Abstract: The aberrant alterations of various epigenetic phenomena, including DNA methylation, histone modification and noncoding RNAs (ncRNAs), are closely related to gliomagenesis and malignant progression, suggesting the fundamental driving roles of epigenomic reprogramming for the occurrence and development of glioma.Since epigenetic modifications are reversible, genes and proteins involved in epigenetic modification have become novel targets in the treatment of glioma.Therefore, small molecule inhibitors targeting epigenetic regulatory factors have a wide application prospect in the treatment of glioma.In this review, we summarize the research progress of small molecule inhibitors targeting epigenetic regulators in the treatment of glioma, in order to provide reference for related research.