Xie Sisi, Li Shu, Tian Jing, Li Fen
Department of Internal Medicine, The 2nd Xiangya Hospital of Central South University, Changsha, China.
Front Pharmacol. 2020 Feb 26;11:73. doi: 10.3389/fphar.2020.00073. eCollection 2020.
Iguratimod (IGU) is a novel synthetic small molecule disease modified anti-rheumatic drug approved only in Japan and China up to date. IGU plays an important immunomodulatory role in the synovial tissue of rheumatoid arthritis by inhibiting the production of immunoglobulins and cytokines and regulating T lymphocyte subsets. IGU also regulates bone metabolism by stimulating bone formation while inhibiting osteoclast differentiation, migration, and bone resorption. In clinical trials, IGU was shown to be superior to placebo and not inferior to salazosulfapyridine. Combined therapy of IGU with other disease-modifying anti-rheumatic drugs showed significant improvements for disease activity. IGU has good efficacy and tolerance as an additional treatment for rheumatoid arthritis patients with inadequate response to methotrexate and biological disease-modifying anti-rheumatic drugs. In this review, we summarize current landscape on the mechanism of action of IGU and its clinical effectiveness and safety. It is expected that further translational studies on IGU will pave the road for wider application of IGU in the treatment of autoimmune diseases other than rheumatoid arthritis.
艾拉莫德（IGU）是一种新型合成小分子疾病改善抗风湿药物，截至目前仅在日本和中国获批。IGU通过抑制免疫球蛋白和细胞因子的产生以及调节T淋巴细胞亚群，在类风湿关节炎的滑膜组织中发挥重要的免疫调节作用。IGU还通过刺激骨形成同时抑制破骨细胞分化、迁移和骨吸收来调节骨代谢。在临床试验中，IGU被证明优于安慰剂且不劣于柳氮磺胺吡啶。IGU与其他改善病情抗风湿药物的联合治疗显示出疾病活动度有显著改善。对于对甲氨蝶呤和生物改善病情抗风湿药物反应不足的类风湿关节炎患者，IGU作为附加治疗具有良好的疗效和耐受性。在本综述中，我们总结了目前关于IGU作用机制及其临床有效性和安全性的研究情况。预计对IGU的进一步转化研究将为IGU在类风湿关节炎以外的自身免疫性疾病治疗中的更广泛应用铺平道路。
