Proprietary Nasal Delivery Formulation of Diazepam Reaches NDA

CLEVELAND, Ohio -- The Lubrizol Corporation announces a proprietary nasal delivery formulation of diazepam for the treatment of epilepsy which was developed by contract development and manufacturing organization (CDMO), Particle Sciences, a Lubrizol LifeSciences company, has been submitted as a New Drug Application (NDA) to the U.S. Food and Drug Administration (FDA) by San Diego-based Neurelis Inc.

VALTOCO™, previously referred to in clinical development as 'NRL-1', is the lead product candidate of Neurelis, worked closely with Particle Sciences on the formulation of the diazepam nasal spray designed to treat acute repetitive seizures in patients over the age of six.

Using its DOSE® platform that combines empirically obtained data with customized solubility software based on Hansen solubility parameters, Particle Sciences was able to achieve extremely high levels of solubilized diazepam using a benign vehicle that is compatible with nasal delivery. The resulting absolute bioavailability of the VALTOCO intranasal formulation was 96% of intravenous diazepam in a Phase 1 cross-over trial of healthy volunteers.

The NDA for VALTOCO is a 505(b)(2) filing utilizing rectal diazepam gel, the only current FDA approved therapeutic product for home treatment of acute repetitive seizures, as the Reference Listed Drug. The NDA is supported by further extensive clinical studies in healthy volunteers and patients with epilepsy, with more than 1,600 seizures treated to date with the nasal spray.

Dr. Robert Lee, president of Particle Sciences states, "It's rewarding to see VALTOCO reach this key milestone after Neurelis' successful clinical trials. This product will bring positive improvements to the lives of many patients with acute repetitive seizures."

Lee adds, "Nasal delivery is often an overlooked route of administration but can offer an ideal path and increase bioavailability for several drug types, particularly those designed to treat diseases of the central nervous system. We are seeing real growth in this area and expect to see an increase in demand for nasal formulations in the future as we continue to focus on the development of complex drug products."

Craig Chambliss, president and CEO of Neurelis comments, "Having assessed dozens of formulation approaches for solving the challenges with delivering intranasal benzodiazepines for epilepsy patients, we partnered with Particle Sciences to leverage their experience and expertise in solving for a formulation issue that has kept poorly soluble drugs from being developed for significant unmet clinical needs."

According to the Centers for Disease Control and Prevention, there are more than 3.4 million people with epilepsy in the United States with approximately 200,000 new patients diagnosed each year.  Despite the availability of chronic, daily oral medications to control epilepsy, a significant number of these patients continue to experience seizures. Of these uncontrolled patients, about 170,000 are at risk for cluster or acute repetitive seizures.

Particle Sciences will be exhibiting at this year's American Association of Pharmaceutical Scientists (AAPS) PharmSci 360 November 4 - 7 on stand #2319.

Particle Sciences is part of Lubrizol Advanced Materials Inc.  For more information, visit www.lubrizolcdmo.com.

About The Lubrizol Corporation

The Lubrizol Corporation, a Berkshire Hathaway company, is a specialty chemical company whose science delivers sustainable solutions to advance mobility, improve wellbeing and enhance modern life. Founded in 1928, Lubrizol owns and operates more than 100 manufacturing facilities, sales and technical offices around the world and has more than 8,000 employees. For more information, visit www.Lubrizol.com.

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