GTx-230

GTx-230 is an orally available, novel indole antimitotic compound developed by GTx Inc. in collaboration with the University of Tennessee. It acts as a tubulin inhibitor by binding to the colchicine site, leading to microtubule destabilization. Beyond its direct antimitotic effects, GTx-230 functions as a vascular disrupting agent (VDA), increasing tumor vascular permeability. Preclinical studies have demonstrated significant antitumor efficacy in multidrug-resistant prostate cancer models, specifically those overexpressing P-glycoprotein, where traditional taxanes like docetaxel often fail. Notably, GTx-230 exhibits reduced neurotoxicity compared to other antimitotic agents in animal models.