nibrozetone + whole brain radiation therapy

RRx-001 (nibrozetone) is an investigational small molecule dinitroazetidine derivative developed by EpicentRx, utilized as a radiosensitizer in combination with whole brain radiation therapy (WBRT) for the treatment of brain metastases. RRx-001 acts as a multi-mechanistic agent with vascular normalizing, anti-angiogenic, and anti-inflammatory properties. Upon intravenous administration, the molecule binds to hemoglobin in red blood cells, which then preferentially home to hypoxic tumor vasculature. Within the tumor microenvironment, RRx-001 promotes vascular normalization and increases oxygenation, thereby sensitizing the tumor to the ionizing effects of radiation. Beyond its role as a radiosensitizer, RRx-001 is a chimeric NLRP3 inhibitor, an Nrf2 inducer, and a nitric oxide superagonist. The combination has been primarily evaluated in the Phase 1/2 BRAINSTORM trial (NCT02215512) for patients with brain metastases from various primary tumors, including radioresistant histologies such as melanoma.

Other names

RRx-001 + WBRTnibrozetone + WBRT