Laquinimod,一种治疗复发-缓解型多发性硬化症的新型口服自身免疫调节剂。

Alex Tselis
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摘要

Laquinimod是第二代喹啉-3-carboxamide,由Active Biotech AB和Teva Pharmaceutical Industries Ltd开发,用于治疗复发缓解型多发性硬化症(RRMS)。拉奎莫德在抑制实验性自身免疫性脑脊髓炎(RRMS的动物模型)方面显示出显著的活性。在I期和II期临床试验中,该药耐受性良好,对少数RRMS患者有一定疗效。药物的作用机制尚不清楚,可能涉及Th1到Th2/Th3的免疫偏离,促进神经营养因子的合成和释放,以及其他可能的神经保护作用。两项III期临床试验正在进行中,如果成功,将导致首个用于抑制多发性硬化症疾病活动的口服免疫调节药物获批。
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Laquinimod, a new oral autoimmune modulator for the treatment of relapsing-remitting multiple sclerosis.

Laquinimod, a second-generation quinoline-3-carboxamide, is being developed by Active Biotech AB and Teva Pharmaceutical Industries Ltd for the treatment for relapsing-remitting multiple sclerosis (RRMS). Laquinimod has demonstrated significant activity in suppressing experimental autoimmune encephalomyelitis, an animal model of RRMS. In phase I and II clinical trials, the drug was well tolerated, with some hints of efficacy in small numbers of patients with RRMS. While the mechanism of action of the drug is unknown, it likely involves Th1 to Th2/Th3 immune deviation, promotion of the synthesis and release of neurotrophic factors, and other possible neuroprotective effects. Two phase III clinical trials are ongoing and, if successful, will lead to the approval of the first oral immunomodulatory drug for suppressing multiple sclerosis disease activity.

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