Tigulixostat

Summary

Tigulixostat (CHEMBL3652780) is a phase-3 clinical-stage small molecule.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Clinical trials: 9
• Chemistry: 294.31 Da · C16H14N4O2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL3652780
Name	Tigulixostat
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	51039100
Molecular formula	C16H14N4O2
Molecular weight	294.31
InChIKey	JLQQRYOWGCIMMZ-UHFFFAOYSA-N

SMILES: CC(C)N1C=C(C2=C1C=CC(=C2)N3C=C(C=N3)C(=O)O)C#N

IUPAC name: 1-(3-cyano-1-propan-2-ylindol-5-yl)pyrazole-4-carboxylic acid

Also known as: LC-350189, Lc350189, LC350189, Tigulixostat, US8729273, 1, TIGULIXOSTAT

Patent coverage: 31 distinct patent families (91 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 57 (63%) 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: Xanthine dehydrogenase/oxidase.

Bioactivity

ChEMBL activities: 2 potent at pChembl ≥ 5 of 2 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
P80457	8.47	IC50	3.4	nM	CHEMBL_ACT_17633333
P80457	8.47	IC50	3.4	nM	CHEMBL_ACT_25597643

Target pathways

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

Indications & clinical

Indications

0 indication records carry no mapped disease name (EFO/MeSH-only); none shown.

Clinical trials

Total trials: 9.

Phase distribution

Phase	Trials
PHASE1	5
PHASE3	3
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT07414394	PHASE3	RECRUITING	Tigulixostat (IBI128) vs Febuxostat in Gout
NCT05586958	PHASE3	COMPLETED	Tigulixostat, Phase 3 Study, Placebo Controlled in Gout Patients
NCT05586971	PHASE3	COMPLETED	Tigulixostat, Phase 3 Study, Allopurinol Controlled in Gout Patients
NCT01361646	PHASE1	COMPLETED	Safety, Tolerability and Pharmacokinetic/Pharmacodynamic Characteristics of LC350189
NCT04066712	PHASE1	COMPLETED	Renal PK Study of LC350189
NCT04070846	PHASE1	COMPLETED	Mass Balance Study of [14C]LC350189 in Healthy Volunteers
NCT04886050	PHASE1	COMPLETED	Relative Bioavailability Study to Assess an LC350189 Tablet Compared to an LC350189 Capsule in Healthy Adults
NCT06189404	PHASE1	COMPLETED	Effect of Tigulixostat on the Pharmacokinetics of Theophylline
NCT04966325	EARLY_PHASE1	COMPLETED	Thorough QT (TQT) Study to Evaluate the Effect of LC350189 on Cardiac Repolarization in Healthy Male and Female Subjects

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).