Rexahn has a robust pre-clinical oncology product pipeline that features potential first-in-class therapeutics:
RX-1792
RX-1792 is a quinazoline analogue that suppresses protein kinase Akt and c-Fos, critical components of tumor growth and metastasis. Preclinical studies showed RX-1792 inhibits tumor growth in xenograft models.
RX-5902
RX-5902 is a first-in-class small molecule that binds to and dysregulates p68 RNA helicase. RX-5902 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 of RX-5902.
RX-3117
RX-3117 is being co-developed with Teva Pharmaceutical Industries for the treatment of cancer cells and tumors, in particular gemcitabine-resistant lung cancer. RX-3117 has shown potent anti-tumor effects in xenograft human tumor models. Preclinical studies revealed the high bioavailability and superior toxicity profile compared to gemcitabine, the current first-line therapy for pancreatic and other cancers.
RX-8243
RX-8243 is a novel isoquinolinamine analogue that inhibits Ark1 (Aurora A) kinase and other Ser/Thr kinase in cancer cells. RX-8243 is a multikinase inhibitor that downregulates signal molecules of RAS as well as PI3K pathways such as activated forms of ERK, p38 and Akt. Preclinical studies showed RX-8243 blocks tumor growth in xenograft models at low nanomolar concentrations.
RX-0201-N
RX-0201, or Archexin™, is a first-in-class, potent inhibitor of Akt protein kinase in the treatment of cancer. Akt regulates signal processes of cell proliferation and survival, angiogenesis, and drug resistance in cancer. Phase II clinical programs are ongoing. Archexin™ is being developed to treat solid tumors and has FDA orphan drug designation for RCC, pancreatic, stomach, glioblastoma, and ovarian cancers. Archexin™ is in Phase II clinical development for pancreatic cancer as lead indication.
RX-0047 and RX-0047-N
RX-0047 is a potent inhibitor of HIF-1α, a key transcription factor involved in cancer cell survival, metastasis, and angiogenesis. HIF-1α is over-expressed in a broad range of human cancers, and associated with increased cancer mortality and resistance. RX-0047 inhibits proliferation of cancer cells of human origin at low nanomolar concentrations by lowering mRNA level of HIF-1α. It is also effective in radiation-resistant cancer cells. Studies in xenografted models showed RX-0047 inhibits tumor growth in the lung and prostate and blocks metastasis.
RX-21101 and RX-21202: Nano-polymer Anticancer Drugs
Among the prominent nano-polymer drugs in Rexahn, RX-21101 (HPMA-docetaxel) and RX-21202 (HPMA-gemcitabine) are anticancer drugs that can overcome the downside of cytotoxic compounds, such as poor solubility, stability, and severe adverse reactions. Conjugating water-soluble and non-toxic HPMA to conventional anticancer compounds bolster efficacy while lowering toxicity by specific tumor targeting and increased stability in body.
Preclinical Oncology Pipeline
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RX-1792 | RX-5902 | RX-3117 | RX-8243 | RX0201-N | RX0047-N | RX-21101 & RX-21202 |  |
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EGFR inhibition | Microtubule inhibition Apoptosis Inducer |
DNA synthesis Inhibition | Aurora kinase inhibition |
Akt-1 inhibitor |
HIF-1 alpha inhibitor |
Anti- metabolite Microtubule Inhibition |
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Targeted anticancer Small molecule |
Targeted anticancer Small molecule Oral delivery |
Targeted anticancer Nucleoside Oral delivery |
Targeted anticancer Small molecule |
Targeted delivery 1st in class Antisense Nano- medicine |
Targeted delivery 1st in class Antisense Nano- medicine |
Targeted delivery Small molecule Nano- medicine |
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