Tetomilast

Summary

Tetomilast (CHEMBL332750) is a phase-3 clinical-stage small molecule; indicated across 3 conditions including ulcerative colitis and chronic obstructive pulmonary disease.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Indications: 3 conditions
• Clinical trials: 6
• Chemistry: 370.4 Da · C19H18N2O4S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL332750
Name	Tetomilast
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	3025803
Molecular formula	C19H18N2O4S
Molecular weight	370.4
InChIKey	XDBHURGONHZNJF-UHFFFAOYSA-N

SMILES: CCOC1=C(C=C(C=C1)C2=NC(=CS2)C3=NC(=CC=C3)C(=O)O)OCC

IUPAC name: 6-[2-(3,4-diethoxyphenyl)-1,3-thiazol-4-yl]pyridine-2-carboxylic acid

Also known as: OPC-6535, Tetomilast, TETOMILAST

Patent coverage: 281 distinct patent families (854 SureChEMBL compound mentions), from 2 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

Broader ChEMBL bioactivity targets: 2 (assay-derived). Sample: Phosphodiesterase 4, 3’,5’-cyclic-AMP phosphodiesterase 4D.

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
PDE4D	7.16	IC50	70	nM	CHEMBL_ACT_19334637
PDE4A	7.13	IC50	74	nM	CHEMBL_ACT_22875413

Target pathways

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

Indications & clinical

Indications

3 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
ulcerative colitis	3	MONDO:0005101	EFO:0000729
chronic obstructive pulmonary disease	2	MONDO:0005002	EFO:0000341
Crohn disease	2	MONDO:0005011	EFO:0000384

Clinical trials

Total trials: 6.

Phase distribution

Phase	Trials
PHASE3	3
PHASE2	2
PHASE2/PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00064441	PHASE3	COMPLETED	FACTS I: A Study to Test the Safety and Effectiveness of a New Medication on the Treatment of Active Ulcerative Colitis
NCT00064454	PHASE3	COMPLETED	FACTS II: A Study to Test the Safety and Effectiveness of a New Medication on the Treatment of Active Ulcerative Colitis
NCT00092508	PHASE3	COMPLETED	CORE: A Study of OPC-6535 With Asacol® in Maintaining Ulcerative Colitis (UC) Remission
NCT00989573	PHASE2/PHASE3	COMPLETED	A Dose-finding and Confirmatory Trial of OPC-6535 in Patients With Active Crohn’s Disease
NCT00874497	PHASE2	TERMINATED	Pilot Study of Tetomilast in Chronic Obstructive Pulmonary Disease (COPD) Associated With Emphysema
NCT00917150	PHASE2	COMPLETED	To Investigate the Efficacy and Safety of OPC-6535 in Chronic Obstructive Pulmonary Disease (COPD) Patients

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).