Drug intelligence / Profile preview

lisaftoclax + decitabine + homoharringtonine

Development stage
Phase 2
Lead developer
Ascentage Pharma
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

This combination therapy, often referred to as the LDH regimen, consists of lisaftoclax (APG-2575), decitabine, and homoharringtonine. Lisaftoclax is a selective, orally active small-molecule inhibitor of the anti-apoptotic protein B-cell lymphoma 2 (BCL-2), which triggers apoptosis in cancer cells by displacing pro-apoptotic proteins. Decitabine is a hypomethylating agent that functions as a DNA methyltransferase inhibitor, promoting the re-expression of tumor suppressor genes. Homoharringtonine is a plant-derived alkaloid that inhibits protein synthesis by interfering with the ribosomal translation process. This triplet combination is currently being evaluated in a Phase 2 clinical trial led by the Second Affiliated Hospital, School of Medicine, Zhejiang University, specifically for patients with acute myeloid leukemia (AML) who have failed or are intolerant to prior treatment with venetoclax and azacitidine.

Other names
LDH regimenLisafotoclaxLisaftoclax
02

Targets

BCL-2 (BCL-2 family)DNMT1 (DNA (cytosine-5)-methyltransferase 1)80S ribosome (Ribosome and ribosomal components)Ribosome

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