Dupilumab

Dupilumab (REGN-668) belongs to antibody inhibitors and is an IL-4Rα-targeted inhibitor that exerts anti-inflammatory effects by blocking IL-4 and IL-13 signaling. This compound possesses high selectivity and is mainly used for the treatment of moderate-to-severe atopic dermatitis.

IL-4Rα (dimeric):12 pM (KD), IL-4Rα (monomeric):33 pM (KD)

Methods: In a skin lesion model, Dupilumab was used for treatment, and mRNA expression of genes related to T cells, dendritic cells, eosinophils, inflammatory pathways, and Th2-induced chemokines was detected by gene expression analysis, with IL-17A and IL-22 levels also assessed.
Results: Dupilumab inhibited mRNA expression of the above genes, showed no activity against IL-17A, but significantly reduced IL-22 levels [1].
Methods: Using 300 mg Dupilumab treatment, expression of IL-17-related genes (such as elafin/PI3, IL23p19/IL23A, S100A8, CXCL1, S100A7) and hyperproliferation-related genes (such as K16, S100A) was detected by microarray and qRT-PCR Methods.
Results: 300 mg Dupilumab significantly reduced expression of IL-17-related genes and hyperproliferation-related genes [1].

Methods: An FVB/N mouse subcutaneous MycCaP prostate cancer model was used. Dupilumab (0.2 mg/mouse) combined with anti-IL-4 antibody (0.5 mg/mouse) was administered by intraperitoneal injection twice weekly for 24 days, with InVivoPure diluent as the vehicle.
Results: CD206 expression in tumor-associated macrophages was significantly reduced in the treatment group, but total macrophage infiltration and tumor growth showed no significant changes.[2]

Human

Monoclonal

Unconjugated