Blick Stephanie K A, Curran Monique P
Wolters Kluwer Health / Adis, Auckland, New Zealand.
BioDrugs. 2007;21(3):195-201; discussion 202-3. doi: 10.2165/00063030-200721030-00006.
Certolizumab pegol is a pegylated humanized Fab' fragment of an anti-tumor necrosis factor-alpha (TNFalpha) monoclonal antibody, which binds with high affinity to both membrane-bound and soluble TNFalpha and demonstrates high neutralizing potency for these factors. The elimination half-life of certolizumab in humans has been extended to approximate/= 2 weeks through pegylation, allowing subcutaneous administration of this agent once every 4 weeks. Subcutaneous certolizumab pegol 400mg once every 4 weeks (with an additional 400mg dose at week 2) was effective as induction and maintenance therapy in patients with moderate to severe Crohn's disease in whom baseline serum C-reactive protein levels were >/=10 mg/L, according to data from two well designed, randomized phase III trials. Certolizumab pegol was, in general, well tolerated, and adverse events associated with the drug were of a mild to moderate nature; no instances of lupus were reported in any of the trials.
赛妥珠单抗是一种聚乙二醇化的抗肿瘤坏死因子-α（TNFα）单克隆抗体人源化Fab′片段，它与膜结合型和可溶性TNFα均具有高亲和力，并对这些因子表现出高效中和能力。通过聚乙二醇化，赛妥珠单抗在人体内的消除半衰期已延长至约2周，使得该药物可以每4周皮下注射一次。根据两项设计良好的随机III期试验数据，对于中度至重度克罗恩病患者，若其基线血清C反应蛋白水平≥10mg/L，每4周皮下注射一次400mg赛妥珠单抗（第2周额外注射400mg剂量）作为诱导和维持治疗有效。总体而言，赛妥珠单抗耐受性良好，与该药物相关的不良事件为轻至中度；在任何试验中均未报告狼疮病例。
