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birabresib

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Overview

NCI Definition [1]:
A synthetic, small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family of bromodomain-containing proteins 2, 3 and 4 with potential antineoplastic activity. Upon administration, the BET bromodomains 2, 3 and 4 inhibitor MK-8628 binds to the acetylated lysine recognition motifs on the bromodomain of BET proteins, thereby preventing the interaction between the BET proteins and acetylated histone peptides. This disrupts chromatin remodeling and gene expression. Prevention of the expression of certain growth-promoting genes, including c-Myc-dependent target genes, may lead to an inhibition of tumor cell growth. Characterized by a tandem repeat of bromodomain at the N-terminus, the BET proteins BRD2, BRD3, BRD4 are transcriptional regulators that play an important role in cellular growth.

Clinical Trials

View Clinical Trials for birabresib

Birabresib has been investigated in 2 clinical trials, of which 0 are open and 2 are closed. Of the trials investigating birabresib, 2 are phase 1 (0 open).

BCR-ABL1 Fusion, ER Negative, and ER No Expression are the most frequent biomarker inclusion criteria for birabresib clinical trials.

Acute myeloid leukemia, breast carcinoma, and diffuse large B-cell lymphoma are the most common diseases being investigated in birabresib clinical trials [2].

Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Birabresib
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating birabresib 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]:
brd 2/3/4 inhibitor mk-8628, brd 2/3/4 inhibitor otx015, otx015, bet bromodomain proteins 2, 3, and 4 inhibitor mk-8628, mk-8628, 6h-thieno(3,2-f)(1,2,4)triazolo(4,3-a)(1,4)diazepine-6-acetamide, 4-(4-chlorophenyl)-n-(4-hydroxyphenyl)-2,3,9-trimethyl-, (6s)-, bet bromodomains 2/3/4 inhibitor mk-8628, bet bromodomains 2/3/4 inhibitor mk-8628
Drug Target(s) [2]:
BRD2, BRD3, BRD4
NCIT ID [1]:
C103298

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.