de Lartigue J
Camberley, Surrey, UK.
Drugs Today (Barc). 2012 Aug;48(8):533-43. doi: 10.1358/dot.2012.48.8.1855926.
The autoimmune disease rheumatoid arthritis (RA) causes severe disability through chronic and destructive inflammation of the synovial joints. Currently available therapeutic options, including disease-modifying antirheumatic drugs (DMARDs) and biologic agents, often fail to adequately prevent disease progression. Tofacitinib (CP-690550) is an inhibitor of the Janus kinase family; tyrosine kinase receptors expressed in lymphoid cells that are involved in the signaling of cytokines important for the production and function of various immune cells implicated in RA pathogenesis. Tofacitinib has been evaluated in phase II, phase III and long-term extension studies, as both monotherapy and in combination with methotrexate and other DMARDs, and demonstrates statistically significant and clinically meaningful improvements in the signs and symptoms of RA, patient health, physical functioning and quality of life, while having a manageable safety profile. It is currently under evaluation for approval for the treatment of adults with RA by several regulatory agencies around the world.
自身免疫性疾病类风湿性关节炎(RA)通过滑膜关节的慢性和破坏性炎症导致严重残疾。目前可用的治疗选择,包括改善病情抗风湿药(DMARDs)和生物制剂,往往无法充分预防疾病进展。托法替布(CP-690550)是一种Janus激酶家族抑制剂;在淋巴细胞中表达的酪氨酸激酶受体,参与细胞因子信号传导,这些细胞因子对RA发病机制中涉及的各种免疫细胞的产生和功能很重要。托法替布已在II期、III期和长期扩展研究中进行了评估,作为单一疗法以及与甲氨蝶呤和其他DMARDs联合使用,在RA的体征和症状、患者健康、身体功能和生活质量方面显示出具有统计学意义和临床意义的改善,同时具有可控的安全性。目前,全球多个监管机构正在对其进行评估,以批准用于治疗成人RA。