capecitabine + entinostat

Capecitabine + entinostat is an investigational combination therapy composed of two small molecule drugs: capecitabine, an oral prodrug of 5-fluorouracil (5-FU) and a widely used antimetabolite chemotherapeutic agent, and entinostat, a selective class I histone deacetylase (HDAC) inhibitor. Capecitabine interferes with DNA synthesis by inhibiting thymidylate synthase after conversion to 5-FU in tumor cells, leading to cytotoxicity. Entinostat modulates gene expression through inhibition of HDACs, resulting in epigenetic reprogramming that can sensitize cancer cells to chemotherapy and potentially overcome resistance mechanisms. The combination has been studied for synergistic anti-tumor activity in preclinical models and was evaluated in a phase I clinical trial for patients with heavily pretreated HER2-negative metastatic breast cancer[1][2][3]. The primary aim was to assess safety and tolerability; the most common toxicities were neutropenia, thrombocytopenia, and palmar-plantar dysesthesia[2]. No new safety signals were observed.

Other names

capecitabine + entinostat