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zen-3694

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Overview

NCI Definition [1]:
An orally bioavailable inhibitor of the bromodomain and extra-terminal (BET) family of proteins, with potential antineoplastic activity. Upon oral administration, the BET inhibitor ZEN-3694 binds to the acetylated lysine recognition motifs in the bromodomains of BET proteins, thereby preventing the interaction between the BET proteins and acetylated histones. This disrupts chromatin remodeling and gene expression. Prevention of the expression of certain growth-promoting genes may lead to an inhibition of proliferation in BET-overexpressing tumor cells. BET proteins, comprised of BRD2, BRD3, BRD4 and BRDT, are transcriptional regulators that play an important role during development and cellular growth.

Clinical Trials

View Clinical Trials for zen-3694

Zen-3694 has been investigated in 2 clinical trials, of which 2 are open and 0 are closed. Of the trials investigating zen-3694, 2 are phase 2 (2 open).

BRCA1 Frameshift (germline), BRCA1 Loss (germline), and BRCA1 Nonsense (germline) are the most frequent biomarker inclusion criteria for zen-3694 clinical trials.

Breast carcinoma and prostate adenocarcinoma are the most common diseases being investigated in zen-3694 clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Zen-3694
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating zen-3694 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]:
zen 3694, zen003694, bet bromodomain inhibitor zen-3694, beti zen-3694
Drug Target(s) [2]:
BRD2, BRD3, BRD4, BRDT
NCIT ID [1]:
C126805

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.