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.

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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