Alten R
Schlosspark-Klinik, Heubnerweg 2, 14059, Berlin, Deutschland,
Z Rheumatol. 2013 Nov;72(9):867-72. doi: 10.1007/s00393-013-1139-4.
Protein kinase inhibitors represent a novel and promising approach to the treatment of rheumatoid arthritis (RA). By targeting intracellular signaling pathways of cytokine-mediated reactions, these substances are able to interfere with critical immune processes that underly the pathology of RA. With tofacitinib, the first Janus kinase (JAK) inhibitor has been approved in the USA, as well as in Switzerland and other countries. Several other substances are currently undergoing phase II or phase III trials.A crucial question that will shape the future of these new drugs is whether they are safe and in particular, whether they are safer than biological therapies. This article provides an overview on current data concerning the efficacy and safety of the most promising substances and discusses the potential future role of intracellular kinase inhibitors.
蛋白激酶抑制剂是治疗类风湿性关节炎(RA)的一种新颖且有前景的方法。通过靶向细胞因子介导反应的细胞内信号通路,这些物质能够干扰构成RA病理学基础的关键免疫过程。托法替布作为首个Janus激酶(JAK)抑制剂已在美国、瑞士及其他国家获批。其他几种物质目前正处于II期或III期试验阶段。一个将决定这些新药未来走向的关键问题是它们是否安全,尤其是它们是否比生物疗法更安全。本文概述了有关最具前景物质的疗效和安全性的当前数据,并讨论了细胞内激酶抑制剂未来可能发挥的作用。