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molibresib

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Overview

NCI Definition [1]:
A small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family of bromodomain-containing proteins with potential antineoplastic activity. Upon administration, the BET inhibitor GSK525762 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 may lead to an inhibition of tumor cell growth. Characterized by a tandem repeat of bromodomain at the N-terminus, BET proteins, comprising 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 molibresib

Molibresib has been investigated in 5 clinical trials, of which 2 are open and 3 are closed. Of the trials investigating molibresib, 3 are phase 1 (2 open), 1 is phase 1/phase 2 (0 open), and 1 is phase 2 (0 open).

NUTM1 Expression, NUTM1 Fusion, and BCL2 Fusion are the most frequent biomarker inclusion criteria for molibresib clinical trials.

Acute myeloid leukemia, breast carcinoma, and hematopoietic and lymphoid malignancy are the most common diseases being investigated in molibresib clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Molibresib
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Molibresib
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating molibresib 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]:
i-bet compound, bet inhibitor gsk525762, i-bet762, gsk 525762a, ibet compound, gsk525762a, gsk525762, gsk-525762a, molibresib besylate
Drug Target(s) [2]:
BRD2, BRD3, BRD4, BRDT
NCIT ID [1]:
C101538

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.