Contezolid

Summary

Contezolid (CHEMBL3287379) is a phase-3 clinical-stage small molecule; indicated across 2 conditions including pulmonary tuberculosis and bacterial infectious disease.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Indications: 2 conditions
• Clinical trials: 7
• Chemistry: 408.3 Da · C18H15F3N4O4

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL3287379
Name	Contezolid
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	25184541
Molecular formula	C18H15F3N4O4
Molecular weight	408.3
InChIKey	SULYVXZZUMRQAX-NSHDSACASA-N

SMILES: C1CN(C=CC1=O)C2=C(C=C(C(=C2F)F)N3C[C@@H](OC3=O)CNC4=NOC=C4)F

IUPAC name: (5S)-5-[(1,2-oxazol-3-ylamino)methyl]-3-[2,3,5-trifluoro-4-(4-oxo-2,3-dihydropyridin-1-yl)phenyl]-1,3-oxazolidin-2-one

Also known as: Contezolid, MRX-1, Mrx-i, MRX-I, CONTEZOLID

Patent coverage: 42 distinct patent families (67 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 55 (82%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: Cytochrome P450 2E1.

Bioactivity

ChEMBL activities: 1 potent at pChembl ≥ 5 of 1 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
CYP2E1	5.02	IC50	9600	nM	CHEMBL_ACT_14735975

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

2 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)	Phase	MONDO	EFO
pulmonary tuberculosis	3	MONDO:0006052	EFO:1000049
bacterial infectious disease	2	MONDO:0005113	EFO:0000771

Clinical trials

Total trials: 7.

Phase distribution

Phase	Trials
PHASE4	2
PHASE2	2
PHASE1/PHASE2	2
PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT07084402	PHASE4	RECRUITING	Short-term Bactericidal Effect of Contezolid in MAC-PD
NCT07213765	PHASE4	RECRUITING	Short-term Antibiotic Therapy in Mycobacterium Avium Complex Pulmonary Disease
NCT06081361	PHASE3	ACTIVE_NOT_RECRUITING	Innovating Shorter, All- Oral, Precised, Individualized Treatment Regimen for Rifampicin Resistant Tuberculosis：Contezolid, Delamanid and Bedaquiline Cohort
NCT06811012	PHASE1/PHASE2	ENROLLING_BY_INVITATION	Phase II Clinical Study of Contezolid for the Treatment of Bone and Joint Tuberculosis
NCT06811025	PHASE1/PHASE2	ENROLLING_BY_INVITATION	Phase II Clinical Study of Contezolid for the Treatment of Tuberculous Meningitis
NCT07372781	PHASE2	ENROLLING_BY_INVITATION	Clinical Study on the Early Bactericidal Activity of Contezolid Against Mycobacterium Abscessus Disease
NCT02269319	PHASE2	COMPLETED	MRX-I Versus Linezolid for the Treatment of Acute Bacterial Skin and Skin Structure Infection

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

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).