| Description |
Iscalimab (CFZ-533) is a non-depleting IGg1 monoclonal antibody targeting CD40 (KD: 0.3 nM). Iscalimab can be used for research of Graves' hyperthyroidism and autoimmune diseases[1][2][3].
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| Related Catalog |
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| Target |
CD40:0.3 nM (IC50)
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| In Vitro |
Iscalimab (0.01-1 μg/mL，过夜) 抑制 rCD154 诱导的原代单核细胞衍生树突状细胞 (moDC) 产生 TNF，IC50 为 0.04 μg/mL[3]。 Iscalimab (3 天) 抑制 rCD154 诱导的人、恒河猴和食蟹猴 PBMC 增殖，IC50 分别为 0.02、0.03 和 0.01 μg/mL[3]。 Iscalimab 结合来自人、恒河猴和食蟹猴的 B 细胞上的 CD40，EC50 值约为 0.2 μg/mL[3]。 Iscalimab (2 μg/mL, 3 h) 以 CD40 依赖性方式被 B 细胞内化[3]。 Cell Viability Assay[3] Cell Line: PBMCs from humans, rhesus and cynomolgus animals Concentration: 0-1 μg/mL approximately Incubation Time: 3 days Result: Inhibited rCD154-induced proliferation of PBMCs with IC50s of 0.02, 0.03, and 0.01 μg/mL, respectively.
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| In Vivo |
Iscalimab (150 mg/kg/周，皮下注射，持续 13 周) 耐受性良好，不会对恒河猴造成任何剂量限制性毒性[3]。 Iscalimab (10 mg/kg，静脉注射) 完全抑制恒河猴的 T 细胞依赖性抗体反应[3]。 Iscalimab (30 mg/kg，静脉内) 可延长肾移植食蟹猴的同种异体移植物存活期[4]。 Animal Model: Kidney transplant cynomolgus[4] Dosage: 30 mg/kg Administration: i.v. Result: Prolonged allograft survival. Well-tolerated with no evidence of thromboembolic events or CD40 pathway activation.
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| References |
[1]. Kahaly GJ, et al. A Novel Anti-CD40 Monoclonal Antibody, Iscalimab, for Control of Graves Hyperthyroidism-A Proof-of-Concept Trial. J Clin Endocrinol Metab. 2020 Mar 1;105(3):dgz013. [2]. Flandre TD, et al. Immunosuppression Profile of CFZ533 (Iscalimab), a Non-Depleting Anti-CD40 Antibody, and the Presence of Opportunistic Infections in a Rhesus Monkey Toxicology Study. Toxicol Pathol. 2022 Jul;50(5):712-724. [3]. Ristov J, et al. Characterization of the in vitro and in vivo properties of CFZ533, a blocking and non-depleting anti-CD40 monoclonal antibody. Am J Transplant. 2018 Dec;18(12):2895-2904. [4]. Cordoba F, et al. A novel, blocking, Fc-silent anti-CD40 monoclonal antibody prolongs nonhuman primate renal allograft survival in the absence of B cell depletion. Am J Transplant. 2015 Nov;15(11):2825-36.
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