Drug intelligence / Profile preview

Nibrozetone

Development stage
Phase 3
Lead developer
EpicentRx
Modality
Classical Binding Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

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].

Other names
2-Bromo-1-(3,3-dinitroazetidin-1-yl)ethanone2-BROMO-1-(3,3-DINITROAZETIDIN-1-YL)ETHAN-1-ONE
02

Targets

KEAP1 (Kelch-like ECH-associated protein 1)CD47 (Cluster of Differentiation 47)DNMTs/HDACs (DNA methyltransferases and histone deacetylases)NLRP3 (Nod-like receptor family pyrin domain-containing protein 3)MYC (MYC proto-oncogene protein)

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