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Nibrozetone is a small molecule dinitroazetidine derivative developed by EpicentRx (formerly RadioRx), also known as RRx‑001. It acts as a bispecific agent with multiple mechanisms of action, including direct inhibition of the NLRP3 inflammasome and on-demand release of nitric oxide under hypoxic conditions. These actions result in anti-inflammatory effects and increased blood flow to poorly oxygenated tissues such as tumors. Nibrozetone also induces activation of the neuroprotective NRF2 pathway and inhibits KEAP1. Its radiosensitizing properties make tumor cells more susceptible to radiation therapy by improving tumor oxygenation through vasodilation. The drug is being investigated for several indications including small cell lung cancer (Phase III), mucositis (Phase II), various solid tumors, neuroendocrine tumors, cholangiocarcinoma, colorectal cancer, ovarian cancer, Alzheimer's disease (preclinical), Parkinson's disease (preclinical), pulmonary fibrosis (preclinical), myocardial infarction (preclinical), amyotrophic lateral sclerosis (preclinical), and endometriosis (preclinical). Nibrozetone has orphan drug status for small cell lung cancer and certain rare cancers[2][5][6][7][8].
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