Ruhr-University Bochum, Department of Neurology at St. Josef-Hospital Bochum, Gudrunstr. 56, 44791 Bochum, Germany.
Expert Opin Drug Metab Toxicol. 2011 Mar;7(3):365-70. doi: 10.1517/17425255.2011.556618. Epub 2011 Feb 10.
MS is a chronic immunological disease of the CNS. Due to a lack of curative treatment approaches, current principles aim at the reduction of inflammatory disease activity. Today, many different substances are under investigation in Phase III clinical trials and hold promise in the treatment of relapsing-remitting MS (RRMS). Laquinimod is a promising new orally administered substance which has demonstrated beneficial effects in placebo-controlled trials in patients with RRMS and is currently under investigation in two global Phase III trials.
The authors review the pharmaceutical properties of laquinimod, its suggested mechanisms of action, clinical efficacy and adverse profile. This review contains data that have been presented by experts in the field at international meetings and congresses and that have been published in peer-reviewed journals.
While laquinimod has been shown to have a promising safety profile, its mechanisms of action are not completely understood and further research is necessary to clarify this. Studies conducted in EAE, the mouse model of MS, have demonstrated immunomodulatory and neuroprotective mechanisms of action. Hopefully, the two current pivotal Phase III trials currently underway will shed some light on laquinimod confirming its clinical potential and add to the current armamentarium for the treatment of RRMS.
多发性硬化症（MS）是一种中枢神经系统的慢性免疫性疾病。由于缺乏有效的治疗方法，目前的治疗原则旨在减少炎症性疾病的活动。目前，许多不同的物质正在进行 III 期临床试验，并在治疗复发缓解型多发性硬化症（RRMS）方面具有前景。拉喹莫德是一种有前途的新型口服药物，在 RRMS 患者的安慰剂对照试验中已显示出有益效果，目前正在两项全球 III 期试验中进行研究。
作者综述了拉喹莫德的药物特性、作用机制、临床疗效和不良反应。本综述包含了在国际会议和大会上由该领域专家介绍的数据，以及已在同行评议期刊上发表的数据。
虽然拉喹莫德已显示出良好的安全性，但它的作用机制尚不完全清楚，需要进一步研究来阐明这一点。在实验性自身免疫性脑脊髓炎（EAE），多发性硬化症的小鼠模型中，已经证实了其免疫调节和神经保护作用机制。希望目前正在进行的两项关键的 III 期临床试验能够揭示拉喹莫德的临床潜力，并为 RRMS 的治疗提供更多的选择。
