Drug intelligence / Profile preview

APG-5918 + APG-2575

Development stage: Preclinical
Lead developer: Ascentage Pharma
Modality: Small Molecules
Administration: Oral

Overview

APG-5918 + APG-2575 is an investigational combination therapy consisting of APG-5918 (an embryonic ectoderm development [EED] inhibitor) and APG-2575 (lisaftoclax, a Bcl-2 inhibitor). APG-5918 is an oral small-molecule epigenetic modulator that binds to the H3K27me3-recognition domain of EED, disrupting the Polycomb Repressive Complex 2 (PRC2) and inhibiting H3K27 methylation. Lisaftoclax is an oral small-molecule BH3-mimetic that selectively inhibits Bcl-2, restoring apoptosis in cancer cells. Developed by Ascentage Pharma, this combination is being investigated for the treatment of hematologic malignancies, particularly diffuse large B-cell lymphoma (DLBCL), including EZH2-mutant subtypes, where dual targeting of EED and Bcl-2 has demonstrated synergistic antitumor activity in preclinical models.

Other names: APG-5918 + lisaftoclaxEEDi-5273 + APG-2575EEDi-5273 + lisaftoclax

Targets

BCL-2 (BCL-2 family)EED (Embryonic ectoderm development protein)

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