Nibrozetone

Summary

Nibrozetone (CHEMBL3526802) is a phase-3 clinical-stage small molecule targeting NLRP3; indicated across 11 conditions including small cell lung carcinoma and colorectal neoplasm.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 1 (NLRP3)
• Indications: 11 conditions
• Clinical trials: 13
• Chemistry: 268.02 Da · C5H6BrN3O5

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL3526802
Name	Nibrozetone
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	15950826
Molecular formula	C5H6BrN3O5
Molecular weight	268.02
InChIKey	JODKFOVZURLVTG-UHFFFAOYSA-N

SMILES: C1C(CN1C(=O)CBr)([N+](=O)[O-])[N+](=O)[O-]

IUPAC name: 2-bromo-1-(3,3-dinitroazetidin-1-yl)ethanone

Also known as: Abdnaz, Nibrozetona, Nibrozetone, Radiosensitizer rrx-001, Rrx 001, Rrx-001, RRx-001, NIBROZETONE

Patent coverage: 224 distinct patent families (589 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
NLRP3	NLRP3	Inhibition		0.2%	Q96P20

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

Aggregated over 1 target gene(s): NLRP3.

Top Reactome pathways

7 total, by targets touching each:

Pathway	Targets	Genes
Metalloprotease DUBs	1	NLRP3
The NLRP3 inflammasome	1	NLRP3
Purinergic signaling in leishmaniasis infection	1	NLRP3
SARS-CoV-1 activates/modulates innate immune responses	1	NLRP3
SARS-CoV-2 activates/modulates innate and adaptive immune responses	1	NLRP3
Cytoprotection by HMOX1	1	NLRP3
Turbulent (oscillatory, disturbed) flow shear stress activates signaling by PIEZO1 and integrins in endothelial cells	1	NLRP3

Dominant GO biological processes

GO term	Targets
pattern recognition receptor signaling pathway	1
negative regulation of acute inflammatory response	1
positive regulation of type 2 immune response	1
apoptotic process	1
defense response	1
inflammatory response	1
signal transduction	1
osmosensory signaling pathway	1
detection of biotic stimulus	1
negative regulation of interleukin-1 beta production	1
positive regulation of interleukin-1 beta production	1
positive regulation of interleukin-4 production	1
NLRP3 inflammasome complex assembly	1
innate immune response	1
positive regulation of T-helper 2 cell differentiation	1

Indications & clinical

Indications

11 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
small cell lung carcinoma	3	MONDO:0008433	EFO:0000702
colorectal neoplasm	2	MONDO:0005335	EFO:0004142
cholangiocarcinoma	2	MONDO:0019087	EFO:0005221
stomatitis	2	MONDO:0004842	EFO:1001904
glioblastoma	1	MONDO:0018177	EFO:0000519
lymphoma	1	MONDO:0005062	EFO:0000574
anaplastic oligodendroglioma	1	MONDO:0016696	EFO:0002501
brain neoplasm	1	MONDO:0021211	EFO:0003833
oligodendroglioma	1	MONDO:0016695	EFO:0000632
neoplasm	1	MONDO:0005070	EFO:0000616

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 13.

Phase distribution

Phase	Trials
PHASE1	6
PHASE2	5
PHASE3	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT05566041	PHASE3	ACTIVE_NOT_RECRUITING	A Phase 3, Controlled, Open-label, Global Randomized Study of RRx-001 With a Platinum Doublet or a Platinum Doublet in Small Cell Lung Cancer
NCT03699956	PHASE3	TERMINATED	RRx-001 Sequentially With a Platinum Doublet or a Platinum Doublet in Third-Line or Beyond in Patients With Small Cell Lung Cancer
NCT05966194	PHASE2	RECRUITING	RRx-001 for Reducing Oral Mucositis in Patients Receiving Chemotherapy and Radiation for Head and Neck Cancer
NCT02096354	PHASE2	COMPLETED	A Phase 2 Randomized, Open-Label Study of RRx-001 vs Regorafenib in Subjects With Metastatic Colorectal Cancer
NCT02452970	PHASE2	TERMINATED	RRx-001 in Second Line Treatment of Advanced Cholangiocarcinoma Prior to Readministration of First-Line Therapy
NCT02489903	PHASE2	COMPLETED	RRx-001 in Lung Cancer, Ovarian Cancer and Neuroendocrine Tumors Prior to Re-administration of Platinum Based Doublet Regimens (QUADRUPLE THREAT)
NCT03515538	PHASE2	COMPLETED	Safety and Efficacy of RRx-001 in the Attenuation of Oral Mucositis in Patients Receiving Chemoradiation for the Treatment of Oral Cancers
NCT01359982	PHASE1	COMPLETED	Safety and Pharmacokinetic Study of RRx-001 in Cancer Subjects
NCT02096341	PHASE1	TERMINATED	A Phase 1 Pilot Study of the Subcutaneous (s.c.) Route to Facilitate the Administration of RRx-001
NCT02215512	PHASE1	COMPLETED	Dose-Escalation Study of RRx-001 in Combination With Whole Brain Radiation in Subjects With Brain Metastases
NCT02518958	PHASE1	COMPLETED	A Phase I, Open-Label, Multiple Ascending Dose Study of RRx-001 and Nivolumab
NCT02801097	PHASE1	TERMINATED	RRx-001 in Combination With Irinotecan in Metastatic or Advanced Cancer (PAYLOAD)
NCT04525014	PHASE1	TERMINATED	RRx-001 Given With Irinotecan and Temozolomide for Pediatric Patients With Recurrent or Progressive Malignant Solid and Central Nervous System Tumors

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

8 molecules share ≥1 primary target. Top 8 by shared-target count:

Molecule	Source	Status	Shared targets
CLOMIPHENE	ChEMBL	Phase 4 (approved)	NLRP3
GLYBURIDE	ChEMBL	Phase 4 (approved)	NLRP3
CURCUMIN	ChEMBL	Phase 3	NLRP3
JT-001	ChEMBL	Phase 3	NLRP3
CLIOXANIDE	ChEMBL	Phase 2	NLRP3
DAPANSUTRILE	ChEMBL	Phase 2	NLRP3
TRICLOCARBAN	ChEMBL	Phase 2	NLRP3
USNOFLAST	ChEMBL	Phase 2	NLRP3