Lesinurad

Summary

Lesinurad (CHEMBL2105720) is an approved small-molecule uricosuric drug (ATC M04AB05) targeting SLC22A12; indicated across 2 conditions including gout.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: M04AB05
• Targets: 1 (SLC22A12)
• Indications: 2 conditions
• Clinical trials: 19
• Chemistry: 404.3 Da · C17H14BrN3O2S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL2105720
Name	Lesinurad
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	53465279
ChEBI	CHEBI:90929
ATC	M04AB05
Molecular formula	C17H14BrN3O2S
Molecular weight	404.3
InChIKey	FGQFOYHRJSUHMR-UHFFFAOYSA-N

SMILES: C1CC1C2=CC=C(C3=CC=CC=C23)N4C(=NN=C4Br)SCC(=O)O

IUPAC name: 2-[[5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-1,2,4-triazol-3-yl]sulfanyl]acetic acid

ChEBI definition: A member of the class of triazoles that is [(3-bromo-1,2,4-triazol-5-yl)sulfanyl]acetic acid substituted at position 1 of the triazole ring by a 4-cyclopropylnaphthalen-1-yl group. Used for treatment of gout.

Pharmacological roles (ChEBI): uricosuric drug.

Also known as: Lesinurad, Lesinurad component of duzallo, RDEA 594, RDEA-594, RDEA594, Zurampic, LESINURAD, (+/-)-Lesinurad, (-)-lesinurad, (+)-lesinurad, Lesinarad, US10584104

Parent form; salt/anhydrous children: CHEMBL2105716

Patent coverage: 252 distinct patent families (604 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		0%	Q96S37

Broader ChEMBL bioactivity targets: 7 (assay-derived). Sample: Solute carrier family 22 member 11, Cytochrome P450 2D6, Cytochrome P450 1A2, Cytochrome P450 2C9, Cytochrome P450 3A4, Cytochrome P450 2C19, Solute carrier family 22 member 12.

Bioactivity

ChEMBL activities: 20 potent at pChembl ≥ 5 of 42 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
SLC22A11	5.69	IC50	2030	nM	CHEMBL_ACT_19057417
SLC22A12	5.45	IC50	3530	nM	CHEMBL_ACT_19057415
SLC22A12	5.43	IC50	3700	nM	CHEMBL_ACT_20627793
SLC22A11	5.43	IC50	3700	nM	CHEMBL_ACT_25704120
SLC22A12	5.36	IC50	4400	nM	CHEMBL_ACT_18001354
SLC22A12	5.26	IC50	5540	nM	CHEMBL_ACT_24889655
SLC22A12	5.26	IC50	5540	nM	CHEMBL_ACT_25935261
SLC22A12	5.19	IC50	6460	nM	CHEMBL_ACT_29310346
SLC22A12	5.17	IC50	6700	nM	CHEMBL_ACT_16663685
SLC22A12	5.14	IC50	7300	nM	CHEMBL_ACT_18001352
SLC22A12	5.14	IC50	7200	nM	CHEMBL_ACT_19124210
SLC22A12	5.14	IC50	7300	nM	CHEMBL_ACT_19124211
SLC22A11	5.14	IC50	7300	nM	CHEMBL_ACT_20627792
SLC22A12	5.14	IC50	7300	nM	CHEMBL_ACT_25704119
SLC22A12	5.14	IC50	7180	nM	CHEMBL_ACT_26123961
SLC22A12	5.14	IC50	7180	nM	CHEMBL_ACT_26124073
SLC22A12	5.14	IC50	7180	nM	CHEMBL_ACT_27908348
SLC22A12	5.14	IC50	7180	nM	CHEMBL_ACT_29153305
SLC22A12	5.12	IC50	7560	nM	CHEMBL_ACT_25577205
SLC22A12	5.03	IC50	9380	nM	CHEMBL_ACT_25055302

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

1 approved indication. FDA phase 4, plus an anticancer drug’s labelled cancer uses (which ChEMBL often logs at phase 3).

Indication	Phase	MONDO	EFO
gout	4	MONDO:0005393	EFO:0004274

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

Clinical trials

Total trials: 19.

Phase distribution

Phase	Trials
PHASE1	9
PHASE3	7
PHASE2	2
PHASE4	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT03226899	PHASE4	TERMINATED	A Phase 4 Safety and Efficacy Study to Evaluate Lesinurad 200 mg in Participants With Gout and Renal Impairment
NCT01493531	PHASE3	COMPLETED	Combining Lesinurad With Allopurinol in Inadequate Responders
NCT01508702	PHASE3	COMPLETED	Lesinurad Monotherapy in Gout Subjects Intolerant to Xanthine Oxidase Inhibitors
NCT01510158	PHASE3	COMPLETED	Combining Lesinurad With Allopurinol in Inadequate Responders
NCT01510769	PHASE3	COMPLETED	Combination Treatment Study in Subjects With Tophaceous Gout With Lesinurad and Febuxostat
NCT01650246	PHASE3	COMPLETED	Open-Label Lesinurad Monotherapy Extension Study in Gout
NCT01808131	PHASE3	COMPLETED	Lesinurad and Allopurinol Combination Extension Study in Gout
NCT01808144	PHASE3	COMPLETED	Lesinurad and Febuxostat Combination Extension Study in Gout
NCT00955981	PHASE2	COMPLETED	Gout Dose Response Study
NCT01001338	PHASE2	COMPLETED	Allopurinol Combination Study
NCT01744379	PHASE1	COMPLETED	Single and Multiple Dose Study in Japanese
NCT01884272	PHASE1	COMPLETED	NSAID Drug Interaction Study
NCT01908257	PHASE1	COMPLETED	Lesinurad Interaction Study With Ranitidine
NCT01982201	PHASE1	COMPLETED	Antacid Interaction Study
NCT02028689	PHASE1	COMPLETED	Metformin and Furosemide Drug-Drug Interaction Study
NCT02039700	PHASE1	COMPLETED	Bioavailability of Lesinurad and Intravenous [14C]Lesinurad
NCT02581553	PHASE1	COMPLETED	Lesinurad/Allopurinol 200/300 FDC Tablets Bioavailability
NCT02888054	PHASE1	COMPLETED	Lesinurad/Allopurinol 200/300 FDC Tablets Bioequivalence
NCT03272425	PHASE1	COMPLETED	Lesinurad/Allopurinol 200/300 Fixed-Dose Combination (FDC) Tablets Bioequivalence.

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

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
SULFINPYRAZONE	ChEMBL	Phase 4 (approved)	SLC22A12
DOTINURAD	ChEMBL	Phase 3	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