On July 31, 2018 Oncoceutics, Inc. reported the publication of a scientific research article in the journal Clinical Cancer Research that demonstrates utility for the company’s imipridone portfolio of compounds in neuro-oncology (Press release, Oncoceutics, JUL 31, 2018, View Source [SID1234558367]). Oncoceutics developed this portfolio of chemical compounds that target G protein-coupled receptors (GPCRs) using the unique core chemical structure of the company’s lead compound ONC201.
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The article identifies several opportunities to use imipridones against gliomas, including identifying effects on an important gene called c-myc on which many cancers depend and which has been deemed "undruggable." The published results also validate the anti-cancer effects, in patient-derived glioma models, of targeting the dopamine receptor DRD2. This is the GPCR antagonized by both ONC201 and ONC206, the second generation DRD2 antagonist with differentiated receptor pharmacology and drug-like characteristics compared to ONC201. In addition, the article provides clinical rationale for the introduction of ONC206 into the clinic in 2019 to treat gliomas and further connects DRD2 antagonism to the previously described downstream signaling effects.
"It is exciting to see the utility of additional imipridones beyond ONC201 for the treatment of lethal cancers with no curative treatments, such as glioblastoma," said Markus Siegelin, M.D, Assistant Professor of Pathology & Cell Biology at Columbia University who served as a senior corresponding author of the publication. "Our study provides unique insights into the mechanism of DRD2 antagonism resulting in the identification of biomarkers for the imipridone clinical program."
"The imipridone family of compounds contains several new therapeutic concepts for oncology that build out from our understanding of ONC201," said Joshua Allen, Ph.D., Senior Vice President of R&D at Oncoceutics. "These exciting new findings set the stage for the upcoming clinical introduction of ONC206 as the next imipridone to make clinical impact."