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小分子靶向 JAKs——类风湿关节炎治疗的新方法。

Small molecules targeting JAKs--a new approach in the treatment of rheumatoid arthritis.

机构信息

Department of Rheumatology and Clinical Immunology, Charité-Universitätsmedizin Berlin, Free University and Humboldt University of Berlin, Charitéplatz 1, D-10117 Berlin, Germany.

出版信息

Rheumatology (Oxford). 2013 Aug;52(8):1352-7. doi: 10.1093/rheumatology/kes417. Epub 2013 Feb 1.

DOI:10.1093/rheumatology/kes417
PMID:23378664
Abstract

Advances in the treatment of RA in the past decade have been achieved mainly by using combinations of different conventional and biologic DMARDs. However, until now no final victory has been achieved over this organ damaging and potentially life-threatening systemic autoimmune disease. Few patients, notably those with established disease, stay in remission permanently, even using advanced treatment concepts. Thus novel approaches, especially for patients resistant to biologics, are urgently needed. Pro-inflammatory signalling pathways beyond the level of cytokines and receptors have been intensively elaborated and provide such potential targets. This review focuses on the development of new small molecule inhibitors of Janus kinases in clinical trials in RA.

摘要

过去十年,RA 的治疗进展主要通过使用不同的传统和生物 DMARDs 联合治疗来实现。然而,到目前为止,尚未在这种可能导致器官损伤和危及生命的系统性自身免疫性疾病上取得最终胜利。即使使用先进的治疗理念,也只有少数患者(尤其是那些患有已确诊疾病的患者)能永久缓解。因此,迫切需要新的治疗方法,尤其是针对生物制剂耐药的患者。细胞因子和受体水平以上的促炎信号通路已经得到了深入研究,并提供了潜在的治疗靶点。本综述重点介绍了在 RA 临床试验中新型 Janus 激酶小分子抑制剂的开发。

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