Vasiliou S
Thomson Reuters, Barcelona, Spain.
Drugs Today (Barc). 2010 May;46(5):315-25. doi: 10.1358/dot.2010.46.5.1497556.
The sphingosine-1-phosphate receptor modulator fingolimod (FTY-720), which acts by preventing lymphocyte egress from lymph nodes thus reducing lymphocyte infiltration into the central nervous system (CNS), represents a novel therapeutic modality for the treatment of multiple sclerosis (MS). Results obtained from preclinical studies have also attributed a potential neuroprotective and reparative function to the agent within the CNS. Clinical evaluation in placebo-controlled trials in healthy individuals and MS patients revealed favorable safety and superior efficacy. Fingolimod was also reported to exhibit superiority, with respect to relapse rates and magnetic resonance imaging (MRI) outcomes, compared with the established MS therapeutic interferon beta-1a (IFN-beta-1a) in patients with relapsing-remitting MS in a 12-month clinical study. The oral route of administration of fingolimod renders it a more convenient therapeutic option than intramuscular IFN-beta-1a, while its lipophilicity which permits ready crossing of the blood-brain-barrier may result in enhanced activity. The positive risk-to-benefit profile of the agent supports the once-daily administration regimen for the treatment of MS.
鞘氨醇-1-磷酸受体调节剂芬戈莫德（FTY-720）通过阻止淋巴细胞从淋巴结流出，从而减少淋巴细胞浸润到中枢神经系统（CNS），代表了一种治疗多发性硬化症（MS）的新型治疗方式。临床前研究结果还表明该药物在中枢神经系统内具有潜在的神经保护和修复功能。在健康个体和MS患者中进行的安慰剂对照试验的临床评估显示出良好的安全性和卓越的疗效。在一项为期12个月的临床研究中，与已确立的MS治疗药物干扰素β-1a（IFN-β-1a）相比，对于复发缓解型MS患者，芬戈莫德在复发率和磁共振成像（MRI）结果方面也显示出优越性。芬戈莫德的口服给药途径使其成为比肌肉注射IFN-β-1a更方便的治疗选择，而其亲脂性使其能够轻松穿过血脑屏障，这可能会增强其活性。该药物积极的风险效益比支持了MS治疗的每日一次给药方案。
