ST LOUIS (MD Consult) - On January 11, 2009, Roche announced that the US Food and Drug Administration approved Actemra (tocilizumab) for the treatment of adult patients with moderately to severely active rheumatoid arthritis (RA) who have experienced an inadequate response to one or more tumor necrosis factor (TNF) antagonist therapies. Actemra is an interleukin-6 (IL-6) receptor-inhibiting monoclonal antibody. It may be used alone or in combination with methotrexate or other disease-modifying antirheumatic drugs (DMARDs).

Several key cytokines, including IL-6, are involved in the inflammatory process that occurs with RA, and research shows that IL-6 levels are elevated in patients with RA. According to Roche, Actemra is the first medication designed to specifically inhibit the biologic activity of IL-6.

 

Actemra has been studied in 5 multinational phase 3 studies involving more than 4,000 patients. Data from these studies showed that Actemra, used alone or in combination with methotrexate or other DMARDs, was associated with a significant reduction in the signs and symptoms of RA regardless of previous therapy, compared with DMARDs alone.

 

The overall safety profile of Actemra is consistent across all global clinical studies. Serious adverse effects associated with Actemra include serious infections that may lead to hospitalization or death, gastrointestinal perforation, and hypersensitivity reactions including anaphylaxis. The most common adverse effects reported in clinical studies were upper respiratory tract infection, nasopharyngitis, headache, hypertension, and increased liver enzyme levels. Elevations in liver enzyme levels were generally mild and reversible and did not result in apparent permanent or clinically evident hepatic injury. Laboratory changes, including increases in total cholesterol values, neutropenia, and thrombocytopenia were also observed.

 

Actemra is approved for once-monthly intravenous administration. The recommended starting dose is 4 mg/kg when used in combination with DMARDs or as a monotherapy in patients who have experienced an inadequate response to one or more TNF antagonists. On the basis of clinical response, the dose of Actemra may be increased to 8 mg/kg.

圣路易斯(MD Consult)——2009年1月11日，罗氏宣布，美国食品药品管理局(FDA)已批准Actemra (托珠单抗)用于治疗经一种或多种肿瘤坏死因子(TNF)拮抗剂治疗不佳的中至重度活动性类风湿性关节炎(RA)成人患者。Actemra是一种抑制白细胞介素-6 (IL-6)受体的单克隆抗体。该药可单用或与甲氨蝶呤或其他改善病情抗风湿药(disease-modifying antirheumatic drugs, DMARD)联用。

包括IL-6在内的几个关键细胞因子共同参与RA的炎症过程。研究发现，在RA患者中，IL-6水平升高。罗氏表示，Actemra是第一个专门抑制IL-6生物活性的药物。

 

5项纳入 4,000多例患者的多国III期研究对Actemra进行了研究。来自这些研究的数据显示，与DMARD单药治疗相比，Actemra单用或与甲氨蝶呤或其他DMARD联用均可显著减少RA症状和体征，不管患者此前曾接受何种治疗。

 

Actemra在所有全球临床研究中的总体安全性一致。Actemra相关严重不良事件包括可导致住院或死亡的严重感染、胃肠穿孔及超敏反应(包括过敏反应)。临床研究中最常见的不良反应是上呼吸道感染、鼻咽炎、头痛、高血压和肝酶水平升高。肝酶水平升幅一般较小，且可逆，不会引起明显永久性或临床可见的肝损伤。另外，还观察到实验室指标改变，包括总胆固醇水平升高、中性粒细胞减少和血小板减少。

 

Actemra获准静脉给药，每月1次。在用于治疗那些经一种或多种TNF拮抗剂反应不佳的患者时，Actemra单药治疗或Actemra/DMARD联合治疗的推荐初始剂量为4 mg/kg。根据临床反应，可将Actemra 剂量增加至 8 mg/kg。