Overview

Generic Name(s):
idasanutlin
NCI Definition [1]:
An orally available, small molecule, antagonist of MDM2 (mouse double minute 2; Mdm2 p53 binding protein homolog), with potential antineoplastic activity. Idasanutlin binds to MDM2 blocking the interaction between the MDM2 protein and the transcriptional activation domain of the tumor suppressor protein p53. By preventing the MDM2-p53 interaction, p53 is not enzymatically degraded and the transcriptional activity of p53 is restored. This may lead to p53-mediated induction of tumor cell apoptosis. MDM2, a zinc finger nuclear phosphoprotein and negative regulator of the p53 pathway, is often overexpressed in cancer cells and has been implicated in cancer cell proliferation and survival.

Idasanutlin has been investigated in 10 clinical trials, of which 5 are open and 5 are closed. Of the trials investigating idasanutlin, 1 is phase 1 (0 open), 7 are phase 1/phase 2 (4 open), 1 is phase 2 (1 open), and 1 is phase 3 (0 open).

Deficient DNA Mismatch Repair (dMMR), ER Positive, and HER2 Deficient Expression are the most frequent biomarker inclusion criteria for idasanutlin clinical trials.

Breast carcinoma, colorectal adenocarcinoma, and lymphoma are the most common diseases being investigated in idasanutlin clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Idasanutlin
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Idasanutlin
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating idasanutlin and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,956 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:
ro 5503781, idasanutlin, rg-7388, mdm2 antagonist ro5503781, ro-5503781, ro5503781, rg7388, idasanutlin
Drug Categories [2]:
MDM2 inhibitors
Drug Target(s) [2]:
MDM2
NCIT ID [1]:
C99131

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.