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Drugs. 2017 Apr;77(6):697-704. doi: 10.1007/s40265-017-0723-3.
Baricitinib (Olumiant™) is an orally-administered, small-molecule, janus-associated kinase (JAK) inhibitor developed by Eli Lilly and Incyte Corporation for the treatment of rheumatoid arthritis (RA), atopic dermatitis and systemic lupus erythematosus. JAKs transduce intracellular signals from cell surface receptors for various cytokines and growth factors involved in inflammation and immune function, suggesting JAK inhibitors may be of therapeutic benefit in inflammatory conditions. In February 2017, baricitinib was approved in the EU, as monotherapy or in combination with methotrexate, for the treatment of moderate to severe active rheumatoid arthritis in adult patients who have responded inadequately to, or who are intolerant to one or more disease-modifying anti-rheumatic drugs (DMARDs). Regulatory approval to market baricitinib as a treatment for RA has also been sought in the USA and Japan. This article summarizes the milestones in the development of baricitinib leading to this first global approval for the treatment for moderate to severe active RA in adult patients who have responded inadequately to, or are intolerant to one or more DMARDs.
巴利昔替尼（Olumiant™）是由礼来公司和因塞特公司开发的一种口服、小分子、Janus 相关激酶（JAK）抑制剂，用于治疗类风湿关节炎（RA）、特应性皮炎和系统性红斑狼疮。JAK 可将细胞表面受体传递给各种细胞因子和生长因子的细胞内信号，参与炎症和免疫功能，这表明 JAK 抑制剂可能对炎症性疾病具有治疗益处。2017 年 2 月，巴利昔替尼在欧盟获得批准，可作为单药或与甲氨蝶呤联合使用，用于治疗对一种或多种疾病修饰抗风湿药物（DMARDs）反应不足或不耐受的中重度活跃性类风湿关节炎成年患者。在美国和日本，也寻求了将巴利昔替尼用于治疗 RA 的监管批准。本文总结了巴利昔替尼开发过程中的重要里程碑，最终该药在全球获批用于治疗对一种或多种 DMARDs 反应不足或不耐受的中重度活跃性 RA 成年患者。
