Fedratinib (INREBIC®) is a JAK2-selective inhibitor that has been developed as an oral treatment for myelofibrosis. It was approved for the first time in the United States in August 2019 to treat adult patients with intermediate-2 or high-risk primary or secondary (post-polycythaemia vera or post-essential thrombocythemia) myelofibrosis. Fedratinib is an anilinopyrimidine derivative and is metabolized by CYP3A4, CYP2C19 and flavin-containing monooxygenase-3. Fedratinib is mainly excreted in faeces, and the effective half-life is 41 hours. The recommended dosage is 400 mg once daily (with or without food. The dosage should be reduced to 200 mg once daily in patients receiving CYP3A4 inhibitors and in patients with severe renal impairment. Fedratinib's recent approval adds to the few therapeutic option choices available to individuals with MF. The most common adverse events were mild gastrointestinal toxicities. Fedratinib comes with a boxed warning about the risk of serious and potentially deadly encephalopathies, such as Wernicke's.

中文翻译：

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Fedratinib：药理学和临床应用综述

Fedratinib (INREBIC®) 是一种 JAK2 选择性抑制剂，已开发为骨髓纤维化的口服治疗药物。该药物于 2019 年 8 月在美国首次获得批准，用于治疗中 2 级或高危原发性或继发性（真性红细胞增多症后或原发性血小板增多症后）骨髓纤维化成年患者。 Fedratinib 是一种苯胺嘧啶衍生物，由 CYP3A4、CYP2C19 和含黄素单加氧酶 3 代谢。 Fedratinib主要经粪便排泄，有效半衰期为41小时。推荐剂量为 400 mg 每日一次（无论是否与食物一起服用）。接受 CYP3A4 抑制剂的患者和严重肾功能不全的患者的剂量应减少至 200 mg 每日一次。Fedratinib 最近的批准增加了个人可用的少数治疗选择MF。最常见的不良事件是轻度胃肠道毒性。Fedratinib 带有黑框警告，提示存在严重且可能致命的脑病（例如韦尼克氏脑病）的风险。