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Publication Reports Role of Dopamine Receptors in Cancer and ONC201 Response

Al's Comment:

 The article they mention is at

but it is not free. It shows that the DRD2 is overexpressed in many types of cancer.  Onc-201 blocks that receptor, but they also found that high levels of DRD5 make the cells resistant to the Onc-201.  So for this drug to work, we need high DRD2 and low DRD5.  That happens in most brainstem gliomas, and high grade gliomas that are in the midline of the brain - especially those in the thalamus, and in younger patients.   There are about 14 clinical trials going on for Onc201 in various cancers, including brain.  For those who do not qualify for the clinical trials, there is a compassionate use program available – contact us (the Musella Foundation)  for details 888-295-4740



Posted on: 01/11/2019

Publication Reports Role of Dopamine Receptors in Cancer and ONC201 Response
Philadelphia, PA (January 11, 2019) – Oncoceutics, Inc. announced the publication of a research article in the scientific journal Clinical Cancer Research that describes the dysregulation of specific dopamine receptors by human cancers. The article also defines therapeutic opportunities associated with selective targeting of these receptors in tumors by ONC201 and other imipridones, Oncoceutics’ novel class of small molecule cancer therapies.
The research findings show that DRD2 is the specific member of the dopamine receptor family that is most often dysregulated in human cancers, implicating it as a therapeutic target for selective antagonism. Overexpression of this receptor was seen across a wide range of human cancers, with the strongest expression detected in neurooncology and neuroendocrine tumors. Further studies showed that selective antagonism of DRD2, while avoiding other receptors, is critical to maximizing anticancer efficacy, a key feature of ONC201.
This report also finds that another dopamine receptor, DRD5, negatively influences the sensitivity of tumor cells to ONC201. Combining the expression of these two dopamine receptors provides a biomarker tool to identify additional types of cancer that respond to ONC201 beyond its current lead indication in H3 K27M-mutant glioma, which appears to be one of many mechanisms that can produce this biomarker signature.
“Decades of research have shown that G protein-coupled receptors (GPCRs) such as dopamine receptors, are hijacked by tumors to support their growth and survival,” said J. Silvio Gutkind, PhD, Associate Director of Basic Science at University of California, San Diego. “It is rewarding to finally see the clinical translation of one of these therapeutic concepts with ONC201. This compound is clearing the path for other GPCR-targeting agents, including additional imipridones in development, to address a previously untargeted axis in cancer.”
“We are excited and compelled by the clinical results that we are seeing with ONC201 in patients with specific types of high grade gliomas,” said Joshua Allen, PhD, senior author of the article and Senior Vice President of Research and Development, Oncoceutics. “Our findings in this research article provide a molecular compass that points to additional indications, within and beyond gliomas, that we can study in the lab and the clinic to help more cancer patients with this novel therapy.”
About Oncoceutics
Oncoceutics, Inc. is a clinical-stage drug discovery and development company with a novel class of compounds, i.e. the “imipridones,” that selectively target G protein-coupled receptors for oncology. The first lead compound to emerge from this program is ONC201, an orally active small molecule DRD2 antagonist. The company is supported by grants from NCI, FDA, Musella Foundation, XCures, Cancer Commons, and a series of private and public partnerships.
Visit Oncoceutics or contact for more information.


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