SAN DIEGO, Oct. 26, 2017 /PRNewswire/ -- Neurana Pharmaceuticals Inc., a specialty pharmaceutical company focused on the development and commercialization of products that address unmet therapeutic needs of the central nervous system, today announced the successful top-line results from a clinical trial designed to confirm the non-sedative effects of tolperisone.
The Neurana study was designed as a three-way cross-over study in healthy volunteers that included tolperisone, placebo and the leading market-share product in the category, cyclobenzaprine (Flexeril®), which has been shown to be sedating in clinical use. The study used a driving simulation trial design acceptable to the U.S. Food and Drug Administration (FDA), and assessed various measures of cognition and sedation including both objective and subjective measures. The primary endpoint for the study was Standard Deviation of Lateral Position (SDLP), a driving performance measure that is highly correlated to blood alcohol levels (BAC).
On Day 1 at Tmax, tolperisone (450 mg total daily dose) was equivalent to placebo (p=0.9) for the primary endpoint of SDLP, while cyclobenzaprine (30 mg total daily dose) demonstrated significant impairment (p=<0.0001), correlating to a BAC of >0.05. On the morning of Day 2 predose, which assesses the next day residual effects ("hangover"), tolperisone was no different than placebo (p=0.7) for SDLP, while cyclobenzaprine demonstrated significant impairment (p=<0.0001). At steady state for both treatments on Day 3, tolperisone was equivalent to placebo (p=0.8) for SDLP, and cyclobenzaprine showed significant impairment (p=<0.0001).
This study was the second successful U.S. trial to assess the effects of sedation with tolperisone. An earlier trial indicated no difference in sedation vs. placebo when using patient-reported symptoms. The company believes that with these two completed positive U.S. studies establishing a lack of sedative effects of tolperisone, there is evidence for inclusion of non-sedation language in the tolperisone package insert. That could make it the only product in the skeletal muscle relaxant class to have a package insert which includes language for lack of sedation.
The company is planning to commence a Phase 2 clinical trial, in the first quarter of 2018, to evaluate the safety and efficacy of tolperisone in subjects with painful acute neuromuscular spasms. In this clinical trial, subjects will be evaluated for patient-reported response to a 2-week treatment of various doses of tolperisone compared to placebo. Completion of the Phase 2 clinical trial is expected to take approximately one year.
Neurana is the exclusive licensee for tolperisone in North America and other territories from Sanochemia. 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.
Previously Approved in International Markets
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 to relieve severe muscular spasms and provide analgesic effects. The product that is available outside the US has an impurity greater than the allowable limit established by the FDA. Sanochemia Pharmazeutica AG developed a highly purified form of tolperisone that provides the basis for a patent portfolio, including a Composition of Matter patent, which extends to 2032 in the U.S.
"We are pleased with the progress that has been made to establish a key differentiating factor in this large market, which now exceeds 60 million annual prescriptions in the United States," said Jeff Raser, Neurana's president and CEO.
"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, analgesic properties, and is non-sedating, which is confirmed by our present study. In addition, the broad clinical experience and patient usage with this compound outside of the United States suggests a 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 plans to initially develop tolperisone for the treatment of acute, painful muscular spasms and subsequently spasticity for the North American markets.
New Chemical Entity for the US Market
Tolperisone represents a novel approach for the treatment of acute, painful muscle spasms and spasticity for U.S. patients utilizing a unique mechanism of action without sedation, which is a common side effect of other marketed skeletal muscle relaxant products. With the positive results of this driving simulation study, Neurana plans to initiate Phase 2 clinical trials in the first quarter of 2018.
About Neurana Pharmaceuticals
San Diego, California-based Neurana Pharmaceuticals is a private company founded by an experienced and successful drug development and commercial team. The company is focused on the development of drugs to treat neuromuscular disorders.
SOURCE Neurana Pharmaceuticals Inc.