Oltipraz

Summary

Oltipraz (CHEMBL178459) is a phase-3 clinical-stage small-molecule antineoplastic agent; indicated across 3 conditions including metabolic dysfunction-associated steatotic liver disease and cirrhosis of liver.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Indications: 3 conditions
• Clinical trials: 5
• Chemistry: 226.3 Da · C8H6N2S3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL178459
Name	Oltipraz
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	47318
ChEBI	CHEBI:77319
Molecular formula	C8H6N2S3
Molecular weight	226.3
InChIKey	CKNAQFVBEHDJQV-UHFFFAOYSA-N

SMILES: CC1=C(SSC1=S)C2=NC=CN=C2

IUPAC name: 4-methyl-5-pyrazin-2-yldithiole-3-thione

ChEBI definition: A 1,2-dithiole that is 3H-1,2-dithiole-3-thione substituted at positions 4 and 5 by methyl and pyrazin-2-yl groups respectively.

Pharmacological roles (ChEBI): antineoplastic agent, antimutagen, protective agent, antioxidant, EC 3.1.3.48 (protein-tyrosine-phosphatase) inhibitor, schistosomicide drug, neurotoxin, angiogenesis modulating agent.

Also known as: NSC-347901, Oltipraz, oltripraz, SID462739, OLTIPRAZ, OltiprazÊ, OltiprazÂ

Patent coverage: 1,058 distinct patent families (4,453 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 4,448 (100%) 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: 2 (assay-derived). Sample: Cytochrome P450 1A2, Replicase polyprotein 1ab.

Bioactivity

ChEMBL activities: 3 potent at pChembl ≥ 5 of 3 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
P0DTD1	6.68	IC50	210	nM	CHEMBL_ACT_19964200
P0DTD1	6.21	IC50	620	nM	CHEMBL_ACT_19964308
CYP1A2	5.05	Ki	9000	nM	CHEMBL_ACT_6074954

Target pathways

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

Indications & clinical

Indications

3 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
metabolic dysfunction-associated steatotic liver disease	3	MONDO:0013209	EFO:0003095
cirrhosis of liver	2	MONDO:0005155	EFO:0001422
lung neoplasm	1	MONDO:0021117	MONDO:0008903

Clinical trials

Total trials: 5.

Phase distribution

Phase	Trials
PHASE3	2
PHASE2	2
PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT02068339	PHASE3	COMPLETED	Efficacy and Safety of Oltipraz for Liver Fat Reduction in Patients With Non-Alcoholic Fatty Liver Disease Except for Liver Cirrhosis
NCT04142749	PHASE3	COMPLETED	Oltipraz for Liver Fat Reduction in Patients With Non-alcoholic Fatty Liver Disease Except for Liver Cirrhosis
NCT00956098	PHASE2	COMPLETED	Efficacy and Safety of Oltipraz in the Patients With Liver Fibrosis and Cirrhosis
NCT01373554	PHASE2	COMPLETED	Efficacy and Safety of Oltipraz in the Patients With Non-alcoholic Fatty Liver Disease
NCT00006457	PHASE1	COMPLETED	Oltipraz in the Prevention of Lung Cancer in People Who Smoke

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Related molecules

Related molecules

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