Dotinurad

Summary

Dotinurad (CHEMBL4594446) is a phase-3 clinical-stage small molecule targeting SLC22A12; indicated across 3 conditions including gout and kidney failure.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 1 (SLC22A12)
• Indications: 3 conditions
• Clinical trials: 21
• Chemistry: 358.2 Da · C14H9Cl2NO4S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL4594446
Name	Dotinurad
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	51349053
Molecular formula	C14H9Cl2NO4S
Molecular weight	358.2
InChIKey	VOFLAIHEELWYGO-UHFFFAOYSA-N

SMILES: C1N(C2=CC=CC=C2S1(=O)=O)C(=O)C3=CC(=C(C(=C3)Cl)O)Cl

IUPAC name: (3,5-dichloro-4-hydroxyphenyl)-(1,1-dioxo-2H-1,3-benzothiazol-3-yl)methanone

Also known as: Dotinurad, Fyu-981, FYU-981, DOTINURAD

Patent coverage: 40 distinct patent families (68 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

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
SLC22A12	Urate anion exchanger 1	Inhibition	6.4	0%	Q96S37

Broader ChEMBL bioactivity targets: 3 (assay-derived). Sample: Cytochrome P450 2C9, Broad substrate specificity ATP-binding cassette transporter ABCG2, Solute carrier family 22 member 12.

Bioactivity

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

Target	pChembl	Type	Value	Unit	Activity ID
SLC22A12	7.43	IC50	37.2	nM	CHEMBL_ACT_22898990
ABCG2	7.43	IC50	37.2	nM	CHEMBL_ACT_25704121
SLC22A12	7.4	IC50	40	nM	CHEMBL_ACT_26124076
CYP2C9	5.24	IC50	5700	nM	CHEMBL_ACT_22934395
SLC22A12	5.17	IC50	6800	nM	CHEMBL_ACT_22898901

Target pathways

Aggregated over 1 target gene(s): SLC22A12.

Top Reactome pathways

9 total, by targets touching each:

Pathway	Targets	Genes
Disease	1	SLC22A12
Transport of small molecules	1	SLC22A12
R-HSA-425366	1	SLC22A12
SLC-mediated transmembrane transport	1	SLC22A12
R-HSA-549132	1	SLC22A12
Organic anion transport by SLC22 transporters	1	SLC22A12
Defective SLC22A12 causes renal hypouricemia 1 (RHUC1)	1	SLC22A12
SLC transporter disorders	1	SLC22A12
Disorders of transmembrane transporters	1	SLC22A12

Dominant GO biological processes

GO term	Targets
monoatomic ion transport	1
response to xenobiotic stimulus	1
obsolete organic anion transport	1
urate transport	1
cellular homeostasis	1
cellular response to insulin stimulus	1
urate metabolic process	1
renal urate salt excretion	1
transmembrane transport	1

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
gout	3	MONDO:0005393	EFO:0004274
kidney failure	1	MONDO:0001106	HP:0000083

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

Clinical trials

Total trials: 21.

Phase distribution

Phase	Trials
PHASE1	9
PHASE3	6
PHASE2	4
PHASE4	1
PHASE1/PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06834230	PHASE4	RECRUITING	Effect of Dotinurad in Hyperuricemia With Hypertension
NCT07089875	PHASE3	RECRUITING	A Study of Dotinurad Versus Allopurinol in Participants With Gout
NCT07089888	PHASE3	RECRUITING	A Study of Dotinurad Versus Allopurinol in Tophaceous Gout
NCT03006445	PHASE3	COMPLETED	Study of FYU-981 in Hyperuricemia With or Without Gout
NCT03100318	PHASE3	COMPLETED	Benzbromarone-Controlled, Double-Blind, Comparative Study of FYU-981 in Hyperuricemia With or Without Gout
NCT03372200	PHASE3	COMPLETED	Febuxostat-Controlled, Double-Blind, Comparative Study of FYU-981 in Hyperuricemia With or Without Gout
NCT05007392	PHASE3	COMPLETED	A Study to Evaluate Efficacy of Dotinurad and Febuxostat for the Treatment of Participants With Gout
NCT07535034	PHASE2	RECRUITING	A Phase 2 Trial of Dotinurad in Xanthine Oxidase Inhibitor (XOI) Intolerant/Uricase Failure Gout Participants
NCT02416167	PHASE2	COMPLETED	Study of FYU-981 in Hyperuricemia With or Without Gout
NCT02515864	PHASE2	COMPLETED	Clinical Pharmacology of FYU-981 (Effect on QT/QTc Interval)
NCT02837198	PHASE2	COMPLETED	Study of FYU-981 in Hyperuricemia (Effect on Two Hyperuricemic Types)
NCT06056570	PHASE1/PHASE2	COMPLETED	Open Label PK, PD and DDI of Dotinurad and Allopurinol in Gout Patients with Hyperuricemia
NCT02344875	PHASE1	COMPLETED	Clinical Pharmacology of FYU-981 (Elder Subjects)
NCT02347046	PHASE1	COMPLETED	Clinical Pharmacology of FYU-981 (Subjects With Renal Insufficiency)
NCT02348307	PHASE1	COMPLETED	Single Dose Phase I Study of FYU-981
NCT02348333	PHASE1	COMPLETED	Repeated Dose Phase I Study of FYU-981
NCT03306667	PHASE1	COMPLETED	Clinical Pharmacology of FYU-981 (Subjects With Hepatic Insufficiency)
NCT03350373	PHASE1	COMPLETED	Clinical Pharmacology of FYU-981 (Final Formulation)
NCT03350386	PHASE1	COMPLETED	Drug-drug Interaction Study of FYU-981 and Oxaprozin
NCT03375632	PHASE1	COMPLETED	Study of FYU-981 in Hyperuricemic Outpatients With or Without Gout (Effect on Two Hyperuricemic Types)
NCT05278676	PHASE1	COMPLETED	A Single and Multiple Dose Study of Dotinurad in Chinese Healthy Participants

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.

12 molecules share ≥1 primary target. Top 12 by shared-target count:

Molecule	Source	Status	Shared targets
PROBENECID	ChEMBL + PubChem	Phase 4 (approved)	SLC22A12
BENZARONE	ChEMBL	Phase 4 (approved)	SLC22A12
BENZBROMARONE	ChEMBL	Phase 4 (approved)	SLC22A12
FENOFIBRIC ACID	ChEMBL	Phase 4 (approved)	SLC22A12
LESINURAD	ChEMBL	Phase 4 (approved)	SLC22A12
SULFINPYRAZONE	ChEMBL	Phase 4 (approved)	SLC22A12
SHR-4640	ChEMBL	Phase 3	SLC22A12
ARHALOFENATE	ChEMBL	Phase 2	SLC22A12
PF-05089771	ChEMBL	Phase 2	SLC22A12
PULIGINURAD	ChEMBL	Phase 2	SLC22A12
VERINURAD	ChEMBL	Phase 2	SLC22A12
Febuxostat	PubChem	Approved	SLC22A12