Drug intelligence / Profile preview

puzerinostat

Development stage
Unknown
Lead developer
West China Hospital of Sichuan University
Modality
Small Molecules
Administration
Intravenous
01

Overview

Puzerinostat (also known as preisinastat or purinostat) is a novel, highly selective small molecule inhibitor of Class I (HDAC1, HDAC2, HDAC3, and HDAC8) and Class IIb (HDAC6 and HDAC10) histone deacetylases (HDACs). Developed by West China Hospital of Sichuan University, Guizhou Bailing, and Zenitar, puzerinostat features an innovative non-linear large triangular cap structure that significantly enhances its binding affinity and selectivity compared to early-generation pan-HDAC inhibitors. By selectively targeting Class I and IIb HDACs, it avoids the cardiotoxicity and immunosuppressive side effects associated with Class IIa and IV HDAC inhibition. Puzerinostat induces chromatin remodeling, alters gene expression patterns to downregulate oncogenes (such as c-Myc and BCR-ABL), and promotes anti-tumor immune responses. It is currently in Phase III clinical development for the treatment of relapsed or refractory diffuse large B-cell lymphoma (DLBCL) and is being evaluated in Phase II trials for other hematologic malignancies, including T-cell lymphomas and multiple myeloma, as well as advanced solid tumors.

Other names
PrexostatPrexostat mesylatepreisinastatpreisinastat mesylatepremilastatpremilastat mesilatepremilastat mesylatepurinostatpurinostat mesylatepuzerinostat mesylate
02

Targets

HDAC6 (Histone deacetylase 6)HDAC1 (Histone Deacetylase 1)HDAC8 (Histone Deacetylase 8)

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