Department of Rheumatology, Hospital Aranda de la Parra, Hidalgo 329-704, León 37000, GTO, Mexico.
Expert Rev Clin Immunol. 2012 Sep;8(7):609-15. doi: 10.1586/eci.12.63.
Fostamatinib (R788) is a prodrug rapidly converted to its active metabolite on oral administration. This (known as R406) is a potent inhibitor of spleen tyrosine kinase, required for the expression of a number of proinflammatory cytokines. Fostamatinib has shown significantly superior efficacy (when compared with placebo) in the control of patients with rheumatoid arthritis not responding to methotrexate in Phase II clinical trials. Treatment emergent adverse events with a higher frequency than in those on placebo included diarrhea, hypertension, urinary tract infections, neutropenia and elevated transaminases. The studied doses have shown a linear pharmacokinetic pattern and the administration of methotrexate does not affect it. Fostamatinib may have a role in the therapy of patients with rheumatoid arthritis with poor response to conventional therapy. If these results are confirmed once Phase III studies are completed, it may find a place in the evolving treatment algorithm for rheumatoid arthritis.
福他替尼（R788）是一种前体药物，在口服给药后迅速转化为其活性代谢物。这种（称为 R406）是一种有效的脾酪氨酸激酶抑制剂，对于表达许多促炎细胞因子是必需的。在 II 期临床试验中，与安慰剂相比，福他替尼在控制对甲氨蝶呤无反应的类风湿关节炎患者方面显示出明显更好的疗效。与安慰剂相比，发生率更高的治疗中出现的不良事件包括腹泻、高血压、尿路感染、中性粒细胞减少症和转氨酸升高。研究剂量表现出线性药代动力学模式，甲氨蝶呤的给药并不影响它。福他替尼可能在对常规治疗反应不佳的类风湿关节炎患者的治疗中发挥作用。如果一旦完成 III 期研究这些结果得到证实，它可能在不断发展的类风湿关节炎治疗算法中找到一席之地。
