Drug intelligence / Profile preview

chiglitazar sodium + venetoclax + azacitidine

Development stage
Unknown
Lead developer
Akeso
Modality
Small Molecules
Administration
Oral, Subcutaneous, Intravenous
01

Overview

CVA is an experimental triple combination regimen consisting of chiglitazar sodium, venetoclax, and azacitidine, currently under investigation for the treatment of relapsed or refractory acute myeloid leukemia (R/R AML). Chiglitazar sodium is a novel pan-peroxisome proliferator-activated receptor (PPAR) agonist that targets PPARα, PPARγ, and PPARδ, potentially sensitizing leukemia cells to apoptosis. Venetoclax is a selective small-molecule inhibitor of the anti-apoptotic protein B-cell lymphoma 2 (BCL-2), which is frequently overexpressed in AML cells to evade programmed cell death. Azacitidine is a hypomethylating agent that acts as a DNA methyltransferase inhibitor, promoting the re-expression of tumor suppressor genes and inducing cell differentiation. This combination therapy aims to achieve synergistic anti-leukemic effects by simultaneously targeting epigenetic regulation, apoptotic pathways, and metabolic/differentiation signaling in resistant leukemia cell populations.

02

Targets

BCL-2 (BCL-2 family)PPARG (Peroxisome proliferator-activated receptor gamma)PPARA (Peroxisome proliferator-activated receptor alpha)PPARD (Peroxisome proliferator–activated receptor delta)DNMT1 (DNA (cytosine-5)-methyltransferase 1)

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