Iguratimod

Summary

Iguratimod (CHEMBL2107455) is a phase-3 clinical-stage small molecule; indicated across 5 conditions including rheumatoid arthritis and graft versus host disease.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Indications: 5 conditions
• Clinical trials: 23
• Chemistry: 374.4 Da · C17H14N2O6S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL2107455
Name	Iguratimod
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	124246
Molecular formula	C17H14N2O6S
Molecular weight	374.4
InChIKey	ANMATWQYLIFGOK-UHFFFAOYSA-N

SMILES: CS(=O)(=O)NC1=C(C=C2C(=C1)OC=C(C2=O)NC=O)OC3=CC=CC=C3

IUPAC name: N-[7-(methanesulfonamido)-4-oxo-6-phenoxychromen-3-yl]formamide

Also known as: Careram, Iguratimod, Kolbet, T-614, SID144206972, IGURATIMOD, iguratimod, IguratimodÊ, IguratimodÂ

Patent coverage: 538 distinct patent families (1,446 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 1,397 (97%) 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: 5 (assay-derived). Sample: Macrophage migration inhibitory factor, Prostaglandin G/H synthase 1, 3’,5’-cyclic-AMP phosphodiesterase 4A, Adenosine receptor A3, 3’,5’-cyclic-AMP phosphodiesterase 4D.

Bioactivity

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

Target	pChembl	Type	Value	Unit	Activity ID
ADORA3	5.84	AC50	1436	nM	CHEMBL_ACT_25199220
PDE4A	5.76	AC50	1753	nM	CHEMBL_ACT_25207708
PTGS1	5.36	AC50	4331	nM	CHEMBL_ACT_25206775
PTGS1	5.35	AC50	4509	nM	CHEMBL_ACT_25205845
MIF	5.17	IC50	6810	nM	CHEMBL_ACT_18550721
PDE4D	5.01	AC50	9800	nM	CHEMBL_ACT_25186042

Target pathways

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

Indications & clinical

Indications

5 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
rheumatoid arthritis	3	MONDO:0008383	EFO:0000685
graft versus host disease	3	MONDO:0013730	MONDO:0013730
Sjogren syndrome	2	MONDO:0010030	EFO:0000699
lupus nephritis	2	MONDO:0005556	EFO:0005761
autoimmune thrombocytopenic purpura	2	MONDO:0008558	EFO:0007160

Clinical trials

Total trials: 23.

Phase distribution

Phase	Trials
PHASE4	9
PHASE2	5
Not specified	5
PHASE3	2
PHASE2/PHASE3	1
PHASE1/PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT04981145	PHASE4	RECRUITING	The Efficacy and Safety of Iguratimod (IGU) in the Treatment of Primary Sjögren’s Syndrome
NCT05626348	PHASE4	RECRUITING	The Clinical Efficacy of Immunomodulators in RA Patients
NCT01548001	PHASE4	UNKNOWN	Long-term Efficacy of Iguratimod Alone or Iguratimod in Combination With Methotrexate in Patients With Rheumatoid Arthritis
NCT01554917	PHASE4	COMPLETED	A Study of Iguratimod in Patients With Active Rheumatoid Arthritis
NCT01893151	PHASE4	UNKNOWN	Effectiveness of Iguratimod Versus Placebo to Treat Early Rheumatoid Arthritis on MRI
NCT02275299	PHASE4	UNKNOWN	Study of Iguratimod Plus Methotrexate Compared to Leflunomid Plus Methotrexate in Patients With Rheumatoid Arthritis
NCT03855007	PHASE4	COMPLETED	The Clinical Efficacy and Safety of Iguratimod in RA and Early RA Patients for 6 Months Treatment
NCT04928066	PHASE4	COMPLETED	The Efficacy and Safety of Tofacitinib (TF) With Iguratimod (IGU) on RA
NCT06146972	PHASE4	UNKNOWN	Efficacy Study of Iguratimod Combined With Tofacitab in Patients With RF Positive/Negative Rheumatoid Arthritis
NCT06244628	PHASE3	RECRUITING	Safety and Efficacy of Iguratimod in the Treatment of Chronic GVHD
NCT00965757	PHASE3	COMPLETED	A Multicenter, Randomized, Double-blind, Placebo-controlled Study of the Combination Therapy of T-614 and Methotrexate in Rheumatoid Arthritis Patients With an Inadequate Response to Methotrexate
NCT05216757	PHASE2/PHASE3	UNKNOWN	Efficacy and Safety of Iguratimod in Patients With Hand Osteoarthritis (ESIGO)
NCT07057778	PHASE2	NOT_YET_RECRUITING	Iguratimod Plus Low-dose Rituximab vs Low-dose Rituximab in Corticosteroid-resistant or Relapsed ITP
NCT02936375	PHASE2	UNKNOWN	The Iguratimod Effect on Lupus Nephritis (IGeLU)
NCT03023592	PHASE1/PHASE2	UNKNOWN	Study of Iguratimod in Sjögren’s Syndrome
NCT04830644	PHASE2	UNKNOWN	A Study to Evaluate the Efficacy and Safety of Iguratimod Compared to Placebo in Patients With Active Primary Sjogren’s Syndrome.
NCT05281068	PHASE2	UNKNOWN	The Combination of Iguratimod and Danazol as the Treatment of Steroid-resistant/Relapse Immune Thrombocytopenia
NCT05302024	PHASE2	UNKNOWN	Efficacy and Safety of Iguratimod in the Treatment of Steroid-resistant/Relapse Immune Thrombocytopenia
NCT07115641	Not specified	NOT_YET_RECRUITING	Clinical Trial of Huoluo Pills Combined With Iguratimod Tablets in the Treatment of Rheumatoid Arthritis
NCT01850966	Not specified	COMPLETED	Investigation of the Safety and Efficacy of Iguratimod in Patients With Rheumatoid Arthritis
NCT02839941	Not specified	UNKNOWN	Iguratimod in Kidney Transplant Recipients
NCT03054545	Not specified	UNKNOWN	Iguratimod as Treatment for Refractory Lupus Nephritis
NCT04515706	Not specified	UNKNOWN	Iguratimod in Systemic Sclerosis

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 4 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).