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gfh009

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Associated Genetic Biomarkers

Overview

NCI Definition [1]:
A selective inhibitor of the serine/threonine cyclin-dependent kinase 9 (CDK9), the catalytic subunit of the RNA polymerase II (RNA Pol II) elongation factor positive transcription elongation factor b (PTEF-b; PTEFb), with potential antineoplastic activity. Upon administration, the CDK9 inhibitor GFH009 targets, binds to and blocks the phosphorylation and kinase activity of CDK9, thereby preventing PTEFb-mediated activation of RNA Pol II, leading to the inhibition of gene transcription of various anti-apoptotic proteins. This induces cell cycle arrest and apoptosis and prevents tumor cell proliferation. CDK9 regulates elongation of transcription through phosphorylation of RNA Pol II at serine 2 (p-Ser2-RNAPII). It is upregulated in various tumor cell types and plays a key role in the regulation of Pol II-mediated transcription of anti-apoptotic proteins. Tumor cells are dependent on anti-apoptotic proteins for their survival.

Clinical Trials

View Clinical Trials for gfh009

Gfh009 has been investigated in 1 clinical trial, of which 1 is open and 0 are closed. Of the trial investigating gfh009, 1 is phase 1 (1 open).

Acute myeloid leukemia, chronic lymphocytic leukemia, and lymphoma are the most common diseases being investigated in gfh009 clinical trials [2].

Drug Details

Synonyms [2]:
gfh 009, gfh-009, cdk9 inhibitor gfh009
Drug Categories [2]:
CDK inhibitors
Drug Target(s) [2]:
CDK9
NCIT ID [1]:
C176965

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.