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pemrametostat

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Overview

NCI Definition [1]:
An orally available, selective small molecule inhibitor of protein arginine methyltransferase 5 (PRMT5), with potential antiproliferative and antineoplastic activities. Although the mechanism of action has not been completely determined, pemrametostat binds to the substrate recognition site of PRMT5 following oral administration and inhibits its methyltransferase activity, which decreases the levels of both monomethylated and dimethylated arginine residues in histones H2A, H3 and H4 and modulates the expression of genes involved in several cellular processes, including cell proliferation. Therefore, this agent may increase the expression of antiproliferative genes and/or decrease the expression of genes that promote cell proliferation and may lead to decreased growth of rapidly proliferating cells, including cancer cells. PRTM5, an arginine methyltransferase that can catalyze the formation of both omega-N monomethylarginine (MMA) and symmetrical dimethylarginine (sDMA) on histones and a variety of other protein substrates, is overexpressed in several neoplasms.

Clinical Trials

View Clinical Trials for pemrametostat

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

CDKN2A Overexpression, ER Expression, and ER Negative are the most frequent biomarker inclusion criteria for pemrametostat clinical trials.

Acute myeloid leukemia, adenoid cystic carcinoma, and anaplastic astrocytoma are the most common diseases being investigated in pemrametostat clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Pemrametostat
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating pemrametostat 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]:
epz015938, gsk-3326595, gsk3326595, prmt5 inhibitor gsk3326595, protein arginine methyltransferase 5 inhibitor gsk3326595, pemrametostat
Drug Target(s) [2]:
PRMT5

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.