INCB059872 (INCB-059872, INCB 59872) is a potent, selective, and orally active lysine-specific demethylase 1 (LSD1) inhibitor.
INCB059872 inhibits the proliferation of a panel of SCLC cell lines with EC50 values ranging from 47 to 377 nM.
Oral administration of INCB059872 on once daily (QD) and alternative day (QoD) dosing regimens inhibited tumor growth in the NCI-H526 and NCI-H1417 human SCLC xenograft models.
INCB059872 treatment in these models led to the induction of the FEZ1 and UMODL1 genes relative to vehicle-treated animals, as part of a gene signature in SCLC cell lines that is predictive of LSD1 responsiveness.
