setanaxib + hyaluronic acid nanoparticle

Setanaxib + hyaluronic acid nanoparticle (often abbreviated in literature as **HANP/GKT831**) is an experimental nanotherapeutic agent consisting of the small-molecule NOX1/4 inhibitor **setanaxib** (GKT831) encapsulated within **hyaluronic acid (HA) nanoparticles**. This formulation is designed to improve the delivery and therapeutic index of setanaxib by targeting CD44-expressing tumor cells, such as those in colorectal cancer. Mechanistically, the drug acts by inhibiting **NADPH oxidase 1 (NOX1)** and **NADPH oxidase 4 (NOX4)**, which are primary sources of reactive oxygen species (ROS) in the tumor microenvironment. By reducing ROS levels, the combination induces redox and bioenergy stress, inhibiting both mitochondrial oxidative phosphorylation (OXPHOS) and glycolysis—a process termed metabolic reprogramming. In preclinical models, this metabolic inhibition has been shown to enhance the efficacy of radiotherapy, increase DNA damage, and remodel the immune microenvironment by increasing cytotoxic T cell infiltration and reducing immunosuppressive cells like M2 macrophages and fibroblasts.

Other names

human atrial natriuretic peptide + GKT831hyaluronic acid nanoparticle encapsulated with GKT831HA-GKT831 nanoparticleHA-GKT-831 nanoparticleHA-GKT 831 nanoparticle