Department of Neurology, Heinrich-Heine-University, Moorenstraße 5, 40225 Düsseldorf, Germany.
Ther Adv Neurol Disord. 2014 Jul;7(4):195-205. doi: 10.1177/1756285614529615.
Multiple sclerosis (MS), an inflammatory disease affecting the central nervous system, is considered to exhibit an important neurodegenerative component as well. Laquinimod is an orally administered quinoline-3-carboxamide under development for the treatment of MS. In vitro and animal studies have revealed various mechanisms by which laquinimod may exert its effects on the immune and nervous systems. These include effects on the innate immune system that promote the differentiation of anti-inflammatory/regulatory T cells, the activation of microglia cells, an increase in the expression of brain-derived neurotrophic factor, as well as the prevention of inflammation-induced excitotoxicity. Two phase III studies revealed the clinical benefits of laquinimod in patients with relapsing-remitting MS and exhibited a benign safety profile for this drug. Ongoing clinical trials will help to define the optimal dose and indication for laquinimod in MS. This article reviews current experimental and clinical evidence on the role of laquinimod in patients with this disabling disease.
多发性硬化症（MS）是一种影响中枢神经系统的炎症性疾病，也被认为具有重要的神经退行性成分。拉喹莫德是一种正在开发用于治疗多发性硬化症的口服喹啉-3-甲酰胺。体外和动物研究揭示了拉喹莫德可能对免疫系统和神经系统产生影响的各种机制。这些机制包括对先天免疫系统的影响，促进抗炎/调节性 T 细胞的分化，激活小胶质细胞，增加脑源性神经营养因子的表达，以及预防炎症引起的兴奋毒性。两项 III 期研究揭示了拉喹莫德在复发缓解型多发性硬化症患者中的临床益处，并显示出该药具有良性的安全性特征。正在进行的临床试验将有助于确定拉喹莫德在多发性硬化症中的最佳剂量和适应症。本文综述了拉喹莫德在这种致残性疾病患者中的作用的现有实验和临床证据。
