TAS1440

TAS1440 is an orally available small molecule inhibitor of lysine-specific demethylase 1 (LSD1, also known as KDM1A), a histone demethylase enzyme involved in the regulation of gene expression and hematopoiesis. It acts as a reversible, histone-competitive inhibitor by binding to the histone H3 binding site of LSD1. Overexpression of LSD1 has been implicated in myeloproliferative neoplasms and acute myeloid leukemia (AML). TAS1440 is being developed for use as a monotherapy or in combination with all-trans retinoic acid (ATRA) for relapsed or refractory AML and potentially other hematologic malignancies. The drug was originally discovered by Taiho Pharmaceutical and has been out-licensed to Benz Sciences for further development[3][4][5][7].