NCI Drug Dictionary

The NCI Drug Dictionary contains technical definitions and synonyms for drugs/agents used to treat patients with cancer or conditions related to cancer. Each drug entry includes links to check for clinical trials listed in NCI's List of Cancer Clinical Trials.

HDM2 inhibitor MK-8242
An orally bioavailable inhibitor of human homolog of double minute 2 (HDM2), with potential antineoplastic activity. Upon oral administration, HDM2 inhibitor MK-8242 inhibits the binding of the HDM2 protein to the transcriptional activation domain of the tumor suppressor protein p53. By preventing this HDM2-p53 interaction, the degradation of p53 is inhibited, which may result in the restoration of p53 signaling. This induces p53-mediated tumor cell apoptosis. HDM2 is a member of the RING finger-type family of E3 ubiquitin protein ligases and targets p53 for degradation; it is often overexpressed in cancer cells and has been implicated in cancer cell proliferation and survival. Check for active clinical trials using this agent. (NCI Thesaurus)

Code name:MK-8242
SCH 900242