Preclinical and Clinical Studies of Chidamide (CS055/HBI-8000), An Orally Available Subtype-selective HDAC Inhibitor for Cancer Therapy

Epigenetic modifications play central roles in cellular differentiation and their deregulations really contribute to tumor development. Histone deacetylase (HDAC) enzymes can exert their functions in the epigenetic regulation of gene expression related to oncogenesis via deacetylating the lysine residues of histones in the chromatin and various non-histone proteins. A majority of HDAC inhibitors (HDACIs) have been in different stages of preclinical and clinical trials with potent anticancer activity recently. Among these agents, chidamide tested as either monotherapeutic agent or in combination regimens for numerous hematological and solid malignancies has shown promising potential as an orally active subtype-selective HDACI. Herein we will highlight the progress of clinical trials of chidamide and rationally analyze those results from both preclinical and clinical studies about chidamide as an epigenetic modulator in cancer therapy.