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cx5461

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Overview

NCI Definition [1]:
An orally bioavailable inhibitor of RNA polymerase I (Pol I), with potential antineoplastic activity. Upon oral administration, CX-5461 selectively binds to and inhibits Pol I, prevents Pol I-mediated ribosomal RNA (rRNA) synthesis, induces apoptosis, and inhibits tumor cell growth. Pol I, the multiprotein complex that synthesizes rRNA, is upregulated in cancer cells and plays a key role in cell proliferation and survival. Hyperactivated rRNA transcription is associated with uncontrolled cancer cell proliferation.

Clinical Trials

View Clinical Trials for cx5461

Cx5461 has been investigated in 1 clinical trial, of which 1 is open and 0 are closed. Of the trial investigating cx5461, 1 is phase 1 (1 open).

ATM Loss (germline), ATM Mutation (germline), and ATR Loss (germline) are the most frequent biomarker inclusion criteria for cx5461 clinical trials.

Breast carcinoma and malignant solid tumor are the most common diseases being investigated in cx5461 clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Cx5461
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating cx5461 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]:
cx-5461, rna pol i inhibitor cx5461, cx 5461, rna pol i inhibitor cx5461, 1138549-36-6, 2-(4-methyl-1,4-diazepan-1-yl)-n-((5-methylpyrazin-2-yl)methyl)-5-oxo-5h-benzo[4,5]thiazolo[3,2-a][1,8]naphthyridine-6-carboxamide, pol i inhibitor cx5461, 5h-benzothiazolo[3,2-a][1,8]naphthyridine-6-carboxamide, 2-(hexahydro-4-methyl-1h-1,4-diazepin-1-yl)-n-[(5-methyl-2-pyrazinyl)methyl]-5-oxo-, 5h-benzothiazolo[3,2-a][1,8]naphthyridine-6-carboxamide, 2-(hexahydro-4-methyl-1h-1,4-diazepin-1-yl)-n-[(5-methyl-2-pyrazinyl)methyl]-5-oxo-, 2-(4-methyl-1,4-diazepan-1-yl)-n-[(5-methylpyrazin-2-yl)methyl]-5-oxo-[1,3]benzothiazolo[3,2-a][1,8]naphthyridine-6-carboxamide, pol i inhibitor cx5461, 2-(4-methyl-1,4-diazepan-1-yl)-n-[(5-methylpyrazin-2-yl)methyl]-5-oxo-[1,3]benzothiazolo[3,2-a][1,8]naphthyridine-6-carboxamide, 2-(4-methyl-1,4-diazepan-1-yl)-n-((5-methylpyrazin-2-yl)methyl)-5-oxo-5h-benzo[4,5]thiazolo[3,2-a][1,8]naphthyridine-6-carboxamide
Drug Target(s) [2]:
POLR2A, POLR2B
NCIT ID [1]:
C126798

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.