mocetinostat

Mocetinostat is a rationally designed, orally available, small molecule inhibitor that selectively targets class I histone deacetylases (HDACs), specifically HDAC1, HDAC2, and HDAC3. As a 2-aminobenzamide derivative, it acts as an epigenetic modulator by inhibiting these enzymes, leading to increased acetylation of histones and reactivation of tumor suppressor genes. This results in antineoplastic effects through mechanisms such as induction of apoptosis, cell cycle arrest, differentiation, inhibition of DNA repair pathways, upregulation of tumor suppressors, downregulation of growth factors, oxidative stress induction, and autophagy. Mocetinostat has been investigated primarily for the treatment of various cancers including bladder cancer (urothelial carcinoma), diffuse large B cell lymphoma (DLBCL), follicular lymphoma (FL), myelodysplastic syndromes (MDS), non-small cell lung cancer (NSCLC), Hodgkin's disease/lymphoma (HL), acute myeloid leukemia (AML; development discontinued for this indication) and rhabdomyosarcoma[1][4][5][7][8][10]. It has also been studied in combination with other agents such as immune checkpoint inhibitors like durvalumab[10].

Other names

mocetinostat dihydrobromide