tefinostat

Tefinostat is a hydroxamic acid-derived small molecule histone deacetylase (HDAC) inhibitor with selective activity toward monocyte and macrophage lineage cells. It is designed to be cleaved into its active acid form by the intracellular esterase human carboxylesterase-1 (hCE-1), which is predominantly expressed in monocytoid cells and some hepatocytes. This selective activation allows for targeted accumulation of the drug in these cell types. Tefinostat inhibits HDACs, leading to increased acetylation of histones, chromatin remodeling, inhibition of oncogene transcription, suppression of tumor cell division, and induction of apoptosis in malignant cells. The drug has shown preclinical efficacy particularly in myelomonocytic leukemias (such as AML M4/M5 subtypes and chronic myelomonocytic leukemia), with minimal toxicity to normal bone marrow progenitors at therapeutic doses. It has also demonstrated potential for modulating peroxisomal β-oxidation pathways relevant to neuroinflammatory diseases such as multiple sclerosis[2][3][4][5][8].

Other names

tefinostattefinostat tartrate914382-60-8ZAU91150SBZAU-91150SBZAU 91150SB