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BioDrugs. 2015 Apr;29(2):133-42. doi: 10.1007/s40259-015-0123-8.
Subcutaneous canakinumab (Ilaris(®)) is a human monoclonal anti-human interleukin (IL)-1β antibody of the immunoglobulin G1/κ isotype that binds with high affinity and specificity to human IL-1β, blocking its interaction with IL-1 receptors. It is approved in the EU as monotherapy or in combination with methotrexate for the treatment of patients aged ≥2 years with active systemic juvenile idiopathic arthritis (SJIA) who have responded inadequately to previous therapy with non-steroidal anti-inflammatory drugs and systemic corticosteroids. In the USA, it is indicated for the treatment of patients aged ≥2 years with active SJIA. In two placebo-controlled, multinational, phase III studies in patients aged 2-19 years with SJIA, canakinumab rapidly reduced disease activity, permitted the tapering of glucocorticoid therapy and delayed the time to disease flare. The efficacy of canakinumab was sustained at a median follow-up of 49 weeks in an ongoing extension study. In clinical studies, canakinumab had an acceptable tolerability profile that was comparable with that observed in patients with cryopyrin-associated periodic syndromes. In general, adverse events were mild or moderate in intensity, with nasopharyngitis, cough, pyrexia, vomiting, diarrhoea and upper respiratory tract infection the most frequently reported treatment-emergent adverse events. Thus, current evidence suggests subcutaneous canakinumab extends the treatment options currently available for patients aged ≥2 years with SJIA.
皮下注射用卡那单抗(依洛尤单抗)是一种人源化单克隆抗人白细胞介素(IL)-1β抗体,属于 IgG1/κ 同种型,与人 IL-1β 具有高亲和力和特异性,可阻断其与 IL-1 受体的相互作用。该药在欧盟被批准用于治疗对非甾体抗炎药和全身皮质类固醇治疗反应不足的 2 岁及以上患有全身型幼年特发性关节炎(SJIA)的患者,作为单药治疗或与甲氨蝶呤联合治疗。在美国,该药被批准用于治疗 2 岁及以上患有 SJIA 的患者。在两项针对 2-19 岁 SJIA 患者的安慰剂对照、多中心、III 期研究中,卡那单抗迅速降低了疾病活动度,允许逐渐减少糖皮质激素治疗,并延迟了疾病复发的时间。在一项正在进行的扩展研究中,中位随访 49 周时,卡那单抗的疗效得以维持。在临床研究中,卡那单抗具有可接受的耐受性,与在伴冷球蛋白血症性血管炎综合征患者中观察到的情况相当。一般来说,不良事件的强度为轻度或中度,最常报告的治疗后不良事件为鼻咽炎、咳嗽、发热、呕吐、腹泻和上呼吸道感染。因此,目前的证据表明,皮下注射用卡那单抗为 2 岁及以上 SJIA 患者提供了更多的治疗选择。