Tranilast

Summary

Tranilast (CHEMBL415324) is a phase-3 clinical-stage small-molecule anti-asthmatic drug targeting TRPV2; indicated across 4 conditions including pterygium and rheumatoid arthritis.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 1 (TRPV2)
• Indications: 4 conditions
• Clinical trials: 13
• Chemistry: 327.3 Da · C18H17NO5

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL415324
Name	Tranilast
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	5282230
ChEBI	CHEBI:77572
Molecular formula	C18H17NO5
Molecular weight	327.3
InChIKey	NZHGWWWHIYHZNX-CSKARUKUSA-N

SMILES: COC1=C(C=C(C=C1)/C=C/C(=O)NC2=CC=CC=C2C(=O)O)OC

IUPAC name: 2-[[(E)-3-(3,4-dimethoxyphenyl)prop-2-enoyl]amino]benzoic acid

ChEBI definition: An amidobenzoic acid that is anthranilic acid in which one of the anilino hydrogens is replaced by a 3,4-dimethoxycinnamoyl group.

Pharmacological roles (ChEBI): anti-asthmatic drug, nephroprotective agent, anti-allergic agent, calcium channel blocker, antineoplastic agent, aryl hydrocarbon receptor agonist, hepatoprotective agent.

Also known as: MK-341, NSC-758970, Rizaben, Tranilast, tranilast, SID26719641, SID50103918, SID85231347, SID855567, SID90341124, SID49645767, SID50103919

Patent coverage: 3,296 distinct patent families (12,365 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 12,302 (99%) 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

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
TRPV2	TRPV2	Inhibition	5	1.4%	Q9Y5S1

Broader ChEMBL bioactivity targets: 32 (assay-derived). Sample: Pyruvate kinase PKM, Lysine-specific demethylase 4E, Nuclear receptor ROR-gamma, Survival motor neuron protein, 15-hydroxyprostaglandin dehydrogenase [NAD(+)], Thrombopoietin, NPC intracellular cholesterol transporter 1, Ras-related protein Rab-9A, Peripheral myelin protein 22, Histone-lysine N-methyltransferase 2A.

Bioactivity

ChEMBL activities: 30 potent at pChembl ≥ 5 of 54 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
NPC1	7.05	Potency	89.1	nM	CHEMBL_ACT_4752973
RAB9A	7.04	Potency	92	nM	CHEMBL_ACT_3851389
RAB9A	7	Potency	100	nM	CHEMBL_ACT_3850496
NPC1	6.99	Potency	103.2	nM	CHEMBL_ACT_4716912
P08482	6.9	Potency	125.9	nM	CHEMBL_ACT_4811368
SMN1	6.45	Potency	354.8	nM	CHEMBL_ACT_3884564
SMN1	6.2	Potency	631	nM	CHEMBL_ACT_3885434
P51450	6.2	Potency	631	nM	CHEMBL_ACT_4971282
RAB9A	6.05	Potency	891.3	nM	CHEMBL_ACT_3870616
ABCC4	6	IC50	1000	nM	CHEMBL_ACT_18130831
MAPK1	6	Potency	1000	nM	CHEMBL_ACT_4542143
P51450	5.9	Potency	1259	nM	CHEMBL_ACT_4111616
NPC1	5.85	Potency	1412	nM	CHEMBL_ACT_4749160
P51450	5.7	Potency	1995	nM	CHEMBL_ACT_4999953
MEN1	5.45	Potency	3548	nM	CHEMBL_ACT_4571822
MAPK1	5.45	Potency	3548	nM	CHEMBL_ACT_4717829
P51450	5.45	Potency	3548	nM	CHEMBL_ACT_5008291
P51450	5.3	Potency	5012	nM	CHEMBL_ACT_4101430
ALOX12	5.15	Potency	7080	nM	CHEMBL_ACT_4532194
Q63921	5.13	AC50	7400	nM	CHEMBL_ACT_25174467
PMP22	5.12	Potency	7569	nM	CHEMBL_ACT_4358670
P51450	5.1	Potency	7943	nM	CHEMBL_ACT_4112270
HIF1A	5.1	Potency	7943	nM	CHEMBL_ACT_4127967
HIF1A	5.1	Potency	7943	nM	CHEMBL_ACT_4520576
MEN1	5.05	Potency	8912	nM	CHEMBL_ACT_4571309
THPO	5	Potency	10000	nM	CHEMBL_ACT_4813359
TP53	5	Potency	10000	nM	CHEMBL_ACT_4874847
CYP3A4	5	Potency	10000	nM	CHEMBL_ACT_5002275
CYP3A4	5	Potency	10000	nM	CHEMBL_ACT_5070889
THPO	5	Potency	10000	nM	CHEMBL_ACT_5074312

Target pathways

Aggregated over 1 target gene(s): TRPV2.

