Oncoprex Shows Synergistic Tumor Suppression in Combination with AKT Inhibitor MK2206
April 2, 2012
CHICAGO, IL and AUSTIN, TX, April 2, 2012 – Genprex, Inc.
New data demonstrating the anti-cancer activities of Oncoprex® were presented at the 2012 Annual Meeting of the American Association for Cancer Research (AACR) in Chicago IL. The study, “Synergistic antitumor activity of AKT inhibitor MK2206 and FUS1 nanoparticles in LKB1 mutant NSCLC” (Meng J, Lara-Guerra H, Ji L, Roth JA) is authored by a team of investigators from The University of Texas MD Anderson Cancer Center. The paper is included in the Proceedings of the Annual Meeting of the American Association for Cancer Research, 2012, Abstract 870. The preclinical study demonstrates that when Oncoprex is combined with Merck’s MK2206, the combination of therapies is more effective in suppressing growth in LKB1 mutant tumors than either of the single agents in animal models bearing H322 LKB1-mutant human lung cancer tumors. The treatment with the combination of Oncoprex and MK2206 resulted in tumor volume reduction of greater than 2.5 times the tumor reduction achieved with MK2206 alone.
A phase I clinical trial evaluating intravenous Oncoprex monotherapy, also known as FUS1 nanoparticles, demonstrated antitumor activity in lung cancer patients. Previously published animal studies showed synergistic cancer-killing activity when Oncoprex is combined with a variety of kinase inhibitory agents including erlotinib and gefitinib. A phase I/II clinical trial evaluating Oncoprex combined with Tarceva® (erlotinib) in lung cancer patients without the EGF receptor mutation or patients who have failed Tarceva therapy will initiate in 2012.
David J. Tomasso, chief operating and business officer at Genprex commented, “Many patients cannot benefit from targeted cancer therapies due to the patient’s genomic characteristics. We are developing Oncoprex combination therapies to expand patient populations benefiting from targeted therapies and to unlock the unrealized potential of a variety of targeted kinase inhibitory drugs. This study broadens the potential application of Oncoprex to include combinations with AKT inhibitors such as MK2206.”
LKB1 is a kinase inactivated in 30% of lung cancers. The study evaluated the combined effects of Oncoprex (FUS1 nanoparticles) combined with MK2206 on tumor cell growth and apoptosis induction in NSCLC and explored the molecular mechanism of their mutual action. The studies revealed that Oncoprex therapy sensitized the response of NSCLC cells to MK2206, resulting in a marked increase in growth suppression and apoptosis in LKB1-mutant NSCLC. Mutations in LKB1 result in loss of LKB1 regulation and are often coincident with KRAS activations, allowing cancer cells unchecked growth and metabolic capacity resulting in highly aggressive and metastatic cancer proliferation. Results from the study show that Oncoprex may play a role in modulating the sensitivity of lung cancer cells to AKT inhibition, and suggest that a combination of Oncoprex and MK2206 may be an effective treatment strategy for LKB1 mutant human lung cancers.
Oncoprex is a nanomolecular therapy harnessing the TUSC2 (also known as FUS1) tumor suppressor. TUSC2 defects are associated with most major cancers and >85% of lung cancers. Intravenous Oncoprex induces apoptosis, or programmed cell death, in cancer cells and controls cell signaling and inflammation to fight cancer along universal cancer pathway. In phase I clinical testing in Stage IV lung cancer patients, Oncoprex monotherapy was well tolerated and demonstrated clinically significant anti-cancer activity in primary lung tumors and metastatic tumors, including liver and pancreas. A phase II clinical trial evaluating Oncoprex in combination with Tarceva® (erlotinib) will begin in 2012. The trial will enroll lung cancer patients without the EGFR mutation and patients with EGFR mutations who have become unresponsive to erlotinib.
Genprex, Inc. is a privately held, clinical-stage biopharmaceutical company developing nanomolecular therapies that control universal cancer pathways to unlock the unrealized potential of a variety of targeted cancer therapies. Genprex controls a portfolio of biomedical technologies including targeted molecular therapeutics for cancer and other diseases. The novel technologies, including those licensed exclusively from The University of Texas MD Anderson Cancer Center, are protected by 15 issued patents and 9 pending applications. These broadly applicable technologies have been the subject of more than 30 peer-reviewed scientific publications in the fields of cancer, genomics and molecular biology.