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].

Human IgG4 kappa

Human IgG4 (S228P) kappa, Isotype Control

Human

IL-33

Itepekimab can bind IL-33 with high affinity and prevent the binding of ST2 D3 domain to IL-33, thus preventing the formation of IL-33/ST2/IL-1RAcP signaling complex and blocking the production of airway inflammatory mediator^[4].
Itepekimab also binds with subnanomolar affinity to different IL-33 cleavage variants, blocks NF-kB signaling in reporter cell lines, and prevents cytokine release from human peripheral blood mononuclear cell^[4].

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

Itepekimab ameliorates type 1 and type 2 lung inflammation and prevents characteristic lung remodeling in mice. Itepekimab prevents IL-33/ST2/IL-1RAcP complex formation and reconstitutes ciliated cells in a mouse model of persistent airway inflammation^[4].

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

90865  [NCBI]

O95760

ELISA, FACS, Functional assay

Unconjugated

The product can be reconstituted/diluted with sterile PBS or saline.

144.64 kDa

2226742-52-3

Liquid

Colorless to light yellow

[Itepekimab]

Shipping with dry ice.

Please refer to the lot-specific COA for specific buffer information.

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

• 
  Human IgG4 kappa

• 
  Immobilized IL-33 Protein, Human (His, HY-P70475) can bind Itepekimab. The EC₅₀ for this effect is 157.7 ng/mL.
• 
  Flow cytometric analysis of 1.5×10⁶ HUVEC cells with Itepekimab (HY-P99673, red). Cells were fixed with 4% paraformaldehyde and permeabilised with 90% methanol. Then stained with the primary antibody at 1/200 dilution for an hour at 4℃. Alexa Goat Anti-Human IgG H&L (AF488) (HY-P83776) was used as the secondary antibody at 1/1,000 dilution for 30 minutes at 4℃. Human IgG4 kappa Isotype Control (HY-P99003, blue) was used as the isotype control, cells without incubation with primary antibody were used as the unlabeled control (black).

• [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]

  [4]. Asrat S, et al. Itepekimab Binds to IL-33 With High Affinity, Prevents the Formation of IL-33/ST2/IL-1RAcP Signaling Complex and Blocks Mediators of Airway Inflammation[M]//C13. CYTOKINES: CYTOKINES IN THE AIRWAYS. American Thoracic Society, 2023: A4478-A4478.