Drug intelligence / Profile preview

e7820

Development stage
Phase 2
Lead developer
Eisai
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

E7820 is a small molecule, aromatic sulfonamide derivative developed as an oral angiogenesis inhibitor with potential antiangiogenic and antitumor activities. Its primary mechanism of action is the inhibition of integrin alpha 2 (ITGA2), a cell adhesion molecule expressed on endothelial cells, leading to suppression of angiogenesis and tumor growth. E7820 acts by downregulating integrin alpha 2 expression at the mRNA level, which disrupts cell-cell and cell-matrix interactions necessary for vascular endothelial proliferation and new blood vessel formation. Additionally, it induces degradation of CAPERα (RBM39), contributing to its transcriptional effects on integrin α2 expression. The drug has been investigated in clinical trials for several malignancies including colorectal cancer, acute myeloid leukemia, chronic myelomonocytic leukemia, myelodysplastic syndromes, and solid tumors[1][4][5][6][7].

Other names
N-(3-cyano-4-methyl-1H-indol-7-yl)-3-cyanobenzene-sulfonamide3-cyano-N-(3-cyano-4-methyl-1H-indol-7-yl)benzenesulfonamide289483-69-8
02

Targets

ITGA2 (Integrin alpha-2)RBM39 (RNA-binding motif protein 39)

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