Philadelphia, PA (September 15, 2016) – Oncoceutics, Inc. announced the publication of a review article in the journal Oncotarget entitled “Discovery and clinical introduction of first-in-class imipridone ONC201.” The article summarizes the history of how the molecule was discovered, its mechanism of action, and its preclinical profile, as well as its move into the clinic for specific types of advanced cancers. Oncoceutics is currently conducting Phase II trials to evaluate the efficacy on ONC201 in Non-Hodgkin’s Lymphomas, acute myeloid leukemias, multiple myeloma, glioblastoma and other solid tumors.
The review describes how ONC201 selectively kills cancer cells by affecting a number of signaling pathways that are critical for cancer cell survival, such as Ras signaling, the integrated stress response, and the extrinsic cell death pathway. This article also references the recently reported discovery of the interaction between ONC201 and Dopamine Receptor D2 (DRD2), a G protein-coupled receptor (GPCR) that controls these downstream signaling pathways and its anti-cancer effects.
In addition, the publication describes how Oncoceutics has extended the therapeutic potential of the molecule’s unique three-ring heterocyclic structure into a new class of compounds, called imipridones, that selectively target GPCRs. GPCRs are a superfamily of receptors that are commonly targeted by therapeutics, but have historically been underexploited in oncology. Nonetheless, there is increasing evidence that GPCRs play key roles in oncology, including that GPCRs are frequently activated by cancer cells to promote pro-survival signaling.
“The phenotypic discovery of ONC201 and years of molecular investigation has led to the understanding of a novel therapeutic target for oncology that controls many known anti-tumor pathways, making this drug an intriguing new option for patients with advanced cancers,” said Joseph Bertino, MD, Chief Scientific Officer of Rutgers Cancer Institute of New Jersey and member of the Oncoceutics Scientific Advisory Board. “ONC201 and the rest of the imipridone class are the start of a new therapeutic paradigm that involves selectively targeting GPCRs for oncology.”
“We have always been intrigued by the ability of ONC201 to broadly impact important signaling pathways, independent of several common resistance mechanisms in cancer and with an exceptional safety profile,” said Keith Flaherty, MD, Director of Developmental Therapeutics, Massachusetts General Hospital Cancer Center. “Now that ONC201’s mechanism has been elucidated, its attractive efficacy and safety can be explained by how the drug interacts with DRD2 and the downstream signaling. There is a growing body of evidence from many independent investigators that supports the importance of this target in oncology, particularly in cancers such as glioblastoma where ONC201 is being evaluated.”
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 recently 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.
