Rexahn’s clinical development portfolio consists of three clinical stage oncology compounds with unique and selective mechanisms of action.
Archexin®, a potential best-in-class compound with FDA orphan designation for the treatment of refractory cancers in various organs including the pancreas and ovaries. In contrast to conventional chemotherapy, Archexin® specifically blocks the production of Akt1, a molecule that plays a central role in the uncontrolled growth of tumor mass. Therefore, Archexin® may be able to replace the current standard cancer therapy with improved efficacy and tolerability. Archexin has completed a Phase I clinical trial in patients with solid tumors and was shown to be safe and well tolerated with predicted pharmacokinetics. In a Phase IIa trial in patients with advanced pancreatic cancer, Archexin in combination with gemcitabine was shown to be safe and well tolerated and demonstrated a preliminary signal of efficacy with a median survival of 9.1 months, compared to the historical survival data of 5.65 months (Burris et al., 1997, J. Clin Oncol 15:2403) for standard single agent gemcitabine therapy. Rexahn is evaluating options for advancing Archexin, including initiating Phase IIa clinical trials for chemo-resistant solid tumors and hematological malignancies in the second half of 2013.
RX-3117 is being developed in collaboration with Teva Pharmaceutical Industries (NYSE:TEVA). It is a proprietary small molecule compound that inhibits inhibits DNA and RNA synthesis and induces apoptotic cell death through activation by a UCK enzyme. Preclinical studies have shown it be effective in solid tumors in the pancreas, lung, colon, renal and others. In August 2012, Rexahn and Teva concluded a first-in-human exploratory clinical study of RX-3117. In the clinical study RX-3117 met its primary objective of determining the drug’s oral bioavailability in humans. The study supports RX-3117’s position as a potential future alternative to market leading anti-metabolite therapies in the treatment of solid tumors in the colon, lung, bladder and pancreas. As a result of this clinical study, Teva increased its ownership in Rexahn to 6.3%. According to the Research and Exclusive License Option Agreement and the Securities Purchase Agreement between Rexahn and Teva, the total money received to date from Teva is $9.1 million. Rexahn expects to receive additional milestone payments from Teva in the second half of 2013 with the submission of an IND and patient enrollment in a phase I clinical trial.
RX-5902, is an orally administered highly potent anti-cancer, first-in-class small molecule that inhibits the phosphorylated p68 RNA helicase, a protein that plays a key role in cancer growth, progression and metastasis. Pre-clinical studies demonstrated that RX-5902 exhibits very potent anti-tumor activity in various cancers including melanoma, renal, ovarian and pancreatic. Additional studies suggest that RX-5902 is effective in drug-resistant cancer cells and is synergistic when combined with current cancer drugs. The IND for RX-5902 has been filed and a Phase I trial is planned to start in the second quarter of 2013.