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US Patent Granted for a New Family of Heat Shock Protein 90 (Hsp90) Inhibitors for the Treatment of Cancer and Neurodegenerative Indications

NEW YORK, May 19, 2011 /PRNewswire/ -- NexGenix Pharmaceuticals Inc., a privately-held company developing treatments for cancer, neurodegenerative diseases, and orphan neurogenetic disorders, today announced that the United States Patent and Trademark Office (USPTO) has issued a Notice of Allowance for a key patent for a platform of Hsp90 inhibitors based on derivatives of the  naturally occurring pochonin family, Pochonia chlamydospora.  The platform of fully synthetic small molecules covered by this composition of matter patent was developed in the laboratory of Dr. Nicolas Winssinger at the University of Strasbourg (UNISTRA) and is exclusively licensed to NexGenix.

The patent, entitled "Macrocyclic Compounds Useful as Inhibitors of Kinases and Hsp90", provides an exclusivity period until August 2027.  The patent specifically covers the proprietary scaffold and its composition along with a large library of compounds, including NexGenix's lead Hsp90 inhibitors aimed at cancer and neurodegenerative indications.  The pochonin scaffold represents an advancement in Hsp90 inhibition beyond several molecules developed over the last decade based on radicicol and geldanamycin derivative (17-AAG) which have been shown to exhibit highly potent anti-tumor activity in numerous pre-clinical and clinical studies.

Professor Nicolas Winssinger of UNISTRA stated, "Through a research collaboration agreement with NexGenix in 2007, we have developed a library of hundreds of molecules based on the scaffold that is covered by the patent allowed by USPTO. These molecules have been developed through an iterative process based on extensive in vitro and in vivo studies conducted by NexGenix in the selection of a lead candidate. I am looking forward to continuing these collaborative development activities."

X-ray crystallography studies have demonstrated deeper binding of NexGenix's molecules to the Hsp90 ATP binding pocket compared to other small-molecule Hsp90 inhibitor compounds for which crystallography has been published.   This generally translates to interaction deep in the protein-binding pocket with the molecule remaining longer and thus inhibiting the protein for longer periods.  Another major key differentiating point of the platform is that a subset of the library of over 500 molecules developed to date has the ability to cross the blood-brain barrier and the blood spinal cord barrier, making them particularly attractive candidate therapeutics for CNS indications, such as primary and secondary tumors of the CNS and neurodegenerative disorders.

Dr. Allan Rubenstein, NexGenix's CEO, said, "The grant of this US patent is part of a broad platform of intellectual property rights.  NexGenix now has seven patent families allowed or pending covering the Company's compounds, various uses of these compounds, and other proprietary know-how.  We believe that this matrix of intellectual property provides NexGenix with a unique position to benefit from the therapeutic applications of Hsp90 inhibitors."

The Company is currently in late stage pre-clinical development for its lead Hsp90 inhibitor with its unique ability to cross the blood-brain-barrier as a treatment for primary and metastatic brain tumors. NexGenix plans to seek regulatory approval to conduct a Phase I clinical trial to evaluate the safety, tolerability, and pharmacokinetics of its lead Hsp90 inhibitor in advanced solid tumor malignancies.

About NexGenix:  NexGenix Pharmaceuticals Inc. is a privately held biotechnology company based in New York City.  The Company's portfolio consists of a series of Hsp90 inhibitors, a novel target therapy for oncology and neurodegenerative disorders, which has attracted an enormous amount of development interest in the past several years.  The Company's proprietary Hsp90 screening platform has already generated over 500 potential compounds.  From this group, five lead drug candidates have been subjected to extensive in vitro and animal studies on the basis of their pharmacokinetics, pharmacodynamics and superior efficacy, safety, and the ability to cross the blood brain barrier, and one drug candidate has been selected for clinical evaluation.  The lead drug candidate profile lends itself to addressing diseases such as glioblastoma (or "glioma", commonly known as malignant brain tumor) and other cancers, as well as neurodegenerative disorders such as Amyotrophic Lateral Sclerosis (ALS), Alzheimer's Disease and Parkinson's Disease. In addition, the Company is pursuing an EMEA hybrid application, a clinical stage intralesional treatment for dermal neurofibromas, the most common lesion in Neurofibromatosis Type 1, and has discovered molecules that represent an early research stage program in inhibitors of p21-activated kinase for indications including Neurofibromatosis Type 2 and Autism Spectrum Disorders.

