Ezabenlimab
Ezabenlimab Basic information
- Product Name:
- Ezabenlimab
- Synonyms:
-
- Ezabenlimab
- Research Grade Ezabenlimab (DHH02220)
- Research Grade Ezabenlimab
- Ezabenlimab (anti-PD-1)
- CAS:
- 2249882-54-8
- MW:
- 0
- Mol File:
- Mol File
Ezabenlimab Chemical Properties
- form
- Liquid
- color
- Colorless to light yellow
Ezabenlimab Usage And Synthesis
Description
Ezabenlimab is a monoclonal antibody directed against the negative immunoregulatory human cell surface receptor programmed cell death protein 1 (PD-1; PDCD1), with immune checkpoint inhibitory and antineoplastic activities. Upon administration, ezabenlimab selectively binds to and blocks the activation of PD-1, an immunoglobulin (Ig) superfamily transmembrane protein, by its ligands programmed cell death ligand 1 (PD-L1), which is overexpressed on certain cancer cells, and programmed cell death ligand 2 (PD-L2), which is primarily expressed on antigen-presenting cells (APCs). This results in the activation of T-cells and T-cell-mediated immune responses against tumor cells. Activated PD-1 negatively regulates T-cell activation and plays a key role in in tumor evasion from host immunity.
Uses
Ezabenlimab (BI-754091) is an anti-PD-1 mAb with binding constant Kd value of 6 nM (CHO cells). Ezabenlimab blocks the interaction of PD-1 with PD-L1 and PD-L2. Ezabenlimab increases interferon-γ secretion in T cells, and inhibits tumor growth in vivo[1].
in vivo
Ezabenlimab (0.3-30 mg/kg; i.p.; single dose or twice per week or every 3 weeks) inhibits tumor progress and shows comparable anti-tumor activity in hPD-1 knock-in mouse model[1].
| Animal Model: | hPD-1 knock-in mouse model[1] |
| Dosage: | 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg |
| Administration: | Intraperitoneal injection; single dose or twice per week or every 3 weeks |
| Result: | Showed tumor growth inhibition (TGI) at day 25 dose-dependently of 99%, 101%, 91%, 48%, and 44%, respectively. |
References
[1] Zettl M, et al. Combination of two novel blocking antibodies, anti-PD-1 antibody ezabenlimab (BI 754091) and anti-LAG-3 antibody BI 754111, leads to increased immune cell responses. Oncoimmunology. 2022 Jun 16;11(1):2080328. DOI:10.1080/2162402X.2022.2080328
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