Kucharz Eugeniusz J, Stajszczyk Marcin, Kotulska-Kucharz Anna, Batko Bogdan, Brzosko Marek, Jeka Sławomir, Leszczyński Piotr, Majdan Maria, Olesińska Marzena, Samborski Włodzimierz, Wiland Piotr
Department of Internal Medicine, Rheumatology, and Clinical Immunology, Medical University of Silesia in Katowice, Poland.
Department of Rheumatology and Autoimmune Diseases, Silesian Centre for Rheumatology, Rehabilitation, and Disability Prevention in Ustroń, Poland.
Reumatologia. 2018;56(4):203-211. doi: 10.5114/reum.2018.77971. Epub 2018 Aug 31.
Tofacitinib is a newly approved small-molecule targeted synthetic disease-modifying antirheumatic drug. The drug was designed as a selective and specific inhibitor of pro-inflammatory receptor signalling. Tofacitinib inhibits the process of intracellular signalling from the receptor to the cellular nucleus and inhibits the inflammation process via a new pathway (inhibition of the Janus kinases), which is unavailable to biological medicines. Tofacitinib has been approved for use in the treatment of patients with moderate to severe active RA. The drug may be used in combination with methotrexate or another conventional synthetic disease-modifying antirheumatic drug or in monotherapy. The efficacy of tofacitinib has been confirmed in several clinical trials. The drug inhibits radiographic progression of the disease. The innovative mechanism of action of tofacitinib is a noteworthy feature because it offers hope of effective treatment for patients who fail to respond to other drugs. The presented article discusses the mechanism of action and the clinical application of tofacitinib. Tofacitinib represents a new group of disease-modifying antirheumatic drugs that can be placed on an equal footing with biological drugs already available.
托法替布是一种新获批的小分子靶向合成抗风湿药物。该药物被设计为促炎受体信号传导的选择性和特异性抑制剂。托法替布抑制从受体到细胞核的细胞内信号传导过程,并通过一种生物药物无法采用的新途径(抑制 Janus 激酶)抑制炎症过程。托法替布已获批用于治疗中度至重度活动性类风湿关节炎患者。该药物可与甲氨蝶呤或另一种传统合成抗风湿药物联合使用,也可单药治疗。托法替布的疗效已在多项临床试验中得到证实。该药物可抑制疾病的影像学进展。托法替布创新的作用机制是一个值得关注的特点,因为它为对其他药物无反应的患者提供了有效治疗的希望。本文讨论了托法替布的作用机制和临床应用。托法替布代表了一类新的抗风湿药物,可与现有的生物药物相媲美。