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azd5153

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Overview

NCI Definition [1]:
An orally bioavailable bivalent inhibitor of bromodomain-containing protein 4 (BRD4), with potential antineoplastic activity. Upon oral administration, the BRD4 inhibitor AZD5153 selectively binds to the acetylated lysine recognition motifs in two bromodomains in the BRD4 protein, thereby preventing the binding of BRD4 to acetylated lysines on histones. This disrupts chromatin remodeling and dysregulates expression of target genes, which leads to the downregulation of the expression of certain growth-promoting genes, induces apoptosis and inhibits the proliferation of BRD4-overexpressing tumor cells. BRD4, a member of the human bromodomain and extra-terminal (BET) family of proteins, is a transcriptional regulator that is overexpressed in certain tumor cells and plays an important role in cellular proliferation.

Clinical Trials

View Clinical Trials for azd5153

Azd5153 has been investigated in 2 clinical trials, of which 1 is open and 1 is closed. Of the trials investigating azd5153, 2 are phase 1 (1 open).

ER Negative, ER No Expression, and HER2 Deficient Expression are the most frequent biomarker inclusion criteria for azd5153 clinical trials.

Aggressive non-hodgkin lymphoma, breast carcinoma, and lymphoma are the most common diseases being investigated in azd5153 clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Azd5153
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Azd5153
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating azd5153 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]:
azd 5153, bet inhibitor azd5153, bivalent bet bromodomain inhibitor azd5153, bivalent brd4 inhibitor azd5153, brd4/bet bromodomain antagonist azd5153, (r)-4-(2-(4-(1-(3-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl)phenoxy)ethyl)-1,3-dimethylpiperazin-2-one
Drug Target(s) [2]:
BRD4
NCIT ID [1]:
C151943

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.