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Portfolio

Rexahn’s portfolio presents unique compounds for a wide variety of conditions from cancer to brain disorders. This highly diversified pipeline promises to bring an improved standard of care in multiple healthcare sectors.

Rexahn’s robust pipeline of clinical-stage and pre-clinical compounds being internally developed or co-developed with a partner:

Serdaxin® – Depression and Parkinson’s disease
Unlike other treatments for mood disorders, Serdaxin tackles three mechanisms simultaneously: serotonin, dopamine, and neuronal survival. Serotonin is a traditional pillar in understanding depression. Previous research indicates that loss of serotonin in the brain underlies common symptoms such as anxiety. Recent findings, however, indicate that dopamine plays a central role in other aspects of the disease, including anhedonia (loss of pleasure) and lack of motivation. In preclinical studies, Serdaxin supports both serotonergic and dopaminergic systems in the brain, enabling a multi-prong approach to treating depression. [READ MORE]

Zoraxel™
Zoraxel is a developmental stage drug for sexual dysfunction that directly modulates the sexual activity control center in the brain. Zoraxel enhances the action of serotonin and dopamine, brain signaling molecules that play a key role in three phases of male sexual activity: arousal, erection and release. Zoraxel is the first ED therapeutic to affect all three of these phases. [READ MORE]

Archexin™
Archexin is a first-in-class, potent inhibitor of Akt-1 protein kinase which is involved in the proliferation of cancer cells. Archexin is in Phase II trials for the treatment of pancreatic cancer and has US FDA orphan drug designation for five cancers (RCC, glioblastoma, and cancers of the ovary, stomach and pancreas). Multiple indications for other solid tumors may also be pursued. [READ MORE]

Pre-Clinical Development

Preclinical Oncology Pipeline

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 novel piperazine-based small molecule that interferes with microtubule structure and G2/M cell cycle in cancer cells. Studies demonstrated drug-resistant tumors recede in xenografted model 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 caner 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 and 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 model showed RX-0047 inhibits tumor growth in lung and prostate and blocks metastasis.

HPMA
Among the prominent nano-polymer drugs in Rexahn, HPMA-gemcitabine and HPMA-docetaxel 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.

Partnering
Part of our strategy for success is to form selective and strategic partnerships with pharmaceutical companies to develop and commercialize some of our drug candidates. We aim to structure these partnerships to retain significant co-promotion or co-commercialization rights in certain worldwide markets to capture long-term value from our innovations. [READ MORE]

Discovery Platform
We have a highly productive discovery platform that continues to yield a portfolio rich in potential first-in-class and best-in-class compounds. Our discovery platform features small signaling molecule discovery (TIMES), computational predictive modeling (3D-GOLD) and nanoscale drug targeting and delivery. Working in concert, these technologies enables us to screen, select and optimize large numbers of compounds while retaining stringent selection criteria. [READ MORE]