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芬戈莫德治疗多发性硬化症:作用机制、临床结局和未来方向。

Fingolimod for multiple sclerosis: mechanism of action, clinical outcomes, and future directions.

机构信息

Department of Neurology and Department of Biomedicine, University Hospital Basel, Petersgraben, Switzerland.

出版信息

Curr Neurol Neurosci Rep. 2011 Oct;11(5):492-7. doi: 10.1007/s11910-011-0216-9.

DOI:10.1007/s11910-011-0216-9
PMID:21789537
Abstract

The oral sphingosine 1-phosphate receptor (S1PR) modulator fingolimod functionally antagonizes S1PR hereby blocking lymphocyte egress from secondary lymphoid organs to the peripheral blood circulation. This results in a reduction in peripheral lymphocyte counts, including potentially encephalitogenic T cells. In patients with relapsing multiple sclerosis fingolimod has been shown to be an effective treatment. In phase 2 and phase 3 studies fingolimod-treated patients had reduced disease activity clinically and in MRI. Although severe infectious complications occurred in single cases treated with fingolimod, the frequency of overall infections was comparable in fingolimod-treated patients and controls. Overall, in clinical studies fingolimod was well tolerated and had a favorable safety profile. In follow-up studies with continuous fingolimod, treatment showed sustained efficacy while being well tolerated.

摘要

口服鞘氨醇 1-磷酸受体(S1PR)调节剂芬戈莫德通过拮抗 S1PR 从而阻止淋巴细胞从次级淋巴器官渗出到外周血液循环。这导致外周淋巴细胞计数减少,包括潜在的致脑炎 T 细胞。在复发型多发性硬化症患者中,芬戈莫德已被证明是一种有效的治疗方法。在 2 期和 3 期研究中,接受芬戈莫德治疗的患者在临床和 MRI 上疾病活动度降低。尽管接受芬戈莫德治疗的个别病例出现了严重的感染并发症,但感染的总发生率在芬戈莫德治疗组和对照组之间无差异。总的来说,在临床研究中,芬戈莫德具有良好的耐受性和有利的安全性特征。在接受连续芬戈莫德治疗的随访研究中,治疗显示出持续的疗效,同时具有良好的耐受性。

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Lancet Neurol. 2011 Jun;10(6):520-9. doi: 10.1016/S1474-4422(11)70099-0. Epub 2011 May 13.
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Differential responses of human microglia and blood-derived myeloid cells to FTY720.人小神经胶质细胞和血源性髓系细胞对 FTY720 的不同反应。
J Neuroimmunol. 2011 Jan;230(1-2):10-6. doi: 10.1016/j.jneuroim.2010.08.006. Epub 2010 Sep 9.
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Sphingosine 1-phosphate receptor 1 and 3 are upregulated in multiple sclerosis lesions.
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IDCases. 2024 Jul 2;37:e02021. doi: 10.1016/j.idcr.2024.e02021. eCollection 2024.
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Sphingosine 1-Phosphate Lyase in the Developing and Injured Nervous System: a Dichotomy?鞘氨醇 1-磷酸裂解酶在发育和损伤神经系统中的双重作用?
Mol Neurobiol. 2023 Dec;60(12):6869-6882. doi: 10.1007/s12035-023-03524-3. Epub 2023 Jul 28.
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