• Philadelphia, PA (May 18, 2017) – Oncoceutics, Inc. announced that the journal Cell Cycle recently published a manuscript detailing the anti-cancer efficacy of members of the imipridone family. The publication, from the laboratory of Wafik El-Deiry MD, PhD, FACP, Scientific Founder of Oncoceutics, and Deputy Cancer Center Director for Translational Research of the Fox Chase Cancer Center at Fox Chase Cancer Center, describes the synthesis and efficacy of a series of imipridone compounds, derived from the core chemical structure of Oncoceutics’ lead clinical stage molecule ONC201, and concludes that the therapeutic utility of the imipridone class extends beyond ONC201.

    The imipridone family represents a novel class of chemical compounds that possess a unique three-ring heterocycle. The paper describes specific changes to the chemical structure that can cause major changes in potency and spectrum of anti-cancer efficacy, while maintaining the desirable drug-like properties of ONC201. Utilizing the imipridone scaffold, Oncoceutics has generated a portfolio of drug candidates with differentiated spectrums of activity.

    In the paper, the efficacy, safety, and engagement of the integrated stress response and other proven mechanisms of cancer cell death similar to those seen with ONC201, were specifically validated for ONC206 and ONC212. ONC212 was efficacious and well tolerated in multiple animal models of cancer, independent of mutations that confer poor prognosis in cancer patients.

    “It is exciting to see the therapeutic potential of ONC201 expanded through the generation of the imipridone family,” said Dr. El-Deiry. “Based on this data, it appears that this novel class of compounds could represent safe, effective therapeutic options for a broad range of cancers. I look forward to seeing our basic research translated into clinical trials that will bring these new compounds to patients with different cancers that are difficult to treat.”

    In addition to the information described in the Cell Cycle article, the differentiated spectrum of activity of imipridones is accompanied by their ability to target various members of the G-protein coupled receptor (GPCR) superfamily. For example, as recently announced at the annual conference of the American Association of Cancer Research (AACR), ONC212’s anti-leukemic activity appears to be driven by selective engagement of GPR132, a GPCR that is established as a tumor suppressor in scientific literature. Overall, it appears that imipridones can potently and selectively engage a variety of GPCRs, allowing for the generation of a suite of differentiated, targeted therapeutics.

    “We are excited to continue working with the oncology community to explore the therapeutic potential of imipridones,” said Varun Prabhu, PhD, Associate Director, Research and Development, at Oncoceutics. “The ability to selectively target GPCRs and modulate the critical signaling pathways that they control presents a novel way to treat a range of malignancies and improve the lives of patients whose diseases have no effective standards of care.”

    About Oncoceutics

    Oncoceutics, Inc. is a clinical-stage drug discovery and development company with a novel class of compounds that selectively target G protein-coupled receptors for oncology. The first lead compound to result from this program is ONC201, an orally active DRD2 small molecule antagonist that is well-tolerated and effective against advanced cancers. The company has completed a successful Phase I study in solid tumors and has begun additional Phase I/II and Phase II clinical programs in both solid and hematological malignancies. Oncoceutics and collaborative groups have received more than $7 million in grants over the last two years, including grants from the National Cancer Institute, the U.S. Food and Drug Administration, the Pennsylvania Department of Health, and The Musella Foundation. In addition, outside interest in the company’s portfolio has resulted in several R&D alliance agreements between Oncoceutics and leading comprehensive cancer centers, including The University of Texas MD Anderson Cancer Center and the Fox Chase Cancer Center.  The company has established a robust intellectual property position, including several issued patents.

    Contact Rohinton Tarapore for more information.

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