Iguratimod

Anti-rheumatic drugs

Aguratimod, chemical name is N-[3-(formamido)-4-oxy-6-phenoxy-4H-1-benzopyran-7-yl] methanesulfonamide, with the appearance of white or off-white crystalline powder, odorless, tasteless, insoluble in water, slightly soluble in acetonitrile, soluble in dichloromethane, tetrahydrofuran, chloroform and ethanol, etc. It is a new type of anti-rheumatic drug for disease relief, which can relieve joint damage and immune abnormalities in chronic arthritis and autoimmune diseases, and inhibit the production of inflammatory cytokines and immunoglobulins. It has significant effect and safety in the treatment of rheumatoid arthritis. It has anti-inflammatory and analgesic effects on acute and chronic inflammation. Unlike traditional non-steroidal anti-inflammatory drugs, Aguratimod basically does not show adverse reactions such as ulcers in the digestive tract. This product can activate osteoclasts, promote bone resorption, and lead to bone loss. Inhibiting these pro-inflammatory factors can play a dual role in controlling rheumatoid arthritis and bone loss caused by it. In August 2011, Jiangsu Xiansheng Pharmaceutical Co., Ltd. was approved by the State Food and Drug Administration (SFDA) to develop and produce iguratimod.

Mechanism of Action

The main mechanism of action of iguratimod is: reducing the production of prostaglandins in inflammatory tissues by selectively inhibiting cyclooxygenase-2; inhibiting the release of bradykinin from inflammatory tissues; inhibiting the proliferation of antigen-specific T cells; reducing the level of proinflammatory factors produced by B cells in patients with rheumatoid arthritis; stimulating osteoblast differentiation and bone construction; inhibiting the expression of synovial cell co-stimulatory factors and the production of cytokines. It can inhibit the production of immunoglobulins, inhibit the production of cytokines, inhibit bone resorption and promote bone formation. It can inhibit the increase of bradykinin in kaolin-induced inflammatory reactions, and its analgesic effect may be related to the inhibition of bradykinin.