Certolizumab pegol (Certolizumab) is a recombinant, polyethylene glycolylated, antigen-binding fragment of a humanized monoclonal antibody that selectively targets and neutralizes tumour necrosis factor-α (TNF-α). Certolizumab pegol can be used for rheumatoid arthritis and Crohn disease research[1-2].
Certolizumab pegol neutralizes soluble TNF-α with an IC90 of 3ng/mL. Preincubation of human monocytes with certolizumab pegol at concentrations of 1μg/mL and above completely inhibited lipopolysaccharide(LPS)-induced IL-1β production, and certolizumab pegol did not induce apoptosis of activated human monocytes or peripheral blood lymphocytes (PBLs), nor did it cause changes in the integrity of polymorphonuclear granules (PMNs)[2]. In addition, certolizumab pegol can directly induce non-apoptotic cell death in transmembrane TNF-α-expressing cells[4].
Certolizumab pegol (10μg, single dose) reduced the severity of acute pancreatitis, and serum amylase, lipase, and lactate dehydrogenase levels were significantly reduced in the certolizumab pegol-treated group[3]. Compared with the control group (non-inflamed tissue), certolizumab pegol (2mg/kg) can effectively penetrate into the inflamed arthritic paws of mice and improve arthritis in mice[5].
References:
[1] Deeks ED. Certolizumab pegol: a review of its use in the management of rheumatoid arthritis. Drugs. 2013 Jan;73(1):75-97.
[2] Nesbitt A, et al. Mechanism of action of certolizumab pegol (CDP870): in vitro comparison with other anti-tumor necrosis factor alpha agents. Inflamm Bowel Dis. 2007 Nov;13(11):1323-32.
[3] Kosekli M A, Sungurtekin U, Cobankara V, et al. Effects of certolizumab on cerulein-induced acute pancreatitis in rats[J]. Pancreas, 2016, 45(8): 1120-1125.
[4] Ueda N, Tsukamoto H, Mitoma H, et al. The cytotoxic effects of certolizumab pegol and golimumab mediated by transmembrane tumor necrosis factor α[J]. Inflammatory bowel diseases, 2013, 19(6): 1224-1231.
[5] Palframan R, Airey M, Moore A, et al. Use of biofluorescence imaging to compare the distribution of certolizumab pegol, adalimumab, and infliximab in the inflamed paws of mice with collagen-induced arthritis[J]. Journal of immunological methods, 2009, 348(1-2): 36-41.
Certolizumab pegol（Certolizumab）是一种重组、聚乙烯糖基化、抗原结合片段的人源化单克隆抗体，选择性靶向和中和肿瘤坏死因子-α（TNF-α）。Certolizumab pegol可用于类风湿关节炎和克罗恩病研究[1-2]。
Certolizumab pegol可中和可溶性TNF-α，IC90为3ng/mL。人单核细胞与浓度为1μg/mL及以上浓度的Certolizumab pegol预孵育完全抑制了脂多糖（LPS）诱导的IL-1β的产生，并且Certolizumab pegol不会诱导活化的人单核细胞或外周血淋巴细胞（PBL）凋亡，也不会导致多形核颗粒（PMN）完整性发生变化[2]。此外，Certolizumab pegol可以直接诱导跨膜TNF-α表达细胞中的非凋亡细胞死亡[4]。
Certolizumab pegol（10μg，单剂量）可降低急性胰腺炎的严重程度，并且Certolizumab pegol治疗组血清淀粉酶、脂肪酶和乳酸脱氢酶水平显著降低[3]。与对照组相比（非炎症组织），Certolizumab pegol（2mg/kg）能有效地渗透小鼠发炎的关节炎爪子，改善小鼠关节炎[5]。