Abstract
Iguratimod (IGU) is a conventional synthetic disease-modifying anti-rheumatic drug (csDMARD) routinely prescribed in Japan since 2012 to patients with rheumatoid arthritis (RA). Iguratimod acts directly on B cells by inhibiting the production of inflammatory cytokines (tumor necrosis factor-α, interleukin (IL)-1β, IL-6, IL-8, IL-17), thereby suppressing the production of immunoglobulin and inhibiting the activity of nuclear factor kappa-light chain enhancer of activated B cells. In Japan, it is one of the most used csDMARDs in daily practice, but it is not recommended as a treatment for RA due to the lack of large-scale evidence established overseas. However, recent reports on the novel pharmacological effects of IGU on lymphocytes and synovial fibroblasts, as well as its efficacy in daily practice, have increased its importance as a drug for the treatment of RA. In this review, we highlighted the basic and clinical studies in IGU and discuss its potential as a new therapeutic agent for the treatment of RA.
Highlights
The indication for methotrexate (MTX) in the treatment of heumatoid arthritis (RA) is maintained as part of the initial therapeutic strategy in the latest (2019) revised recommendations from the European League Against Rheumatism (EULAR) [1]
This review summarizes the evidence obtained from basic research and clinical trials of new conventional synthetic disease-modifying anti-rheumatic drug (csDMARD) developed in Japan, and the potenbteicaaluuseseitfeuxlenrtessvsaorifouIGs iUmmausnaenefefwectsthanedraapffeeucttsicbosnteramtetgaybofloisrmRbAy iinsfldueinsciunsgsiend
A 20% improvement in the American College of Rheumatology Criteria (ACR20) was observed in Japanese patients with active rheumatoid arthritis (RA) treated with IGU at 50 mg/day in a Phase III study by Hara et al, and this was comparable to the improvement obtained with SASP (IGU vs. SASP: 63.1% vs. 57.7%) [45]
Summary
The indication for methotrexate (MTX) in the treatment of heumatoid arthritis (RA) is maintained as part of the initial therapeutic strategy in the latest (2019) revised recommendations from the European League Against Rheumatism (EULAR) [1]. According to these recommendations, the MTX dose should be increased to approx. The updated 2019 EULAR recommendation for patients with contraindications (or early intolerance) to MTX is to consider leflunomide or sulfasalazine (SASP) as part of combination therapy [1]. Real-world clinical benefits of combination therapy for RA with the first conventional synthetic (1st cs) DMARDs together with biological (b) DMARDs and abstinence from the use of steroids have been reported [5,6], whereas only bench research and in vitro studies have been reported concerning IGU’s mechanisms of action in the inflammatory cytokine network [7], the nuclear translocation of NF-κB (nuclear factor kappa light chain enhancer of activated B cells) [8], the production of immunoglobulin [9], the differentiation of B cells [9], and bone and cartilage metabolism [10]
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