Drug Class Detail

Drug Class MDM2 Inhibitor

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Idasanutlin RG7388 MDM2 Inhibitor 18 Idasanutlin (RG7388) binds to MDM2 to block subsequent interaction with p53, which restores p53 activity (PMID: 23808545).
CGM097 NVP-CGM097 MDM2 Inhibitor 18 CGM097 binds to the p53 binding region of MDM2 and prevents MDM2-p53 interaction, resulting in activation of p53 signaling and decreased tumor growth (Cancer Res October 1, 2014 74:4638).
RO6839921 MDM2 Inhibitor 18 RO6839921 binds to MDM2 and inhibits its interaction with p53, preventing degradation of p53, thereby potentially resulting in restoration of wild-type p53 activity and apoptosis of tumor cells (NCI Drug Dictionary).
MK-8242 MDM2 Inhibitor 18 MK-8242 binds MDM2 and prevents its interaction with p53, thereby inhibiting degradation of p53 and potentially resulting in increased tumor cell apoptosis (NCI Drug Dictionary).
AQ-101 MDM2 Inhibitor 18 AQ-101 interferes with the interaction between MDM2 and MDM4 and induces degradation of MDM2, resulting in activation of Tp53, and potentially leading to decreased proliferation and increased apoptosis of tumor cells (PMID: 29282301).
SAR405838 MI-77301|MI-773 MDM2 Inhibitor 18 SAR405838 binds to MDM2 and inhibits MDM2-p53 interaction, resulting in activation of wild-type p53 signaling and decreased tumor growth (PMID: 25145672).
ATSP-7041 MDM2 Inhibitor 18 MDM4 inhibitor 8 ATSP-7041 is a stapled peptide that inhibits MDM2 and MDM4 (MDMX), resulting in activation of p53 and decreased tumor growth (PMID: 23946421).
DS-3032b MDM2 Inhibitor 18 DS-3032b binds to MDM2 and prevents binding to p53, resulting in activation of p53 signaling and increased tumor cell apoptosis (NCI Drug Dictionary).
MI-63 MDM2 Inhibitor 18 MI-63 is a small molecule, high-affinity, non-peptide inhibitor of MDM2 and in cancer cells with wild type Tp53, MI-63 treatment results in reactivation of Tp53 (PMID: 19707204).
APG-115 MDM2 Inhibitor 18 APG-115, a derivative of SAR405838, inhibits MDM2 and its interaction with p53, thereby stabilizing and activating wild-type p53, which may result in antitumor activity (PMID: 28498808).
HDM201 MDM2 Inhibitor 18 HDM201 binds to MDM2 and inhibits its interaction with p53, which prevents p53 degradation and potentially leads to restoration of p53 signaling and increased tumor cell death (NCI Drug Dictionary).
AMG 232 AMG-232 MDM2 Inhibitor 18 AMG 232 is a potent inhibitor of the MDM2-p53 interaction, and inhibits proliferation of tumor cells in a p53 dependent manner (PMID: 24456472).
ALRN-6924 MDM2 Inhibitor 18 MDM4 inhibitor 8 ALRN-6924 binds to MDM2 and MDM4 (MDMX) and prevents their interaction with p53, resulting in restoration of p53 activity and potentially leading to increased tumor cell death (PMID: 29643228).
KRT-232 KRT 232|KRT232 MDM2 Inhibitor 18 KRT-232 binds to MDM2 and inhibits MDM2-p53 interaction, thereby potentially resulting in the restoration of wild-type p53 activity and apoptosis of tumor cells (NCI Drug Dictionary).
MX69 MDM2 Inhibitor 18 MX69 is an inhibitor of the interaction between MDM2 and XIAP, which results in MDM2 degradation and subsequent repression of TP53 activation thereby possibly leading to antitumor activity (PMID: 27666947).
Nutlin-3 Nutlin|Nutlin-3a MDM2 Inhibitor 18 Nutlin-3 is an MDM2 inhibitor which activates p53 and results in cancer cells undergoing apoptosis and cellular senescence. Nutlin-3 is a candidate for neoadjuvant therapy in cancers with a functional p53 (PMID: 18451145).
RG7112 RO5045337 MDM2 Inhibitor 18 RG7112 (RO5045337) binds to the p53-binding region of MDM2 and inhibits MDM2-p53 interaction, resulting in activation of p53 signaling, and decreased tumor cell growth (PMID: 24900694, PMID: 23400593).
RO5503781 MDM2 Inhibitor 18 RO5503781 binds to MDM2 and inhibits its interaction with p53, preventing degradation of p53, thereby resulting in restoration of wild-type p53 activity and potentially promoting apoptosis of tumor cells (NCI Drug Dictionary).
Molecular Profile Protein Effect Treatment Approaches