Drug intelligence / Profile preview

iguratimod + methotrexate

Development stage
Phase 4
Lead developer
Eisai
Modality
Small Molecules
Administration
Oral, Subcutaneous, Intramuscular
01

Overview

Iguratimod + methotrexate is a fixed drug combination used primarily for the treatment of active rheumatoid arthritis (RA), especially in patients with an inadequate response to conventional disease-modifying antirheumatic drugs (DMARDs). Iguratimod is a small molecule immunomodulatory agent that inhibits nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) activation, leading to reduced production of inflammatory cytokines such as IL-6, TNF-alpha, and IL-17. It also inhibits cyclooxygenase 2 (COX-2) selectively and modulates immune cell function, including B cell activity and osteoclast differentiation. Methotrexate is a folic acid antagonist that inhibits dihydrofolate reductase, blocking DNA synthesis and exerting anti-inflammatory effects by suppressing immune cell proliferation. The combination has demonstrated superior efficacy compared to monotherapy with either agent in improving clinical symptoms, reducing inflammatory markers, and slowing joint damage in RA without significantly increasing adverse events[1][2][3][4][5][7].

Brand names
Careram + methotrexateKolbet + methotrexate
Other names
IGU + MTXIGU plus MTXMethotrexate and Iguratimod combination therapy
02

Targets

PTGS2 (Prostaglandin-Endoperoxide Synthase 2)DHFR (Dihydrofolate reductase)IL-17A (Interleukin-17A)IL-6 (Interleukin 6)NF-κBTNFA (Tumor necrosis factor alpha (soluble))

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