Guarnera Cristina, Bramanti Placido, Mazzon Emanuela
IRCCS Centro Neurolesi "Bonino-Pulejo", Messina, Italy.
Drug Des Devel Ther. 2017 Jul 28;11:2193-2207. doi: 10.2147/DDDT.S137572. eCollection 2017.
In the therapeutic scenario of disease-modifying therapies for relapsing-remitting multiple sclerosis, the introduction of oral agents, starting in 2010 with fingolimod, has been a huge step forward in therapeutic options due to the easier administration route. Three oral drugs fingolimod, teriflunomide, and dimethyl fumarate, which are clinically approved for the treatment of relapsing-remitting multiple sclerosis, are reviewed in this work. Results of Phase III clinical trials and their extension studies showed that the three oral agents significantly reduced the annualized relapse rate - a superior efficacy compared to placebo. Fingolimod 0.5 mg consistently reduced clinical relapses and brain volume loss. In all Phase III studies, teriflunomide 14 mg dose showed a reduction in the risk of disability accumulation. Regarding safety profile, fingolimod had more safety issues than the other two agents. For this reason, it should be strictly monitored for risks of infections, cancers, and certain transitory effects such as irregular cardiac function, decreased lymphocyte count, and a higher level of liver enzymes. Adverse effects of teriflunomide are well characterized and can be considered manageable. The main risks marked with dimethyl fumarate were flushing and gastrointestinal events.
在复发缓解型多发性硬化症疾病修饰疗法的治疗方案中，自2010年芬戈莫德开始，口服药物的引入因给药途径更简便，在治疗选择上迈出了巨大的一步。本文综述了三种临床上被批准用于治疗复发缓解型多发性硬化症的口服药物——芬戈莫德、特立氟胺和富马酸二甲酯。III期临床试验及其扩展研究结果表明，这三种口服药物显著降低了年化复发率，与安慰剂相比疗效更佳。0.5毫克的芬戈莫德持续降低临床复发率和脑容量损失。在所有III期研究中，14毫克剂量的特立氟胺显示出残疾累积风险降低。在安全性方面，芬戈莫德比其他两种药物存在更多安全问题。因此，应严格监测其感染、癌症风险以及某些短暂效应，如心功能异常、淋巴细胞计数降低和肝酶水平升高。特立氟胺的不良反应特征明确，可认为是可控的。富马酸二甲酯的主要风险是潮红和胃肠道事件。
