Itepekimab  (Synonyms: REGN-3500; SAR-440340)

Itepekimab (REGN-3500) is an IgG4 monoclonal antibody against IL-33. Itepekimab reduced airway inflammation and related tissue damage in preliminary clinical studies. Itepekimab has potential effects in asthma, chronic obstructive pulmonary disease (COPD), and atopic dermatitis (AD)^[1][2][3][4].

Itepekimab 能以高亲和力结合 IL-33，阻止 ST2 D3 结构域与 IL-33 的结合，从而阻止 IL-33/ST2/IL-1RAcP 信号复合物的形成，阻断气道炎症介质产生^[4]。
Itepekimab 还可以与不同的 IL-33 裂解变体以亚纳摩尔亲和力结合，阻止报告细胞系中的 NF-kB 信号传导，并阻止人外周血单核细胞释放细胞因子^[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Itepekimab 可改善小鼠 1 型和 2 型肺部炎症。Itepekimab 可防止肺部重塑特征，阻止 IL-33/ST2/IL-1RAcP 复合物的形成，并在持续性气道炎症小鼠模型中重建纤毛细胞的存在^[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

2226742-52-3

液体

Colorless to light yellow

Shipping with dry ice.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Wechsler ME, et al. Efficacy and Safety of Itepekimab in Patients with Moderate-to-Severe Asthma. N Engl J Med. 2021 Oct 28;385(18):1656-1668.  [Content Brief]

  [2]. Rabe KF, et al. Safety and efficacy of itepekimab in patients with moderate-to-severe COPD: a genetic association study and randomised, double-blind, phase 2a trial. Lancet Respir Med. 2021 Nov;9(11):1288-1298.  [Content Brief]

  [3]. Kosloski MP, et al. Pharmacokinetics and pharmacodynamics of itepekimab in healthy adults and patients with asthma: Phase I first-in-human and first-in-patient trials. Clin Transl Sci. 2022 Feb;15(2):384-395.  [Content Brief]