[关键词]
[摘要]
JAK/STAT是一类重要的细胞因子信号传导通路,与类风湿性关节炎及银屑病等许多疾病相关。美国辉瑞公司研发的JAK抑制剂托法替尼(Tofacitinib,CP-690550)能选择性抑制JAK3激酶,美国食品和药物管理局(FDA)已于2012年11月批准其用于中至重度类风湿性关节炎的治疗。综述其作用机制、合成方法、药效与药动学、临床研究进展,为同类新药的研发提供参考。
[Key word]
[Abstract]
Janus kinase (JAK)/STAT cytokine signal transduction pathway is believed to play an important role in many diseases,such as rheumatoid arthritis and psoriasis. Tofacitinib (CP-690550) is a selective inhibitor of JAK3 kinase developed by Pfizer Inc.. The U.S. Food and Drug Administration approved tofacitinib for the treatment of moderate to severe rheumatoid arthritis disease in November 2012. The mechanism, synthetic method, efficacy, pharmacokinetics, and clinical research progress of tofacitinib have been summarized in the paper. We would like to provide some reference for the research and development of congeneric new drugs.
[中图分类号]
[基金项目]
国家重大新药创制专项(2011ZX09401-009)