iguratimod 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definition	Drug id	CAS RN
immunomodulators, both stimulant/suppressive and stimulant	4894	123663-49-0

Description:

Molecule

Description

Molfile Inchi Smiles

Synonyms:

iguratimod
kolbet
careram
T-614

a methanesulfonanilide disease-modifying antirheumatic drug that has been developed exclusively in Japan and China

Molecular weight: 374.37
Formula: C17H14N2O6S
CLOGP: 1.63
LIPINSKI: 0
HAC: 8
HDO: 2
TPSA: 110.80
ALOGS: -3.75
ROTB: 4

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
kinase-safety-class	ACVR2A,ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,ERBB2,FLT3,GRK2,GRK3,GSK3B,IKBKB,ITK,JAK2,KIT,MAP2K6,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MAPKAPK5,MARK4,MET,MTOR,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PIM2,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK,ZAP70	53
kinase-selectivity-class	AXL,ERBB2,GRK2,MAP2K6,MAPK7,MAPK8,PIK3CB,STK33,TEK	9
pfas-class	PFAS structural alert (1 = True, 0 = False)	0

Approvals:

Date	Agency	Company	Orphan
June 29, 2012	PMDA

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Pneumocystis jirovecii pneumonia	198.35	43.17	48	1171	21568	90605660
Interstitial lung disease	130.73	43.17	46	1173	76359	90550869
Lymphoproliferative disorder	127.26	43.17	25	1194	4237	90622991
Adult T-cell lymphoma/leukaemia	69.48	43.17	10	1209	254	90626974
Varicella zoster pneumonia	59.58	43.17	8	1211	120	90627108
Herpes zoster	53.96	43.17	26	1193	94618	90532610
Osteonecrosis of jaw	53.45	43.17	20	1199	39083	90588145
Pneumonia bacterial	47.84	43.17	14	1205	12776	90614452
Diffuse large B-cell lymphoma	43.81	43.17	12	1207	8633	90618595

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Interstitial lung disease	80.57	50.72	29	354	78433	42542519
Lymphoproliferative disorder	54.24	50.72	11	372	3296	42617656
Pneumonia bacterial	50.77	50.72	14	369	15678	42605274

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Interstitial lung disease	186.06	34.85	74	1765	139260	110448200
Pneumocystis jirovecii pneumonia	181.34	34.85	54	1785	42681	110544779
Lymphoproliferative disorder	169.80	34.85	36	1803	7182	110580278
Pneumonia bacterial	89.15	34.85	28	1811	26233	110561227
Adult T-cell lymphoma/leukaemia	62.75	34.85	10	1829	408	110587052
Herpes zoster	59.23	34.85	31	1808	108348	110479112
Osteonecrosis of jaw	48.57	34.85	21	1818	47996	110539464
Varicella zoster pneumonia	48.49	34.85	8	1831	406	110587054
Diffuse large B-cell lymphoma	45.90	34.85	15	1824	15883	110571577
Atypical mycobacterial infection	38.71	34.85	9	1830	2709	110584751
Listeriosis	38.40	34.85	9	1830	2805	110584655
Lymphoma	34.92	34.85	13	1826	20158	110567302

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
CHEBI has role	CHEBI:35842	antirheumatic drug
CHEBI has role	CHEBI:67079	anti-inflammatory agent

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Rheumatoid arthritis	indication	69896004	DOID:7148

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	6.64	acidic
pKa2	9.55	acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Macrophage migration inhibitory factor	Cytokine	P14174	MIF_HUMAN		IC50	5.17		CHEMBL

External reference:

ID	Source
4IHY34Y2NV	UNII
D01146	KEGG_DRUG
C1872427	UMLSCUI
CHEBI:31689	CHEBI
7TN	PDB_CHEM_ID
CHEMBL2107455	ChEMBL_ID
124246	PUBCHEM_CID
DB12233	DRUGBANK_ID
8176	INN_ID
C519076	MESH_SUPPLEMENTAL_RECORD_UI
9736	IUPHAR_LIGAND_ID
C077313	MESH_SUPPLEMENTAL_RECORD_UI
4IHY34Y2NV	INXIGHT DRUGS

Pharmaceutical products:

None