Breast cancer accounts for 29% of malignant
tumors. It is an heterogenous disease covering a spectrum of different molecular subtypes. Epigenetic aberrations may affect gene expression through
DNA and
histone proteins modifications thus promoting
tumor progression and resistance to anti-
tumor treatment. Area covered: This article explores the potential role of
entinostat in the treatment of
breast cancer. The clinical trials evaluating
entinostat are discussed, highlighting preclinical data and early-phase clinical studies results. The emerging activity of
entinostat in several clinical settings is evaluated by focusing on endocrine-resistant, HER2 positive and
triple-negative breast cancer with promising activity in boosting the immune-system. Expert opinion:
Entinostat, a synthetic
benzamide derivative
class I histone deacetylases (HDACs) inhibitor, inhibits cell proliferation and promotes apoptosis in
breast cancer. Several results from clinical trials demonstrate that the addition of an epigenetic
therapy to
antiestrogen therapy may be an effective approach to targeting resistance pathways in
breast cancer, particularly in
hormone-positive disease. Agents such as
entinostat may have a role in immunogenic modulation. Genetic and pharmacological inhibition studies identified HDAC as a key determinant in the reversal of
carcinoma immune escape. This offers the rationale for combining
HDAC inhibitors with
immunotherapy, including therapeutic
cancer vaccines.