Leflunomide治疗风湿性关节炎。

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李EK, Tam LS,汤姆林森B

Leflunomide治疗风湿性关节炎。

其他。2004年4月,26 (4):447 - 59。

PubMed ID

15189743 (在PubMed

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文摘

背景:目前的药物治疗类风湿性关节炎(RA),包括非甾体类抗炎药物和疾病修饰治疗风湿病的药物,帮助控制炎症,但会导致显著的毒性。需要药物能够抑制炎症和修改底层免疫反应与改进的耐受性。Leflunomide代理影响炎症过程,尤其是在RA。目的:本文综述leflunomide的药理学,RA的批准使用,和主要临床试验的结果,包括不良事件。方法:通过搜索相关试验确定的英文文献索引EMBASE, MEDLINE,当前内容,科克伦对照试验从1980年1月至2003年11月注册。搜索条件仅限于leflunomide。结果:在3大III期临床试验(US301、MN301 MN302), leflunomide等价的临床疗效和耐受性甲氨蝶呤、柳氮磺胺吡啶,与安慰剂比较,卓越的疗效和耐受性。US301 (N = 482), ACR(美国风湿病学院)20反应率(> = 20%的患者比例从基线改进招标和关节肿胀数,病人的评估疼痛,病人和医生的全球评估疾病活动、身体功能、和急性期反应物值)在1年类似leflunomide和甲氨蝶呤与积极治疗显著大于安慰剂(分别为52%、46%和26%;同时,P < 0.001)。leflunomide被早期的功效(治疗4周后),并持续整个研究。 There was less radiographic damage in both active-treatment groups compared with placebo (leflunomide, P < or = 0.001; methotrexate, P = 0.02). In MN301 (N = 358), the ACR20 response rate at 6 months was similar with leflunomide and sulfasalazine and significantly greater with both active treatments compared with placebo (55%, 56%, and 29%, respectively; both, P < 0.001). Radiographic progression was also similar with leflunomide and sulfasalazine, both of which were significantly superior to placebo (Larsen score, 0.42, 0.41, and 1.4; both, P < 0.001). An extension of this study revealed maintenance of efficacy at 12 and 24 months. In MN302 (intent-to-treat population, N = 999), 50.5% of patients in the leflunomide group were ACR20 responders at the end of 1 year, compared with 64.8% in the methotrexate group (P < 0.001 vs leflunomide). After 2 years, ACR20 response rates were similar with leflunomide and methotrexate (64.3% and 71.7%). The overall safety profile of leflunomide appears promising, although monitoring for elevations in liver enzymes and bone marrow suppression is recommended. The most common drug-related adverse events associated with leflunomide in these clinical trials were diarrhea, abnormalities in liver enzymes, rash, and hypertension.

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药物

Leflunomide

药物靶点

药物	目标	类	生物	药理作用	行动
Leflunomide	Dihydroorotate脱氢酶(醌),线粒体	蛋白质	人类	是的	抑制剂	细节