McKeage Kate, Lyseng-Williamson Katherine A
Springer, Private Bag 65901, Mairangi Bay, Auckland, 0754 New Zealand.
Drugs Ther Perspect. 2018;34(10):451-456. doi: 10.1007/s40267-018-0551-x. Epub 2018 Aug 29.
Oral fostamatinib is an orally administered small molecule spleen tyrosine kinase (SYK) inhibitor approved for the treatment of adults with chronic immune thrombocytopenia (ITP) who have an inadequate response to a previous treatment. Fostamatinib has a unique mechanism of action, whereby its active metabolite targets the SYK-mediated pathway of platelet destruction. In clinical trials, fostamatinib provided durable responses in adults with chronic ITP who had not responded or had relapsed following treatment with one or more prior ITP therapies, including corticosteroids, thrombopoietin receptor agonists, rituximab, and/or splenectomy. Most patients who respond to fostamatinib maintain platelet counts of > 50 × 10/L for periods of ≥ 12 months. The most common adverse events reported with fostamatinib in clinical trials were diarrhea, hypertension, nausea, and increased transaminase levels.
口服福斯替尼是一种口服小分子脾酪氨酸激酶（SYK）抑制剂，被批准用于治疗对先前治疗反应不足的成人慢性免疫性血小板减少症（ITP）。福斯替尼具有独特的作用机制，其活性代谢产物靶向SYK介导的血小板破坏途径。在临床试验中，福斯替尼为患有慢性ITP的成人提供了持久的反应，这些患者在用一种或多种先前的ITP疗法（包括皮质类固醇、血小板生成素受体激动剂、利妥昔单抗和/或脾切除术）治疗后没有反应或复发。大多数对福斯替尼有反应的患者血小板计数>50×10⁹/L并维持≥12个月。在临床试验中，福斯替尼报告的最常见不良事件是腹泻、高血压、恶心和转氨酶水平升高。
