Idasanutlin is an orally available, small-molecule antagonist of MDM2 (mouse double minute 2), with potential antineoplastic activity. It binds to MDM2, preventing its interaction with the transcriptional activation domain of the tumor suppressor protein p53. This blocks MDM2-mediated enzymatic degradation of p53, restoring its transcriptional activity and potentially inducing tumor cell apoptosis. MDM2, a zinc finger nuclear phosphoprotein and negative regulator of the p53 pathway, is frequently overexpressed in cancer cells and is involved in their proliferation and survival.
