Tofacitinib (Tasocitinib, CP-690550, CP690550)，也称托法替尼或托法替布，是一种新型可口服的JAK3抑制剂，IC₅₀值为1 nM，作用于JAK1和JAK2的选择性相比于JAK3分别低100和20倍。Tofacitinib通过抑制JAK1和JAK3可阻断几种细胞因子的信号，包括IL-2、4、7、9、15和21。临床上，Tofacitinib用于治疗对甲氨蝶呤治疗反应不足或不耐受的中度至重度活动性类风湿性关节炎(RA)成人患者。

参考文献

1.Changelian PS, et al. Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor. Science. 2003;302(5646):875-8.

2.LaBranche TP, et al. JAK inhibition with tofacitinib suppresses arthritic joint structural damage through decreased RANKL production. Arthritis Rheum. 2012;64(11):3531-42.

3.Calama E, et al. Tofacitinib ameliorates inflammation in a rat model of airway neutrophilia induced by inhaled LPS. Pulm Pharmacol Ther. 2017;43:60-67.

4.Jiang JK, et al. Examining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550). J Med Chem. 2008;51(24):8012-8.

冰袋运输。粉末直接保存于-20℃，有效期2年。建议分装后-20℃避光保存，避免反复冻融。