Best-in-class inhibitor of DNA synthesis
RX-3117 is a novel small-molecule chemotherapy agent being developed to treat cancers. It belongs to the class of cytotoxic antimetabolite nucleoside compounds. In vitro and in vivo studies have demonstrated successful preliminary efficacy and therapeutic potential.
- Potent in vitro inhibition of proliferation of many solid tumor types.
- Potent in vitro anti-proliferation effects on gemcitabine drug-resistant cancer cells.
- Significant in vivo anti-tumor activity in mouse xenograft models, including colon, lung, pancreas, renal and others.
RX-3117 interferes with enzymes or metabolites responsible for the process of cell division, nucleic acid synthesis, arrests cells in G1 phase and induces apoptosis. RX-3117 also inhibits cdc2 kinase and DNMT-1 protein expression, which are further involved in cell division processes. RX-3117 is activated by uridine-cytidine kinase and is activated by a mechanism different from that of gemcitabine.
Rexahn is developing RX-3117 to address some of the highest unmet needs in cancer, such as the need for new drugs to treat drug-resistant cancers. Based on our preclinical study findings, RX-3117 has the potential to effectively treat gemcitabine-resistant solid tumors in indications such as pancreatic, NSCLC, colon, renal and other solid tumors.
RX-3117 completed an exploratory clinical trial in patients for oral bioavailability and PK. A phase Ib clinical trial began in January 2014.
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