Top Reactome pathways

1 total, by targets touching each:

Pathway	Targets	Genes
TRP channels	1	TRPV2

Dominant GO biological processes

GO term	Targets
sensory perception	1
response to temperature stimulus	1
positive regulation of axon extension	1
calcium ion transmembrane transport	1
positive regulation of calcium ion import	1
calcium ion import across plasma membrane	1
positive regulation of cold-induced thermogenesis	1
monoatomic ion transport	1
calcium ion transport	1
monoatomic ion transmembrane transport	1
transmembrane transport	1

Indications & clinical

Indications

4 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
pterygium	3	MONDO:0005085	EFO:0000678
rheumatoid arthritis	2	MONDO:0008383	EFO:0000685
scleredema adultorum	0	MONDO:0006606	EFO:1000762
sarcoidosis	0	MONDO:0019338	MONDO:0019338

Clinical trials

Total trials: 13.

Phase distribution

Phase	Trials
PHASE2	6
PHASE4	3
EARLY_PHASE1	3
PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00818805	PHASE4	COMPLETED	Efficacy Investigation Study of Olopatadine Hydrochloride Ophthalmic Solution Using OHIO Chamber in Patients With Seasonal Allergic Rhinitis (SAR)
NCT05130892	PHASE4	COMPLETED	Effect of Inflammasome Inhibitor on hsCRP in Patients After PCI
NCT06307288	PHASE4	UNKNOWN	Efficacy and Safety of Tranilast Combined With Minocycline in the Treatment of Rosacea
NCT06643689	PHASE2	NOT_YET_RECRUITING	Tranilast Vs. Steroids to Prevent Esophageal Stricture (TAPES) After Endoscopic Resection for Superficial Neoplasms
NCT00882024	PHASE2	COMPLETED	Safety and Efficacy Study of Tranilast in Patients With Active Rheumatoid Arthritis (RA)
NCT00995618	PHASE2	COMPLETED	Study of Tranilast Alone or in Combination With Febuxostat in Patients With Hyperuricemia
NCT01052987	PHASE2	COMPLETED	Study of Tranilast Alone or in Combination With Allopurinol in Subjects With Hyperuricemia
NCT03923140	PHASE2	UNKNOWN	A Clinical Study of Tranilast in the Treatment of Cryopyrin-Associated Periodic Syndrome (CAPS)
NCT05626829	PHASE2	UNKNOWN	Tranilast as a Radiosensitizer in Reradiation of Nasopharyngeal Carcinoma
NCT00717808	PHASE1	WITHDRAWN	Effects of Tranilast on Pharmacokinetics of Methotrexate (MTX) in Patients With Rheumatoid Arthritis (RA)
NCT03490708	EARLY_PHASE1	UNKNOWN	A Clinical Study of Tranilast in the Treatment of Mucinoses
NCT03512873	EARLY_PHASE1	UNKNOWN	A Clinical Study of Tranilast in the Treatment of Scleredema Diabeticorum
NCT03528070	EARLY_PHASE1	UNKNOWN	A Clinical Study of Tranilast in the Treatment of Sarcoidosis

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 1 clinical and 1 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

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.

5 molecules share ≥1 primary target. Top 5 by shared-target count:

Molecule	Source	Status	Shared targets
CANNABINOL	ChEMBL	Phase 3	TRPV2
CANNABIDIVARIN	ChEMBL	Phase 2	TRPV2
CANNABIGEROL	ChEMBL	Phase 2	TRPV2
TETRAHYDROCANNABIVARIN	ChEMBL	Phase 2	TRPV2
Cannabidiol	PubChem	Approved	TRPV2