vadimezan

Vadimezan (DMXAA) is a small-molecule tumor vascular disrupting agent (tumor-VDA) that targets the blood vessels supplying tumors to induce tumor regression. Its mechanism of action involves direct and indirect effects on tumor vasculature—inducing apoptosis in endothelial cells, causing hemorrhagic necrosis and ischemia within tumors, stimulating the innate immune system (notably macrophages), and promoting the release of inflammatory cytokines such as TNF-α. In mice, DMXAA acts as an agonist of the stimulator of interferon genes (STING) pathway; however, it does not activate human STING due to species-specific differences. This explains its failure in late-stage clinical trials despite promising preclinical results. It was originally developed for solid tumors including non-small cell lung cancer (NSCLC), prostate cancer, and HER2-negative metastatic breast cancer[1][2][5][7][9].

Brand names

Vadimezan

Other names

5,6-dimethylxanthenone-4-acetic aciddimethylxanthenone acetic acid