AUSTIN, TX, May 20, 2014 – Genprex, Inc. announced today that it has enrolled the first patient in a clinical trial evaluating its lead product candidate Oncoprex® in combination with erlotinib (Tarceva®) for late-stage lung cancer patients. Oncoprex is a targeted biologic incorporating the pan-kinase inhibitor TUSC2, which inhibits oncogenic kinases via multiple pathways.
The trial is significant in that it seeks to determine if patients without the EGFR activating mutation as well as patients with the EGFR activating mutation whose cancer has progressed after erlotinib treatment can benefit from the Oncoprex + erlotinib combination therapy. While erlotinib is a blockbuster drug helping many cancer patients worldwide, research shows that the vast majority of patients who have lung cancers without the activating EGFR mutation are unlikely to benefit from erlotinib. Additionally, many patients with the activating EGFR mutation who respond to erlotinib therapy eventually become resistant to the therapy.
The Phase II clinical trial evaluates Oncoprex + erlotinib in late-stage lung cancer patients without an activating EGFR mutation who have received prior chemotherapy or in patients with the activating EGFR mutation whose cancer has progressed after treatment with erlotinib. An initial safety and dose-finding portion of the trial tests four escalating doses of the Oncoprex + erlotinib combination. Approximately 40 patients enrolled in the highest dose cohort will be evaluable for efficacy. The trial is being conducted at The University of Texas MD Anderson Cancer Center.
Research conducted previously at MD Anderson Cancer Center shows significant cancer-killing synergy when Oncoprex is combined with erlotinib and a variety of other kinase inhibitors (TKIs) including EGFR, AKT, PDGFR, and Src targeted agents. Notably, these data show Oncoprex works synergistically with EGFR TKIs, including erlotinib, in multiple cancers without the activating EGFR mutation. Data also demonstrated that when Oncoprex is combined with EGFR TKI therapy in EGFR mutated and TKI resistant cancers, the Oncoprex combination overcomes intrinsic and acquired therapeutic resistance by simultaneously inactivating the EGFR and the AKT signaling pathways in the cancers that have become resistant to EGFR TKI to restore apoptotic pathways. Importantly, synergistic anticancer results were also obtained from studies combining Oncoprex with EGFR TKIs in K-ras mutant cancers, which are generally unresponsive to EGFR TKIs.
A previously reported phase I safety study in 32 late-stage lung cancer patients demonstrated that intravenous Oncoprex was well tolerated as a single agent. The study showed that non-immunogenic Oncoprex nanovesicles safely travel through the patients’ bodies to selectively and preferentially target cancer cells with therapeutic doses of TUSC2 in both primary and metastatic tumors. Tumor responses were seen in both primary and metastatic tumors.
Intravenous Oncoprex, also known as TUSC2 (also known as FUS-1) nanoparticles, is a novel biologic therapy harnessing the TUSC2 pan-kinase inhibitor that induces apoptosis, programmed cancer cell death, and controls cell signaling and inflammatory pathways to treat cancer at the molecular level without harming normal cells. Oncoprex regulates the activation of multiple oncogenic kinases and has shown synergistic anti-cancer activity when combined with a number of kinase inhibitor drugs. TUSC2 plays a vital role in cancer suppression and normal cell regulation. Normal TUSC2 function is inactivated at the early onset of cancer development making it a potential target for all stages of cancer including metastatic disease. TUSC2 protein is reduced or absent in over 80% of lung cancers.
Genprex Inc. is a biopharmaceutical company founded to bridge critical gaps in the cancer therapeutics sector by developing products to unlock the potential of proven but limited cancer drugs. The Company is working to expand clinical populations benefitting from targeted, small molecule therapies by using its biologic agents to combine small molecule drugs to promote genome-wide applications of the combination therapy and to participate in expanding proven markets. The Company’s biologics are designed to program cells to overcome intrinsic and acquired small molecule drug resistance without additional toxicities and to sensitize cancer cells to small and large molecule cancer drugs. Genprex, based in Austin, Texas, works with world-class institutions and collaborators to in-license and develop drug candidates and controls 16 issued and 9 pending patents, including its Oncoprex technologies. Its discovery and R&D programs have been the subject of more than 30 peer-reviewed publications and have been supported by $50 million from investigator grant awards and corporate funding.