Instituto de Neurociencias Clínicas, Hospital Regional Universitario Carlos Haya, Málaga, Spain.
Neurologia. 2011 Mar;26(2):111-7. doi: 10.1016/j.nrl.2010.07.027.
Multiple sclerosis (MS) is a chronic disease of the central nervous system, probably of autoimmune origin. Its early treatment with interferon beta or glatiramer acetate reduces the number of exacerbations, slows disability progression and improves the quality of life, but these treatments are only partially effective and require parenteral administration.
To review current experience with laquinimod as a novel immunomodulatory therapy for relapsing-remitting MS (RRMS).
Laquinimod is a new quinolone-carboxamide that has shown efficacy in various animal models of autoimmune disease, including MS. Laquinimod shows immunomodulatory effects, probably through Th1/Th2 shift, but does not lead to immunosuppression. Laquinimod is metabolised primarily by the CYP3A4 enzyme in the liver. Phase II studies in RRMS demonstrate a dose-response effect on disease activity, measured by the number of active lesions on brain magnetic resonance imaging, and show favourable tolerability and safety based on clinical and laboratory indicators. Two Phase III studies currently in progress are evaluating the efficacy of laquinimod 0.6 mg/day in RRMS. The drug was granted a fast track review by the FDA in 2009.
Laquinimod is a novel, orally administered immunomodulator that has advanced to phase III study, a pre-submission stage to the regulatory agencies, and may become an alternative to the current injectable first-line treatments for RRMS.
多发性硬化症（MS）是一种中枢神经系统的慢性疾病，可能是自身免疫性疾病。早期使用干扰素β或醋酸格拉替雷治疗可减少恶化次数，减缓残疾进展并提高生活质量，但这些治疗方法仅部分有效，且需要进行肠胃外给药。
综述拉克替胺作为一种新型免疫调节疗法治疗复发缓解型多发性硬化症（RRMS）的最新临床经验。
拉克替胺是一种新型喹诺酮羧酸酰胺类药物，已在包括多发性硬化症在内的多种自身免疫性疾病的动物模型中显示出疗效。拉克替胺具有免疫调节作用，可能通过 Th1/Th2 偏移发挥作用，但不会导致免疫抑制。拉克替胺主要通过肝脏中的 CYP3A4 酶代谢。RRMS 的 II 期研究表明，该药对疾病活动具有剂量反应作用，通过脑部磁共振成像上的活跃病变数量来衡量，并且基于临床和实验室指标，具有良好的耐受性和安全性。目前正在进行两项 III 期研究，评估拉克替胺 0.6mg/天治疗 RRMS 的疗效。该药于 2009 年获得 FDA 的快速通道审查。
拉克替胺是一种新型的口服免疫调节剂，已进入 III 期研究阶段，这是向监管机构提交申请前的一个阶段，可能成为 RRMS 目前一线注射治疗的替代方案。
