DDP-38003 trihydrochloride is a novel, orally available histone lysine-specific demethylase 1A (KDM1A/LSD1) inhibitor with an IC50 of 84 nM.

KDM1A/LSD1:84 nM

DDP-38003 inhibits KDM1A with an IC 50 of 84 nM. DDP-38003 is more active in reducing the colony-forming ability and in inducing the differentiation of THP-1 cells than the 1R, 2S analogue [1].

DDP-38003 exhibits in vivo efficacy after oral administration, determining a 62% increased survival in mouse leukemia models with evidence of KDM1A inhibition. The half life of DDP-38003 is 8 h. A significant dose dependent increase of mice survival is obtained by DDP-38003 treatment. The survival rate increases 35% and 62% at the dose of 11.25 and 22.50 mg/kg, respectively. DDP-38003 has the potential as cancer therapeutic [1].