entinostat

Entinostat is a synthetic benzamide derivative and a selective oral small molecule inhibitor of class I and IV histone deacetylases (HDACs). By inhibiting HDAC1 and HDAC3 in particular, entinostat promotes histone hyperacetylation and transcriptional activation of specific genes. This leads to inhibition of cell proliferation, induction of terminal differentiation and apoptosis in cancer cells. Entinostat also modulates the tumor immune microenvironment by enhancing antigen presentation on cancer cells and increasing cytotoxic T cell activity. It has demonstrated synergistic anti-tumor effects when combined with immune checkpoint inhibitors in preclinical models. The drug is being developed primarily for hormone-resistant (HER2-negative) breast cancer but has been studied across multiple solid tumors including non-small cell lung cancer (NSCLC), renal cell carcinoma, lymphoma, melanoma, pancreatic cancer and others. Entinostat does not currently have regulatory approval but has received FDA breakthrough designation for advanced breast cancer in combination with exemestane[1][3][4][5][6].

Brand names

景助达

Other names

entinostat