WAC-224

WAC-224 is a novel quinolone-class small molecule inhibitor of DNA topoisomerase II (Topo II) developed by Wakunaga Pharmaceutical for the treatment of various cancers, including hematological malignancies and multi-drug resistant solid tumors. Unlike traditional Topo II inhibitors like etoposide or doxorubicin, WAC-224 is designed to overcome drug resistance mechanisms. In preclinical studies, it demonstrated potent anti-proliferative activity across multiple cancer cell lines, including acute myeloid leukemia (AML) models, by inducing G2/M phase cell cycle arrest and apoptosis. Notably, WAC-224 has shown significant anti-tumor efficacy in mouse xenograft models with a favorable safety profile, specifically lacking the gastrointestinal toxicity often associated with this class of drugs.

Other names

5-methyl-7-{3-[(oxan-2-ylmethyl) carbamoyl] azetidin-1-yl}-4-oxo-1-(1,3-thiazol-2-yl)-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid