In the present article we target the PELP1-KDM1 axis using a nanoliposomal formulation of PELP1-siRNA-1,2-dioleoyl-sn-glycero-3-phosphatidylcholine (DOPC) administered systemically and KDM1 inhibitors in xenograft-based preclinical breast tumor models. Here, KDM1A is linked to breast neoplasm.