JAK/STAT是一類重要的細(xì)胞因子信號傳導(dǎo)通路，與類風(fēng)濕性關(guān)節(jié)炎及銀屑病等許多疾病相關(guān)。美國輝瑞公司研發(fā)的JAK抑制劑托法替尼（Tofacitinib，CP-690550）能選擇性抑制JAK3激酶，美國食品和藥物管理局（FDA）已于2012年11月批準(zhǔn)其用于中至重度類風(fēng)濕性關(guān)節(jié)炎的治療。綜述其作用機(jī)制、合成方法、藥效與藥動學(xué)、臨床研究進(jìn)展，為同類新藥的研發(fā)提供參考。

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.

國家重大新藥創(chuàng)制專項(xiàng)（2011ZX09401-009）