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 kidneys, pancreas and ovaries. In contrast to conventional chemotherapy, Archexin® specifically blocks the production of Akt-1, 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 paired with with gemcitabine was shown to be safe and well tolerated. The combination of the two drugs 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 plans to initiate a Phase IIa clinical trial in the fourth quarter of 2013.
RX-3117 is a proprietary small molecule compound that inhibits DNA and RNA synthesis and induces apoptotic cell death through activation by a UCK enzyme. Preclinical studies have shown it be effective in pancreatic, lung, colon, and renal tumors among others.
In August 2012, a first-in-human exploratory clinical study of RX-3117 was completed. 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. The IND for RX-3117 has been filed, and a Phase I clinical trial will be initiated in the fourth quarter 2013.
Supinoxin (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 Supinoxin exhibits very potent anti-tumor activity in various cancers including renal, ovarian, pancreatic, and melanoma. Additional studies suggest that Supinoxin is effective in drug-resistant cancer cells and is synergistic when combined with current cancer drugs. A Phase I trial is currently enrolling patients, and data is expected in the first half of 2014.