Overview

NCI Definition [1]:
An orally available morpholino-pyrimidine-based inhibitor of ataxia telangiectasia and rad3 related (ATR) kinase, with potential antineoplastic activity. Upon oral administration, ATR kinase inhibitor AZD6738 selectively inhibits ATR activity by blocking the downstream phosphorylation of the serine/threonine protein kinase CHK1. This prevents ATR-mediated signaling, and results in the inhibition of DNA damage checkpoint activation, disruption of DNA damage repair, and the induction of tumor cell apoptosis. In addition, AZD6738 sensitizes tumor cells to chemo- and radiotherapy. ATR, a serine/threonine protein kinase upregulated in a variety of cancer cell types, plays a key role in DNA repair, cell cycle progression and survival; it is activated by DNA damage caused during DNA replication-associated stress.

Ceralasertib has been investigated in 22 clinical trials, of which 18 are open and 4 are closed. Of the trials investigating ceralasertib, 5 are phase 1 (3 open), 1 is phase 1/phase 2 (1 open), and 16 are phase 2 (14 open).

ATM Loss, ATM Mutation, and BRCA1 Loss are the most frequent biomarker inclusion criteria for ceralasertib clinical trials.

Malignant solid tumor, breast carcinoma, and fallopian tube carcinoma are the most common diseases being investigated in ceralasertib clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Ceralasertib
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Ceralasertib
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating ceralasertib 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]:
azd6738, atr kinase inhibitor azd6738, azd-6738
Drug Categories [2]:
Serine/threonine kinase inhibitors
Drug Target(s) [2]:
ATR
NCIT ID [1]:
C111993

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.