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onametostat

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Overview

NCI Definition [1]:
An orally available small molecule inhibitor of protein arginine methyltransferase 5 (PRMT5), with potential antiproliferative and antineoplastic activities. Upon oral administration, PRMT5 inhibitor JNJ-64619178 selectively targets and irreversibly binds to the S-adenosylmethionine (SAM)- and substrate-binding pockets of the PRMT5/methylosome protein 50 (MEP50) complex, and inhibits its function. By inhibiting its methyltransferase activity, levels of both monomethylated and dimethylated arginine residues in histones H2A, H3 and H4 are decreased. This modulates the expression of genes involved in several cellular processes, including cellular proliferation. This may increase the expression of antiproliferative genes and/or decrease the expression of genes that promote cell proliferation, which may lead to decreased growth of rapidly proliferating cells, including cancer cells. PRMT5, a type II methyltransferase that catalyzes the formation of both omega-N monomethylarginine (MMA) and symmetric dimethylarginine (sDMA) on histones and a variety of other protein substrates involved in signal transduction and cellular transcription, is overexpressed in several neoplasms. Elevated levels are associated with decreased patient survival.

Clinical Trials

View Clinical Trials for onametostat

Onametostat has been investigated in 1 clinical trial, of which 1 is open and 0 are closed. Of the trial investigating onametostat, 1 is phase 1 (1 open).

Complex karyotype, Loss of Y, and Monosomy 7 are the most frequent biomarker inclusion criteria for onametostat clinical trials.

Diffuse large B-cell lymphoma, malignant solid tumor, and myelodysplastic syndromes are the most common diseases being investigated in onametostat clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Onametostat
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating onametostat and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,931 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:
jnj 64619178, protein arginine methyltransferase 5 inhibitor jnj-64619178, prmt5 inhibitor jnj-64619178, jnj64619178, jnj-64619178
Drug Target(s) [2]:
PRMT5
NCIT ID [1]:
C163980

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.