azacitidine + entinostat

Azacitidine + entinostat is a combination of two small molecule epigenetic modulators used in investigational cancer therapy. Azacitidine is a DNA methyltransferase inhibitor (DNMTi) that incorporates into DNA and RNA, leading to hypomethylation of DNA and cytotoxicity through disruption of nucleic acid metabolism. Entinostat is a synthetic benzamide derivative that selectively inhibits class I and IV histone deacetylases (HDACs), resulting in increased acetylation of histones, reactivation of silenced genes, inhibition of cell proliferation, induction of differentiation, and apoptosis. The combination aims to synergistically reactivate tumor suppressor genes by targeting both DNA methylation and histone deacetylation pathways. This regimen has been studied in phase I/II clinical trials for advanced breast cancer (including hormone-resistant or triple-negative subtypes), metastatic colorectal cancer, myelodysplastic syndromes (MDS), acute myeloid leukemia (AML), and non-small cell lung cancer (NSCLC)[1][2][4][5][6].

Brand names

Vidaza

Other names

5-azacitidine + entinostat5AC + entinostatAZA + entinostat