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特立氟胺

Teriflunomide.

作者信息

Oh Jiwon, O'Connor Paul W

机构信息

Department of Neurology (JO), Johns Hopkins University, Baltimore, MD; and Division of Neurology, Department of Medicine (JO, PWO), St. Michael's Hospital, University of Toronto, Toronto, Canada.

出版信息

Neurol Clin Pract. 2013 Jun;3(3):254-260. doi: 10.1212/CPJ.0b013e318296f299.

DOI:10.1212/CPJ.0b013e318296f299
PMID:23914327
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3721245/
Abstract

Teriflunomide is a novel disease-modifying agent that was recently approved for use in the treatment of multiple sclerosis (MS). Teriflunomide has demonstrated clinical efficacy and safety in a number of large, multicenter, phase III clinical trials and is an attractive agent to add to the growing repertoire of available treatments for MS, as it has the benefit of oral administration. Furthermore, existing clinical experience with its parent drug, leflunomide, provides indirect long-term safety data. This review summarizes teriflunomide's pharmacologic properties, pivotal clinical trials, and safety profile, and ends with a discussion of the role of teriflunomide in the context of current and emerging MS treatment options.

摘要

特立氟胺是一种新型疾病修正药物,最近被批准用于治疗多发性硬化症(MS)。特立氟胺在多项大型多中心III期临床试验中已证明其临床疗效和安全性,并且由于其具有口服给药的优势,是可添加到不断增加的MS可用治疗药物中的一种有吸引力的药物。此外,其母体药物来氟米特的现有临床经验提供了间接的长期安全性数据。本综述总结了特立氟胺的药理特性、关键临床试验和安全性概况,并最后讨论了特立氟胺在当前和新兴的MS治疗选择背景下的作用。

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Teriflunomide.特立氟胺
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Teriflunomide, an immunomodulatory drug, exerts anticancer activity in triple negative breast cancer cells.来氟米特,一种免疫调节药物,在三阴性乳腺癌细胞中发挥抗癌活性。
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本文引用的文献

1
Teriflunomide added to interferon-β in relapsing multiple sclerosis: a randomized phase II trial.特立氟胺联合干扰素-β治疗复发型多发性硬化症的随机 II 期临床试验
Neurology. 2012 Jun 5;78(23):1877-85. doi: 10.1212/WNL.0b013e318258f7d4. Epub 2012 May 23.
2
Long-term follow-up of a phase 2 study of oral teriflunomide in relapsing multiple sclerosis: safety and efficacy results up to 8.5 years.口服特立氟胺治疗复发型多发性硬化症的 2 期研究的长期随访:安全性和疗效结果长达 8.5 年。
Mult Scler. 2012 Sep;18(9):1278-89. doi: 10.1177/1352458512436594. Epub 2012 Feb 3.
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Randomized trial of oral teriflunomide for relapsing multiple sclerosis.随机试验口服特立氟胺治疗复发型多发性硬化症。
N Engl J Med. 2011 Oct 6;365(14):1293-303. doi: 10.1056/NEJMoa1014656.
4
Leflunomide use in New Zealand. A national prospective post-marketing study.来氟米特在新西兰的应用。一项全国性前瞻性上市后研究。
Intern Med J. 2009 Feb;39(2):95-102. doi: 10.1111/j.1445-5994.2008.01792.x.
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Leflunomide-associated progressive multifocal leukoencephalopathy.
Arch Neurol. 2008 Nov;65(11):1538-9. doi: 10.1001/archneur.65.11.1538.
6
A Phase II study of the safety and efficacy of teriflunomide in multiple sclerosis with relapses.特立氟胺治疗复发型多发性硬化症安全性和有效性的II期研究。
Neurology. 2006 Mar 28;66(6):894-900. doi: 10.1212/01.wnl.0000203121.04509.31.
7
Disruption of the interaction of T cells with antigen-presenting cells by the active leflunomide metabolite teriflunomide: involvement of impaired integrin activation and immunologic synapse formation.活性来氟米特代谢物特立氟胺破坏T细胞与抗原呈递细胞的相互作用:整合素激活受损和免疫突触形成的参与。
Arthritis Rheum. 2005 Sep;52(9):2730-9. doi: 10.1002/art.21255.
8
Infectious CNS disease as a differential diagnosis in systemic rheumatic diseases: three case reports and a review of the literature.感染性中枢神经系统疾病作为系统性风湿性疾病的鉴别诊断:三例病例报告及文献综述
Ann Rheum Dis. 2003 Jan;62(1):50-7. doi: 10.1136/ard.62.1.50.
9
Inhibition of protein tyrosine phosphorylation in T cells by a novel immunosuppressive agent, leflunomide.新型免疫抑制剂来氟米特对T细胞中蛋白酪氨酸磷酸化的抑制作用。
J Biol Chem. 1995 May 26;270(21):12398-403. doi: 10.1074/jbc.270.21.12398.
10
The immunosuppressant leflunomide inhibits lymphocyte proliferation by inhibiting pyrimidine biosynthesis.免疫抑制剂来氟米特通过抑制嘧啶生物合成来抑制淋巴细胞增殖。
J Pharmacol Exp Ther. 1995 Nov;275(2):1043-9.