This news release may contain forward-looking statements that reflect NexGenix's current expectations regarding future events, including development and regulatory clearance of the NexGenix's products. Forward-looking statements involve risks and uncertainties.  Actual events could differ materially from those projected herein and depend on a number of factors, including (inter alia), the success of the NexGenix's research strategies, the applicability of the discoveries made therein, the successful and timely completion of uncertainties related to the regulatory process, and the acceptance of NexGenix's Hsp90 inhibitor and other products by consumer and medical professionals.

Other Notes

Patent: "Macrocyclic Compounds Useful as Inhibitors of Kinases and Hsp90"
Patent serial number: US 11/891,652. Filed: August 10, 2007.  Inventors: Nicolas Winssinger, et. al. Patent abstract: The invention relates to novel derivatives, analogs and intermediates of the naturally occurring pochonin family, Pochonia chlamydospora, and to their syntheses. The invention is further related to use of these compounds as inhibitors of kinases and of the enzyme family known as heat shock protein 90 (Hsp90).

Prior Hsp90 Inhibitors developments: The Hsp90 inhibitors, that have been subject of pre-clinical and clinical studies by a number of pharmaceutical companies over the past decade, have been primarily based on either radicicol, isolated from naturally occurring Diheterospora chlamydosporia, or geldanamycin (which is also a naturally occurring benzoquinone ansamycin antibiotics that can be isolated from Streptomyces hygroscopicus) and its derivative 17 allylamino-17-demethoxygeldanamycin


Potential Therapeutic Use of the Company's Hsp90 Inhibitors:  Cancer indications represent the initial target indication for the Company's Hsp90 Inhibitors in the United States. NexGenix has planned a Phase I, Open-Label, multi-center, dose-escalation study to evaluate the safety, tolerability, and pharmacokinetics of NexGenix's lead Hsp90 Inhibitor in patients with various solid tumor cancers including enrichment cohorts with recurrent high-grade gliomas and Her2+ breast cancer.  Additional cancer indications are under pre-clinical evaluation as further possibility for clinical trials.

Potential Therapeutic Use in Glioma:  Glioma is the most common primary, malignant brain tumor, with 15,000 new cases presenting each year in the United States alone.  Prognosis is invariably poor, with few treatment options.  Current standard of care includes surgical resection, followed by radiation and/or chemotherapy.  Even with such treatment, median survival for patients with glioma multiforme is 10-15 months, with a one-year survival rate of only 29%, and a five-year survival rate of only 6%.  The very aggressive nature of gliomas is attributed to their highly angiogenic and highly invasive nature.  Thus, anti-angiogenic therapies are only partly effective – as they do not inhibit invasion.  Another limitation in treating gliomas is the presence of the blood-brain barrier.  Thus, for a therapeutic to be an effective treatment for glioma, it must target both angiogenesis and invasion, and must penetrate the blood-brain barrier.

Potential Therapeutic Use in HER2+ Breast Cancer with Brain Metastases:  Amplification of Her2 receptor tyrosine kinase ("Her2") appears to occur in 20%-30% of all breast cancers.  Antibody-directed therapy with trastuzumab, which targets the extracellular domain of Her2, has been efficacious to some degree.  However, resistance to trastuzumab is common and added complications of resistance include metastatic disease where approximately 60% develop resistance after a year.  An alternate therapy which also targets Her2 is needed.  Treatment with Hsp90 inhibitors appears to induce the degradation of the Her2 receptor, thereby providing an alternate means for treating Her2+ tumors.  In fact, in clinical studies, Hsp90 inhibitors have demonstrated activity – clinical partial or complete response to therapy – against Her2+ tumors.

SOURCE NexGenix Pharmaceuticals Inc.
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