OXi8007

OXi8007 is a water-soluble phosphate prodrug of the trimethoxyaryl-indole phenol OXi8006, developed as a vascular-disrupting agent (VDA). It is designed to selectively damage tumor-associated vasculature by targeting the colchicine binding site of tubulin. Upon administration, OXi8007 is rapidly converted in vivo by non-specific phosphatases into its active form, OXi8006. This active agent binds to the tubulin heterodimer, inhibiting microtubule polymerization and triggering a cascade of events including RhoA activation and actin cytoskeleton reorganization. These morphological changes cause activated endothelial cells to round up and detach from the vessel lining, leading to rapid vascular shutdown, increased permeability, ischemia, and selective necrosis within solid tumors. Preclinical studies have demonstrated its efficacy in orthotopic models of renal cell carcinoma, breast cancer, and prostate cancer, particularly when used in combination with tyrosine kinase inhibitors like cabozantinib or immune checkpoint inhibitors.

Other names

2-Aryl-3-aroyl indole salt