非戈替尼，一种新型的 JAK1 选择性抑制剂，用于治疗类风湿关节炎：临床试验概述。
Filgotinib, a novel JAK1-preferential inhibitor for the treatment of rheumatoid arthritis: An overview from clinical trials.
机构信息
The First Department of Internal Medicine, University of Occupational and Environmental Health Japan, Kitakyushu, Japan.
School of Medicine, University of California, San Diego, CA, USA.
出版信息
Mod Rheumatol. 2022 Jan 5;32(1):1-11. doi: 10.1080/14397595.2021.1902617.
In the treatment of rheumatoid arthritis (RA), Janus kinase inhibitors (jakinibs) represent an emerging class of targeted therapies in addition to biologics. The number of jakinibs has been growing and as of 2020, filgotinib was the latest jakinib to enter the international market for treating RA. Filgotinib has demonstrated preferential inhibition of JAK1-dependent cytokine signaling in in vitro assays. It has been evaluated in the DARWIN (phase 2) and FINCH (phase 3) series of clinical studies for treating patients with moderately-to-severely active RA. Filgotinib received regulatory approval in Japan and Europe in September 2020, while in August 2020 the United States Food and Drug Administration requested additional data from two ongoing clinical studies assessing the potential impact of filgotinib on sperm parameters. This article will review the pharmacological properties, efficacy, and safety of filgotinib as demonstrated in clinical studies. Expert opinion will be provided on jakinibs for RA treatment from the viewpoints of basic research and clinical practice.
在类风湿关节炎（RA）的治疗中，除了生物制剂外，Janus 激酶抑制剂（Jakinibs）代表了一类新兴的靶向治疗药物。Jakinib 的数量一直在增加，截至 2020 年，非戈替尼是最新进入治疗 RA 的国际市场的 Jakinib。非戈替尼在体外试验中表现出对 JAK1 依赖性细胞因子信号的优先抑制作用。它已在 DARWIN（第 2 阶段）和 FINCH（第 3 阶段）系列临床研究中进行了评估，用于治疗中重度活跃性 RA 患者。非戈替尼于 2020 年 9 月在日本和欧洲获得监管批准，而 2020 年 8 月，美国食品和药物管理局要求对两项正在进行的评估非戈替尼对精子参数潜在影响的临床研究提供额外数据。本文将综述临床研究中显示的非戈替尼的药理学特性、疗效和安全性。从基础研究和临床实践的角度提供了关于 RA 治疗用 Jakinib 的专家意见。
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