Ward Melanie D, Jones David E, Goldman Myla D
University of Virginia, Department of Neurology , PO Box 800394, Charlottesville, VA 22908 , USA.
Expert Opin Drug Saf. 2014 Jul;13(7):989-98. doi: 10.1517/14740338.2014.920820.
Fingolimod (Gilenya®, FTY720) is an oral sphingosine-1-phosphate analogue that was approved by the FDA in 2010 for the treatment of relapsing forms of multiple sclerosis (MS). Fingolimod's mechanism of action is primarily related to lymphocyte sequestration in primary and secondary lymphoid tissues. Phase III trials demonstrated a reduction in annualized relapse rate and MRI progression in fingolimod-treated subjects compared with both placebo and IFN-β-treated subjects. Frequent adverse effects include fatigue, gastrointestinal disturbance, headache and upper respiratory tract infection. More serious, but rare, adverse events associated with fingolimod include atrioventricular block, symptomatic bradycardia, herpetic viral infections and macular edema.
We discuss the mechanism of action, pharmacokinetics, clinical efficacy and safety profile of fingolimod in patients with relapsing MS.
Fingolimod is an effective treatment for relapsing MS and its oral route of administration may be preferred by some. Fingolimod is generally well tolerated but requires diligence in patient selection and monitoring. Additional information is needed regarding risk of infection, malignancy and rebound disease with long-term use of fingolimod.
芬戈莫德（捷灵亚®，FTY720）是一种口服的1-磷酸鞘氨醇类似物，于2010年获美国食品药品监督管理局（FDA）批准用于治疗复发型多发性硬化症（MS）。芬戈莫德的作用机制主要与淋巴细胞在一级和二级淋巴组织中的滞留有关。III期试验表明，与安慰剂组和干扰素-β治疗组相比，接受芬戈莫德治疗的受试者年化复发率和磁共振成像（MRI）进展均有所降低。常见的不良反应包括疲劳、胃肠道不适、头痛和上呼吸道感染。与芬戈莫德相关的更严重但罕见的不良事件包括房室传导阻滞、症状性心动过缓、疱疹病毒感染和黄斑水肿。
我们讨论了芬戈莫德在复发型MS患者中的作用机制、药代动力学、临床疗效和安全性。
芬戈莫德是复发型MS的一种有效治疗方法，其口服给药途径可能为一些患者所青睐。芬戈莫德总体耐受性良好，但在患者选择和监测方面需要谨慎。关于长期使用芬戈莫德的感染风险、恶性肿瘤风险和疾病复发风险，还需要更多信息。
