Department of Respiratory Medicine, Allergy and Rheumatic Diseases, Osaka University Graduate School of Medicine, 2-2 Yamada-oka, Suita City, Osaka 565-0871, Japan.
Expert Rev Clin Immunol. 2010 Nov;6(6):843-54. doi: 10.1586/eci.10.70.
Tocilizumab is a humanized anti-IL-6 receptor monoclonal antibody, which binds to circulating soluble IL-6 receptor and membrane-expressed IL-6 receptor, inhibiting IL-6 binding to both forms of IL-6 receptor. Several Phase III clinical trials demonstrate the clinical efficacy of tocilizumab as monotherapy or with disease-modifying anti-rheumatic drugs for adult patients with moderately to severely active rheumatoid arthritis. Tocilizumab in combination with methotrexate after 24 weeks of treatment could induce disease remission in 30% of patients with rheumatoid arthritis refractory to anti-TNF antagonist therapy. The most common adverse reactions reported in clinical studies are upper respiratory tract infection, nasopharyngitis, headache, hypertension and mild, reversible increases in alanine aminotransferase enzymes. Serious adverse reactions include infections, gastrointestinal perforations and hypersensitivity reactions, including anaphylaxis. The clinical efficacy and safety of tocilizumab has led to the approval of this innovative drug for the treatment of rheumatoid arthritis in more than 70 countries worldwide.
托珠单抗是一种人源化抗 IL-6 受体单克隆抗体，可与循环中的可溶性 IL-6 受体和膜表达的 IL-6 受体结合，从而抑制 IL-6 与这两种形式的 IL-6 受体结合。几项 III 期临床试验表明，托珠单抗作为单药或与改善病情的抗风湿药物联合用于中重度活动性类风湿关节炎成年患者具有临床疗效。托珠单抗联合甲氨蝶呤治疗 24 周后，可诱导 30%对 TNF 拮抗剂治疗耐药的类风湿关节炎患者疾病缓解。在临床研究中报告的最常见不良反应为上呼吸道感染、鼻咽炎、头痛、高血压和丙氨酸氨基转移酶轻度、可逆升高。严重不良反应包括感染、胃肠道穿孔和过敏反应，包括过敏反应。托珠单抗的临床疗效和安全性已促使该创新药物在全球 70 多个国家获得批准，用于治疗类风湿关节炎。
