Neurana Pharmaceuticals, a specialty pharmaceutical company focused on the development and commercialization of products that address unmet therapeutic needs of the central nervous system, announced receipt of a Notice of Allowance from the US Patent and Trade Office (USPTO) for two new tolperisone patents, including a second Composition of Matter patent for a novel form of tolperisone.

The company also received a Notice of Allowance for a Method of Making patent. Tolperisone, an approved product that has regulatory approval and is commercialized in many countries outside the United States, has demonstrated improvement in the treatment of skeletal muscle disorders without sedation. A requirement by the US Food and Drug Administration (FDA) for a highly purified form of tolperisone provided the basis for the four patents that are either issued or subject to issuance.  The tolperisone patent family term extends to 2032. Tolperisone also was granted a composition of matter patent that has been issued in Canada.

Neurana is the exclusive licensee for tolperisone in North America and other territories from Sanochemia Pharmazeutika . The licensing agreement provides Neurana the right to develop and market Sanochemia's proprietary and patent protected tolperisone formulation in the United States and other licensed territories.  Neurana plans to initially develop tolperisone for the treatment of acute, painful muscle spasms as well as for spasticity.

Tolperisone holds a market-leading position in Eastern Europe, Germany and parts of Asia as an approved treatment for muscular pain and neuromuscular spasms.  The product has a unique, dual mechanism of action that acts on the peripheral neural system as well as in the spinal cord and brainstem to relieve severe muscular spasms and significantly improve patient mobility.  Another major benefit is that clinical studies have shown that tolperisone is efficacious without sedation, which is a common side effect of other marketed skeletal muscle relaxant products.  

"We are pleased with the progress that has been made to establish broad intellectual property protection for tolperisone. Due to this new process, tolperisone is designated as a New Chemical Entity (NCE) in the US. Several of tolperisone's patents will be eligible for listing in the Food and Drug Administration's Approved Drug Products with Therapeutic Evaluation Equivalence List (Orange Book), which confers long term intellectual property protection for this differentiated product.  If approved, tolperisone is expected to provide significant advantages for patients in the large skeletal muscle relaxant market," said Jeff Raser, Neurana's president and chief executive officer.


"Based on market research and actual patient use data, physicians and patients have expressed a strong preference for an effective muscle relaxant that has the profile of tolperisone: a rapid onset of action, no risk of abuse, and non-sedating. In order to confirm the non-sedating properties of tolperisone, Neurana will commence a Driving Simulation study in the second quarter of 2017. Results are expected by the fourth quarter of this year.  In addition, the broad clinical experience and patient usage with this compound outside of the United States suggests low clinical development and regulatory risk," said Judy Caron, PhD., Neurana's chief operating officer and head of Clinical Development.

Neurana's experienced team has successfully developed, gained regulatory approval for, and commercialized CNS drugs. The team will initially develop tolperisone for the treatment of acute, painful muscular spasms and subsequently spasticity for the North American markets (United States, Canada and Mexico).  In the United States, treatment for these indications accounts for more than 60 million prescriptions per year and represents a significant branded market potential.

"We are excited to receive these patents and to continue to advance the clinical development of tolperisone, which builds on the already issued patent family and significant existing development work," said David F. Hale, Neurana's executive chairman.

While tolperisone has demonstrated efficacy and safety in years of clinical practice in Germany, Eastern Europe and Asia, it has never been fully clinically tested or approved in the United States.  Tolperisone will represent a novel approach for the treatment of acute, painful muscle spasms and spasticity for US patients.  Accordingly, tolperisone will be classified as a new chemical entity (NCE) for the US market, which, in addition to the issued patents confers regulatory exclusivity.  There is an approved open investigational new drug application (IND), and data from recent tolperisone pre-clinical and clinical trials have already been submitted to the FDA.  The product is ready for Phase 2 clinical studies and Neurana believes that, subject to successful Phase 2 and Phase 3 clinical trials, a New Drug Application (NDA) can be filed within four years.