Rutgers, The State University of New Jersey, Piscataway, NJ, USA.
Ann Pharmacother. 2013 Sep;47(9):1153-60. doi: 10.1177/1060028013500647.
To review the pharmacology and clinical data for teriflunomide in relapsing multiple sclerosis (MS).
A literature search from 1966 to May 2013 using PubMed/MEDLINE, Web of Science, International Pharmaceutical Abstracts, Academic Search Premiere, Science Citation Index, and the national clinical trials registry was performed using the terms teriflunomide, HMR1726, and A771726. All articles containing human clinical trial data and relevant pharmacologic information were reviewed.
STUDY SELECTION/DATA EXTRACTION: Phase 2 and phase 3 clinical trials for teriflunomide were evaluated. All peer-reviewed articles with clinically relevant information were reviewed. Priority for inclusion was placed on randomized controlled trials.
Three phase 2 and three phase 3 clinical trials have evaluated teriflunomide as monotherapy or as adjunctive therapy in approximately 3000 patients with relapsing forms of MS. The phase 3 studies used annualized relapse rate, magnetic resonance imaging changes, and Expanded Disability Status Scale scores as outcome measures. One additional Phase 3 clinical study is ongoing. The annualized relapse rates and magnetic resonance imaging findings were improved compared to those with placebo and similar to or improved compared with those with subcutaneously administered interferon-β-1a 44 µg thrice weekly. Durability of response is supported by open-label extension studies. Common adverse events include increased liver function enzymes, alopecia, diarrhea, influenza, nausea, and paresthesias. Treatment discontinuation was not common and occurred in approximately 10% of patients in phase 3 studies.
Teriflunomide is an effective and safe oral treatment option for relapsing MS. It can be used as monotherapy or added to an interferon or glatiramer acetate. It reduces the rate of relapse and may slow disease progression. The advantages of this drug are the convenience of oral administration and good tolerability. The disadvantage is the lack of long-term safety data and data about the benefit of combination therapy.
综述特立氟胺在多发性硬化症（MS）复发中的药理学和临床数据。
使用 PubMed/MEDLINE、Web of Science、国际药学文摘、学术搜索 Premiere、科学引文索引和国家临床试验注册处，从 1966 年到 2013 年 5 月进行文献检索，检索词为特立氟胺、HMR1726 和 A771726。所有包含人类临床试验数据和相关药理信息的文章均进行了回顾。
研究选择/数据提取：评估了特立氟胺的 2 期和 3 期临床试验。所有具有临床相关信息的同行评议文章均进行了回顾。纳入的优先顺序为随机对照试验。
3 项 2 期和 3 项 3 期临床试验评估了特立氟胺作为单药或作为辅助治疗在约 3000 例复发型多发性硬化症患者中的应用。3 期研究的结果测量指标为年复发率、磁共振成像变化和扩展残疾状况量表评分。一项额外的 3 期临床研究正在进行中。与安慰剂相比，年复发率和磁共振成像结果得到改善，与皮下注射每周 3 次的干扰素-β-1a 44 µg 相比，结果相似或改善。开放性扩展研究支持疗效的持久性。常见的不良反应包括肝功能酶升高、脱发、腹泻、流感、恶心和感觉异常。治疗中断并不常见，约占 3 期研究中 10%的患者。
特立氟胺是一种有效的、安全的多发性硬化症复发治疗选择。它可以作为单药治疗或与干扰素或那他珠单抗联合使用。它可降低复发率并可能减缓疾病进展。该药的优点是口服给药方便且耐受性良好。缺点是缺乏长期安全性数据和联合治疗获益的数据。
