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BioDrugs. 2014 Feb;28(1):75-106. doi: 10.1007/s40259-013-0076-8.
Tocilizumab (Actemra®, RoActemra®) is a humanized monoclonal antibody that acts as an interleukin-6 receptor antagonist. Intravenous tocilizumab as monotherapy or in combination with disease-modifying anti-rheumatic drugs (DMARDs) is indicated for the treatment of adult patients with moderate to severe active rheumatoid arthritis (RA) who had an inadequate response to one or more DMARDs or tumor necrosis factor (TNF) α antagonists (the specific indication varies between countries); it may also be used as monotherapy in patients for whom continued methotrexate use is inappropriate. This article reviews the efficacy and tolerability of tocilizumab in these patients and briefly summarizes its pharmacology. Several large well-designed clinical trials and routine clinical practice studies showed that tocilizumab was an effective and generally well tolerated biologic for the treatment of adults with RA, including those with an inadequate response to DMARDs or TNFα antagonists. In these studies, tocilizumab as monotherapy or in combination with DMARDs (including methotrexate) had beneficial effects on the signs and symptoms of disease, health-related quality of life/physical function, and/or radiologic disease progression. In addition, tocilizumab monotherapy was more effective than adalimumab monotherapy in improving the signs and symptoms of disease in patients for whom continued methotrexate use was inappropriate. As with other biologic DMARDS, infections were the most common adverse event associated with tocilizumab therapy. Pooled and meta-analyses demonstrated that the efficacy and tolerability profile of tocilizumab was sustained during long-term (up to 9 years) therapy. Although additional comparative data are needed to position tocilizumab more definitively with respect to other biologic DMARDs, current evidence indicates that tocilizumab is effective as a first- or subsequent-line biologic in patients with moderate to severe RA.
托珠单抗(雅美罗)是一种人源化的单克隆抗体,作为白细胞介素-6 受体拮抗剂发挥作用。静脉注射托珠单抗单药治疗或与改善病情的抗风湿药物(DMARDs)联合治疗,适用于对一种或多种 DMARDs 或肿瘤坏死因子(TNF)α拮抗剂治疗反应不足的中重度活动性类风湿关节炎(RA)成年患者(具体适应证因国家而异);也可用于继续使用甲氨蝶呤不合适的患者。本文综述了托珠单抗在这些患者中的疗效和耐受性,并简要总结了其药理学。几项大型精心设计的临床试验和常规临床实践研究表明,托珠单抗是一种有效且通常耐受性良好的生物制剂,可用于治疗 RA 成人患者,包括对 DMARDs 或 TNFα拮抗剂反应不足的患者。在这些研究中,托珠单抗单药或联合 DMARDs(包括甲氨蝶呤)对疾病的体征和症状、健康相关生活质量/身体功能和/或影像学疾病进展均有有益影响。此外,托珠单抗单药治疗在继续使用甲氨蝶呤不合适的患者中改善疾病体征和症状的效果优于阿达木单抗单药治疗。与其他生物 DMARDs 一样,感染是托珠单抗治疗最常见的不良事件。汇总分析和荟萃分析表明,托珠单抗在长期(长达 9 年)治疗期间疗效和耐受性特征保持不变。尽管需要更多的比较数据来更明确地确定托珠单抗与其他生物 DMARDs 的地位,但现有证据表明,托珠单抗是中重度 RA 患者的有效一线或二线生物制剂。