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Iguratimod

Iguratimod structure

CAS No:
123663-49-0
Formula:
C17H14N2O6S
Chemical Name:
Iguratimod
Synonyms:
Methanesulfonamide,N-[3-(formylamino)-4-oxo-6-phenoxy-4H-1-benzopyran-7-yl]-;N-[3-(Formylamino)-4-oxo-6-phenoxy-4H-1-benzopyran-7-yl]methanesulfonamide;T 614;3-Formylamino-7-methylsulfonylamino-6-phenoxy-4H-1-benzopyran-4-one;Iguratimod;N-[3-(Formylamino)-4-oxo-6-phenoxy-4H-chromen-7-yl]methanesulfonamide;T 614 (antiinflammatory);Careram;Kolbet
Categories:
Active Pharmaceutical Ingredients > Antipyretic Analgesics

Description

In August 2011, China’s State FDA approved Simcere Pharmaceutical Group’s new drug application for iguratimod (T-614), a disease modifying anti-rheumatic drug (DMARD) for the treatment of rheumatoid arthritis (RA). Preclinical in vivo studies indicated that iguratimod was effective in an established adjuvant-induced arthritis model (ED40=3.6 mg/kg) in rats and also efficacious in a type II collagen-induced arthritis model in DBA/1J mice at 30 mg and 100 mg/kg.

Iguratimod is an organic molecular entity.|Iguratimod is under investigation in Rheumatoid Arthritis.

Iguratimod Basic Attributes

Molecular Weight：

374.37

Exact Mass：

374.37

EC Number：

1308068-626-2

UNII：

4IHY34Y2NV

DSSTox ID：

DTXSID0048971

HScode：

2935009090

Characteristics

PSA：

119

XLogP3：

1.4

Density：

1.52±0.1 g/cm3(Predicted)

Melting Point：

238.0 to 242.0 °C

Boiling Point：

580.6±60.0 °C(Predicted)

Flash Point：

304.9±32.9 °C

Refractive Index：

1.674

Safety Information

Precautionary statement(s)：

P201, P202, P281, P308+P313, P405, P501

Hazard Statements：

H361

GHS Classification：

|Warning|H361 (100%): Suspected of damaging fertility or the unborn child [Warning Reproductive toxicity]|P201, P202, P281, P308+P313, P405, and P501|The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory.

Drug Information

MeSH Entry Terms：

3-formylamino-7-methylsulfonylamino-6-phenoxy-4H-1-benzopyran-4-one

Iguratimod Use and Manufacturing

Iguratimod acts as an anti-inflammatory agent, used primarily in the treatment of rheumatoid arthritis.

Computed Properties

Molecular Weight:374.4
XLogP3:1.4
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:7
Rotatable Bond Count:5
Exact Mass:374.05725734
Monoisotopic Mass:374.05725734
Topological Polar Surface Area:119
Heavy Atom Count:26
Complexity:665
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

Drug Function and Efficacy

It can inhibit foot swelling in collagen arthritis model rats and alleviate the destruction of rat bone and cartilage tissue; it can inhibit the activity of nuclear factor-κB (NF-κB) in vitro, thereby inhibiting the production of inflammatory cytokines; it can directly interact with mouse and human B cells in vitro to inhibit the production of immunoglobulins; it can inhibit the activity of purified cyclooxygenase-2 (COX-2) in vitro (IC50=7.7μg/ml), but has no effect on the activity of cyclooxygenase-1 (COX-1).

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Eguratimod Tablets
Ingredients	The active ingredient of this product is iguratimod.
Indication	The interaction between Edixin and other drugs has not been systematically studied. In vitro tests have shown that Edixin has little inhibitory effect on CYP2D6, CYP1A2, CYP2C9, CYP2C19 and CYP3A4, indicating that Edixin will not affect drugs metabolized by these enzymes due to the inhibition of the above P450 isoenzymes.
Specifications	25 mg
Manufacturer	Hainan Simcere Pharmaceutical Co., Ltd.

Ailamode
Specifications	－－－－
Manufacturer	Hainan Simcere Pharmaceutical Co., Ltd.

Registered Holders

Zhejiang Hengkang Pharmaceutical Co., Ltd.

China
Active
TianJin TaiPu Pharmaceutical Co., Ltd.

China
Active
CHEER FINE Pharmaceutical Co., Ltd.

China
Active

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