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fhd-286

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Overview

NCI Definition [1]:
An orally bioavailable, allosteric, small molecule inhibitor of transcription activator BRG1 (SWI/SNF-related matrix-associated actin-dependent regulator of chromatin subfamily A member 4; SMARCA4) and BRM (SWI/SNF-related matrix-associated actin-dependent regulator of chromatin subfamily A member 2; SMARCA2), with potential antineoplastic activity. Upon oral administration, BRG1/BRM inhibitor FHD-286 targets, binds to, and inhibits the activity of BRG1 and/or BRM, the primary ATPase components and mutually exclusive subunits of the BRG1/BRM-associated factor (BAF) complexes. This may lead to the inhibition of the SWI/SNF chromatin remodeling complex, disrupt chromatin remodeling and gene expression, and result in the downregulation of oncogenic pathways and the inhibition of tumor cell proliferation. BAF is an important regulator of transcriptional programs and gene expression. Mutations in BAF or its transcription factor partners are found in certain diseases including cancers.

Clinical Trials

View Clinical Trials for fhd-286

Fhd-286 has been investigated in 2 clinical trials, of which 2 are open and 0 are closed. Of the trials investigating fhd-286, 2 are phase 1 (2 open).

Acute myeloid leukemia, myelodysplastic syndromes, and uveal melanoma are the most common diseases being investigated in fhd-286 clinical trials [2].

Drug Details

Synonyms [2]:
fdh286, brg1/brm inhibitor fhd-286, smarca4/smarca2 atpase inhibitor fhd-286, fdh 286
Drug Target(s) [2]:
SMARCA2, SMARCA4
NCIT ID [1]:
C179408

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.