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.
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.
About Rexahn Pharmaceuticals, Inc.
Rexahn Pharmaceuticals is a clinical stage pharmaceutical company dedicated to developing and commercializing first in class and market leading therapeutics for cancer, CNS disorders, sexual dysfunction and other unmet medical needs. Rexahn currently has three drug candidates in Phase II clinical trials, Archexin®, Serdaxin®, and Zoraxel™ - all potential best in class therapeutics - and a robust pipeline of preclinical compounds to treat multiple cancers and CNS disorders. Rexahn also operates key R&D programs of nano-medicines, 3D-GOLD, and TIMES drug discovery platforms. For more information, please visit
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