Overview

NCI Definition [1]:
An orally available inhibitor of DNA-dependent protein kinase (DNA-PK), with potential antineoplastic and chemo/radiosensitizing activities. Upon oral administration, the DNA-PK inhibitor MSC2490484A binds to and inhibits the activity of DNA-PK. This inhibits the ability of tumor cells to repair damaged DNA, which may lead to a reduction in cellular proliferation of cancer cells expressing DNA-PK. DNA-PK, a serine/threonine kinase and a member of the PI3K-related kinase subfamily of protein kinases, is activated upon DNA damage and plays a key role in repairing DNA double-strand breaks (DSBs) via the DNA nonhomologous end joining (NHEJ) pathway. The enhanced ability of tumor cells to repair DSBs plays a major role in the resistance of tumor cells to chemo- and radiotherapy.

Nedisertib has been investigated in 11 clinical trials, of which 11 are open and 0 are closed. Of the trials investigating nedisertib, 7 are phase 1 (7 open) and 4 are phase 1/phase 2 (4 open).

MGMT Promoter Methylation Negative, PML-RARA Fusion, and SSTR1 Expression are the most frequent biomarker inclusion criteria for nedisertib clinical trials.

Malignant solid tumor, acute myeloid leukemia, and cholangiocarcinoma are the most common diseases being investigated in nedisertib clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Nedisertib
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating nedisertib 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]:
peposertib, m3814, msc2490484a, dna-dependent protein kinase inhibitor m3814, m 3814, m-3814, dna-pk inhibitor msc2490484a
Drug Target(s) [2]:
PRKDC
NCIT ID [1]:
C120036

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.