incb059872

INCB059872 is an orally available, selective, and irreversible small molecule inhibitor of lysine-specific demethylase 1 (LSD1; also known as KDM1A), developed by Incyte. LSD1 is a flavin adenine dinucleotide (FAD)-dependent amine oxidase that regulates gene expression through histone demethylation. By inhibiting LSD1, INCB059872 increases methylation of histone H3 at lysine 4 (H3K4), leading to enhanced expression of tumor suppressor genes and reduced transcription of tumor-promoting genes via increased H3K9 methylation. This mechanism results in potential antineoplastic activity by inhibiting the growth and survival of LSD1-overexpressing tumor cells. The drug has been investigated for various indications including acute myeloid leukemia (AML), myelodysplastic syndromes (MDS), small cell lung cancer (SCLC), Ewing sarcoma, poorly differentiated neuroendocrine tumors, sickle cell disease, prostate cancer, and other advanced malignancies[1][2][5][6][7].

Other names

1802909-49-412XU6D9FLM