APG-5918 + lisaftoclax

APG-5918 + 利生妥 (APG-5918 + lisaftoclax) is an investigational combination therapy being developed by Ascentage Pharma. It consists of APG-5918, a novel, potent, and highly selective orally active small-molecule inhibitor of embryonic ectoderm development (EED), and lisaftoclax (APG-2575; marketed as 利生妥), a selective Bcl-2 inhibitor. APG-5918 binds to the H3K27me3-binding pocket of EED, disrupting the Polycomb Repressive Complex 2 (PRC2) and reducing H3K27 trimethylation (H3K27me3) to reactivate tumor suppressor genes. Lisaftoclax selectively inhibits Bcl-2, restoring the normal apoptotic pathway in cancer cells. The combination of these two agents targets both PRC2-mediated epigenetic dysregulation and Bcl-2-mediated anti-apoptotic signaling, demonstrating synergistic antitumor activity in preclinical models of diffuse large B-cell lymphoma (DLBCL), particularly EZH2-mutant DLBCL.

Other names

APG-5918 + APG-2575APG-5918 + lisaftoclaxAPG-5918 + 利生妥APG-5918 + 利沙托克拉EEDi-5273 + APG-2575EEDi-5273 + lisaftoclax