bomedemstat

Bomedemstat is an orally available, irreversible small molecule inhibitor of lysine-specific demethylase 1 (LSD1, also known as KDM1A), developed primarily for the treatment of myeloproliferative neoplasms and certain cancers. By inhibiting LSD1, which regulates gene expression through histone demethylation (notably H3K4 and H3K9), bomedemstat increases methylation at these sites, leading to enhanced expression of tumor suppressor genes and reduced transcription of genes promoting tumor growth. This mechanism results in decreased proliferation and survival of malignant cells. Bomedemstat has received Orphan Drug Designations for essential thrombocythemia (ET), myelofibrosis (MF), and acute myeloid leukemia (AML) in the US and EU. It is currently being evaluated in Phase 3 trials for ET and polycythemia vera (PV), Phase 2 trials for MF, AML, myelodysplastic syndromes (MDS), as well as early-phase studies in small cell lung cancer[1][3][5][6][7].

Other names

bomedemstat tosylateIMG-241 bis-tosylate saltIMG241 bis-tosylate saltIMG 241 bis-tosylate salt