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Iguratimod: a new disease-modifying antirheumatic drug.

机译:伊古拉莫德(Iguratimod):一种新的能改变疾病的抗风湿药。

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摘要

Iguratimod, a methanesulfonanilide, is a novel disease-modifying antirheumatic drug that has been developed exclusively in Japan and China. It inhibits the production of immunoglobulins and various inflammatory cytokines (interleukin-1, -6 and -8 and TNF), and exerts anabolic effects on bone metabolism by stimulating osteoblastic differentiation and inhibiting osteoclastogenesis. On the molecular level, it inhibits the nuclear transcription factor NF-κB but not its inhibitor, IκBα. In addition to these immunomodulatory and other long-lasting effects, iguratimod inhibits cyclooxygenase-2, which provides a synergistic short-term action against pain and inflammation. Efficacy and tolerability are comparable to salazosulfapyridine, and probably also to methotrexate. Combination with methotrexate is synergistic in patients with insufficient response to methotrexate and does not significantly increase adverse events. Liver enzyme elevations and thrombocytopenia are the most significant side effects to watch for. In summary, iguratimod is a welcome addition to the small-molecule drug therapy of rheumatoid arthritis.
机译:甲磺酰苯胺伊古拉莫德(Iguratimod)是一种新型的改善疾病的抗风湿药,仅在日本和中国开发。它抑制免疫球蛋白和各种炎性细胞因子(白介素-1,-6和-8和TNF)的产生,并通过刺激成骨细胞分化和抑制破骨细胞生成对骨代谢产生合成代谢作用。在分子水平上,它抑制核转录因子NF-κB,但不抑制其抑制剂IκBα。除了这些免疫调节作用和其他持久作用外,艾拉莫德还抑制环氧合酶2,该环氧合酶2可提供针对疼痛和炎症的协同短期作用。功效和耐受性与萨拉索磺胺吡啶相当,也许也与甲氨蝶呤相当。对甲氨蝶呤反应不足的患者与甲氨蝶呤联合使用具有协同作用,并且不会显着增加不良事件。肝酶升高和血小板减少症是最需要注意的副作用。总而言之,伊古拉莫德是类风湿关节炎小分子药物治疗的受欢迎的补充。

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