• At the upcoming Cambridge Healthtech Institute’s 12th Annual GPCR-Based Drug Discovery conference, September 26th and 27th in Boston, Oncoceutics will be presenting data on the company’s lead imipridone ONC201, and other members of the imipridone class.

    On September 26th at 11:55am, Dr. Varun Prabhu will present “Imipridones: A New Class of Anti-Cancer Small Molecules that Selectively Engage GPCRs.”

    GPCRs are the most commonly exploited target in modern medicine; however, efforts in oncology have been limited. This talk will describe imipridone small molecules with a unique tri-heterocyclic core structure that selectively target GPCRs. Lead candidates were profiled using the DiscoverX GPCR platform and characterized for mechanism of action and anti-cancer efficacy.

    At 2:55pm Dr. Joshua Allen will present “Phenotypic Discovery of ONC201 as the First Selective DRD2 Antagonist for Clinical Oncology.”

    Imipridones are a new class of anti-cancer small molecules that share a unique tri-heterocyclic core structure and selectively engage GPCRs. Experimental GPCR profiling revealed imipridone ONC212 selectively targets orphan GPCR GPR132/G2A at nanomolar concentrations. GPR132 is a stress-inducible orphan GPCR with highest expression in leukemia and shown to be a tumor suppressor in the context of lymphoid leukemogenesis. ONC212 was non-toxic to normal cells at therapeutic concentrations and demonstrated robust in vivo safety/efficacy in leukemia xenografts.

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