milademetan free base

Milademetan (DS-3032b or DS-3032) is a potent and selective MDM2 inhibitor with potential antineoplastic activity. Milademetan (p.o.) binds to and prevents the binding of MDM2 protein to the transcriptional activation domain of the tumor suppressor protei

Milademetan is a potent and selective MDM2 inhibitor. MDM2 inhibitor DS-3032b binds to and prevents the binding of MDM2 protein to the transcriptional activation domain of the tumor suppressor protein p53 upon oral administration. By preventing this MDM2-p53 interaction, the proteosome-mediated enzymatic degradation of p53 is inhibited and the transcriptional activity of p53 is restored. This results in the restoration of p53 signaling and leads to the p53-mediated induction of tumor cell apoptosis.