Drug intelligence / Profile preview

Iguratimod + tofacitinib

Development stage
Preclinical
Lead developer
Simcere Pharmaceutical Group
Modality
Recombinant Proteins and Enzymes, Antibody-Based Therapeutics, Small Molecules
Administration
Oral
01

Overview

Iguratimod + tofacitinib is a combination therapy of two small molecule disease-modifying antirheumatic drugs (DMARDs) used primarily in the treatment of moderate-to-severe rheumatoid arthritis (RA), especially in cases that are difficult to treat or associated with interstitial lung disease. Tofacitinib is a Janus kinase inhibitor that suppresses immune cell activation and cytokine signaling by inhibiting the JAK-STAT pathway. Iguratimod acts as an immunomodulator with anti-inflammatory properties, reducing pro-inflammatory cytokines and modulating B-cell function. The combination has shown synergistic effects in preclinical models and clinical studies, alleviating joint inflammation, reducing bone erosion, suppressing pyroptosis via inhibition of NLRP3 inflammasome activation and gasdermin D-mediated pathways, and potentially slowing fibrosis progression in RA-associated usual interstitial pneumonia (RA-UIP). This dual approach targets both articular symptoms and extra-articular manifestations such as secondary osteoporosis and interstitial lung disease[1][2][3][4][5][8].

Brand names
Iremod
Other names
IGU + TOFTOF-IGU combination
02

Targets

TYK2 (Tyrosine kinase 2)JAK2 (Janus kinase 2)NLRP3 (Nod-like receptor family pyrin domain-containing protein 3)GSDMD (Gasdermin D)JAK1 (Janus kinase 1)JAK3 (Janus kinase 3)

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