Reslizumab is a humanized IgG4/κ monoclonal antibody that targets IL-5 molecules, with the Kd value of 81pM[1]. Reslizumab binds to the α chain of the IL-5 receptor on the surface of eosinophils, thereby inhibiting the proliferation of eosinophils, Reslizumab can be metabolized through enzymatic protein hydrolysis into small peptides and amino acids[2]. Reslizumab has been widely used in animal models of asthma to control asthma symptoms and improve lung function[3].
In vitro, Reslizumab significantly inhibited the proliferation of TF-1 cells stimulated by IL-5 after 48 hours of treatment, with an IC50 value of 0.091nM[4].
In vivo, seven days after intraperitoneal injection of a single dose of 200mg/kg Reslizumab, the number of eosinophils in the blood and the level of serum IL-5 in the ovalbumin (OVA)-treated mice were significantly reduced, without affecting the production of IL-13[5]. In OVA-sensitized guinea pig model, Reslizumab (1mg/kg) administered intraperitoneally 2 hours before the OVA challenge reduced eosinophilia, airway hyperreactivity, and bronchoconstriction[6].
References:
[1] Padilla Galo A, Labor M, Tiotiu A, et al. Impact of reslizumab on outcomes of severe asthmatic patients: current perspectives[J]. Patient Related Outcome Measures, 2018: 267-273.
[2] Hom S, Pisano M. Reslizumab (Cinqair): an interleukin-5 antagonist for severe asthma of the eosinophilic phenotype[J]. Pharmacy and Therapeutics, 2017, 42(9): 564.
[3] Xu Y, Yang L, Zhao T, et al. Multifunctional Gold Nanoclusters for a Lung Tissue Distribution Study of a Novel Anti-asthma Inhaled Antibody[J]. Analytical Chemistry, 2025, 97(36): 19635-19653.
[4] Liddament M, Husten J, Estephan T, et al. Higher binding affinity and in vitro potency of reslizumab for interleukin-5 compared with mepolizumab[J]. Allergy, Asthma & Immunology Research, 2018, 11(2): 291-298.
[5] Kageyama K, Kikuchi E, Hoshino N. Effect of anti-interleukin-5 antibody on development of vasculitis in an ovalbumin-induced eosinophilic vasculitis mouse model[J]. Frontiers in Pharmacology, 2025, 16: 1546785.
[6] Egan R W, Athwal D, Bodmer M W, et al. Effect of Sch 55700, a humanized monoclonal antibody to human interleukin-5, on eosinophilic responses and bronchial hyperreactivity[J]. Arzneimittelforschung, 1999, 49(09): 779-790.
Reslizumab是一种靶向IL-5分子的人源化IgG4/κ单克隆抗体，Kd值为81pM[1]。Reslizumab与嗜酸性粒细胞表面的IL-5受体α链结合，从而抑制嗜酸性粒细胞的增殖，并且Reslizumab可通过酶促蛋白水解代谢为小肽和氨基酸[2]。Reslizumab已广泛用于哮喘动物模型，以控制哮喘症状并改善肺功能[3]。
在体外，Reslizumab处理48小时后能显著抑制IL-5刺激的TF-1细胞增殖，IC50值为0.091nM[4]。
在体内，单次腹腔注射200mg/kg剂量的Reslizumab 7天后，卵清蛋白（OVA）处理小鼠血液中的嗜酸性粒细胞数量及血清IL-5水平显著降低，且不影响IL-13的产生[5]。在OVA致敏的豚鼠模型中，于OVA处理前2小时腹腔注射Reslizumab（1mg/kg），可减轻嗜酸性粒细胞增多、气道高反应性及支气管收缩[6]。