Philadelphia, PA (November 15, 2016) – Oncoceutics, Inc. announced four abstracts describing the efficacy of its lead compound ONC201 and lead analog ONC212 were selected for the 2016 annual meeting of the American Society of Hematology (ASH). The abstracts, detailing results from experiments designed and executed by the company as well as collaborators at the University of Texas MD Anderson Cancer Center and Fox Chase Cancer Center, describe the effectiveness of the two drug candidates, both members of the imipridone class of compounds, on a variety of hematological malignancies.
Imipridones are a novel class of small-molecule chemical compounds possessing a unique three-ring heterocycle that exhibit significant anti-cancer activities. ONC201, the founding member of this novel chemical class, has demonstrated attractive drug-like chemical and physical characteristics: excellent chemical stability, high aqueous solubility at low pH, high lipophilicity at physiological pH, and a low molecular weight. These attributes enable oral bioavailability that achieves therapeutic concentrations and wide distribution throughout the body to target tissues that include brain, bone marrow, lymph nodes, and muscle.
The three abstracts related to ONC201 describe: preliminary results from the ongoing trial in acute leukemias at MD Anderson, the demonstration of synergy between ONC201 and cytarabine in preclinical models, and the downstream anti-cancer effects of dopamine receptor 2 (DRD2) antagonism in multiple myeloma. ONC201 is currently being evaluated as a single agent in six ongoing clinical trials – including acute leukemias, non-Hodgkin’s lymphomas and multiple myeloma – and the company is evaluating combinations with approved agents in future trials.
The fourth abstract highlights the activity of ONC212 in synergy with the approved Bcl-2 inhibitor ABT-199 (venetoclax). ONC212, which activates the same downstream pathways as ONC201 and shows significant anti-cancer effects against leukemia and lymphoma at nanomolar concentrations, synergizes with, and causes significant pro-apoptotic effects in cancer cell lines resistant to ABT-199 alone.
Details of the abstracts and their presentation time and location at the ASH meeting (San Diego Convention Center) are provided below. In addition, the abstracts are now available online in a special issue of the journal Blood:
• A Phase I/II Clinical Trial of the First-in-Class GPCR Antagonist ONC201 in Relapsed/Refractory Acute Leukemias: Abstract 3997 Session 613, Acute Myeloid Leukemia Clinical Studies: Poster III Monday, December 5, 2016 6:00-8:00 PM, Hall GH
• ONC201 Overcomes Chemotherapy Resistance by Upregulation of Bim in Multiple Myeloma: Abstract 4476 Session 652, Myeloma: Pathophysiology and Pre-Clinical Studies, excluding therapy: Poster III, Monday, December 5, 2016 6:00-8:00 PM, Hall GH
• Single Agent and Combinatorial Efficacy of First-in-Class Small Molecule ONC201 in Acute Leukemia and Multiple Myeloma: Abstract 2759 Session 604 Molecular Pharmacology and Drug Resistance in Myeloid Diseases: Poster II, Sunday, December 4, 2016 6:00-8:00 PM, Hall GH
• ONC212 Is a Potent Member of the Imipridone Class of Anti-Cancer Compounds that Induces p53-Independent Apoptosis in Hematological Malignancies: Abstract 4059 Session 616 Acute Myeloid Leukemia: Novel Therapy, excluding Transplantation: Poster III, Monday, December 5, 2016 6:00-8:00 PM, Hall GH
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.
Imipridones are a novel class of small-molecule chemical compounds possessing a unique three-ring heterocycle that exhibit significant anti-cancer activities. ONC201, the founding member of this novel chemical class, has demonstrated attractive drug-like chemical and physical characteristics: excellent chemical stability, high aqueous solubility at low pH, high lipophilicity at physiological pH, and a low molecular weight. These attributes enable oral bioavailability that achieves therapeutic concentrations and wide distribution throughout the body to target tissues that include brain, bone marrow, lymph nodes, and muscle.
The three abstracts related to ONC201 describe: preliminary results from the ongoing trial in acute leukemias at MD Anderson, the demonstration of synergy between ONC201 and cytarabine in preclinical models, and the downstream anti-cancer effects of dopamine receptor 2 (DRD2) antagonism in multiple myeloma. ONC201 is currently being evaluated as a single agent in six ongoing clinical trials – including acute leukemias, non-Hodgkin’s lymphomas and multiple myeloma – and the company is evaluating combinations with approved agents in future trials.
The fourth abstract highlights the activity of ONC212 in synergy with the approved Bcl-2 inhibitor ABT-199 (venetoclax). ONC212, which activates the same downstream pathways as ONC201 and shows significant anti-cancer effects against leukemia and lymphoma at nanomolar concentrations, synergizes with, and causes significant pro-apoptotic effects in cancer cell lines resistant to ABT-199 alone.
Details of the abstracts and their presentation time and location at the ASH meeting (San Diego Convention Center) are provided below. In addition, the abstracts are now available online in a special issue of the journal Blood:
• A Phase I/II Clinical Trial of the First-in-Class GPCR Antagonist ONC201 in Relapsed/Refractory Acute Leukemias: Abstract 3997 Session 613, Acute Myeloid Leukemia Clinical Studies: Poster III Monday, December 5, 2016 6:00-8:00 PM, Hall GH
• ONC201 Overcomes Chemotherapy Resistance by Upregulation of Bim in Multiple Myeloma: Abstract 4476 Session 652, Myeloma: Pathophysiology and Pre-Clinical Studies, excluding therapy: Poster III, Monday, December 5, 2016 6:00-8:00 PM, Hall GH
• Single Agent and Combinatorial Efficacy of First-in-Class Small Molecule ONC201 in Acute Leukemia and Multiple Myeloma: Abstract 2759 Session 604 Molecular Pharmacology and Drug Resistance in Myeloid Diseases: Poster II, Sunday, December 4, 2016 6:00-8:00 PM, Hall GH
• ONC212 Is a Potent Member of the Imipridone Class of Anti-Cancer Compounds that Induces p53-Independent Apoptosis in Hematological Malignancies: Abstract 4059 Session 616 Acute Myeloid Leukemia: Novel Therapy, excluding Transplantation: Poster III, Monday, December 5, 2016 6:00-8:00 PM, Hall GH
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.
