caspase inhibition. Oncology Reports (2009), 22(2), 361-367.