抗类风湿关节炎新药托法替尼的药理与临床研究进展

Pharmacological and clinical studies of tofacitinib citrate

托法替尼为作用于细胞内酪氨酸激酶的小分子口服抑制剂,用于治疗成人甲氨喋呤反应不佳或不能耐受的中度至重度活动性类风湿性关节炎,临床可与甲氨喋呤及其他非生物类DMARDs联合使用。本文就其作用机制、药效学、药动学、相互作用、临床评价及安全性等方面进行综述。

Tofacitinib citrate, an inhibitor of Janus kinases （JAKs）, is indicated for the treatment of adult patients with moderately to severely active rheumatoid arthritis who have had an inadequate response or intolerance to methotrexate. It may be used as monotherapy or in combination with methotrexate or other nonbiologic disease-modifying antirheumatic drugs. The mechanism, pharmacodynamics, pharmacokinetics, drug interaction, clinical evaluation and safety of tofacitinib citrate were reviewed.