Rexahn Pharmaceuticals, Inc. (REXN)

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Rexahn Pharmaceuticals Publishes New Preclinical Data for Quinoxalinyl-Piperazine Compounds
Business WirePress Release: Rexahn Pharmaceuticals, Inc. – Wed, Jan 25, 2012 8:00 AM EST


ROCKVILLE, Md.--(BUSINESS WIRE)-- Rexahn Pharmaceuticals, Inc. (NYSE Amex: RNN), a clinical stage pharmaceutical company developing and commercializing best in class oncology and CNS therapeutics, today announced the publication of preclinical results for RX-5902 in Bioorganic & Medicinal Chemistry [20:1303-1309, 2012] titled, “Synthesis, anticancer activity and pharmacokinetic analysis of 1-[(substituted 2-alkoxyquinoxalin-3-yl)aminocarbonyl]-4-(hetero)arylpiperazine derivatives.”

In the study, various new quinoxalinyl-piperazine derivatives were shown to have excellent anti-proliferative activity against different human cancer cells, and some selected compounds showed excellent pharmacokinetic properties in rats. In particular, RX-5902 exhibited desirable pharmacokinetic properties – such as in oral bioavailability, half-life, and plasma concentration - supporting its continued development as an orally deliverable potent anti-cancer drug.

“In this second published study of RX-5902, we further establish that it is a potent anti-cancer compound with the optimal pharmacokinetic properties for oral administration,” said Rick Soni, President of Rexahn. “For RX-5902, as a first-in-class RNA helicase inhibitor, we plan to file an Investigational New Drug application in the second quarter of this year.”

In November 2010, Rexahn published additional pre-clinical data in Bioorganic & Medicinal Chemistry [18:7966-7974, 2010], demonstrating that RX-5902, significantly inhibited the growth of human cancer cells, including paclitaxel (Taxol®) resistant HCT-15 human colorectal cancer cells, and showed potential use in combination therapy with known anticancer drugs such as paclitaxel, doxorubicin, gemcitabine, 5-FU and cisplatin.

About RX-5902

RX-5902 is a first-in-class small molecule that binds to and dysregulates p68 RNA helicase. RX-5902 also inhibits G2/M cell cycle progression, which is critical for cell cycle growth and cancer progression, and induces apoptotic cell death in cancer cells. Preclinical studies showed RX-5902 inhibits tumor growth, including drug-resistant tumors, in xenograft models by oral administration.