MAPLE GROVE, Minn., March 12, 2012 /PRNewswire/ -- Upsher-Smith Laboratories, Inc. (http://www.upsher-smith.com) today presented Phase I pharmacokinetic data evaluating the profiles of 10 internally developed once-daily, extended-release formulations of the epilepsy medication topiramate. Of the formulations investigated, one extended-release (ER) formulation of topiramate emerged as being optimal for further development by meeting all pre-established single-dose and simulated steady-state goals as compared with immediate-release (IR) topiramate (Topamax) administered to healthy volunteers. These findings led to the further development of USL255, an investigational treatment for the management of epilepsy in adults. USL255 is currently the subject of a global Phase III clinical trial (PREVAIL). Information about the trial can be found at: http://clinicaltrials.gov/ct2/show/NCT01142193?term=upsher+smith&rank=4.
The poster was presented on Saturday, March 10, at the American Pharmacists Associations' (APhA) 2012 Annual Meeting in New Orleans, LA (http://www.aphameeting.org).
"With the identification of an optimal formulation of extended-release topiramate, we hope to reduce the blood level fluctuations that can occur when taking immediate-release topiramate and that may be associated with adverse events at peak levels and break-through seizures at trough levels," said Mark Halvorsen, Pharm.D., Senior Director, Clinical Development at Upsher-Smith.
The abstract of this poster is available in the March/April edition of the Journal of the American Pharmacists Association. Copies of the journal are available onsite at the APhA Annual Meeting.
About The PosterAll trials were randomized, open-label, single-dose, crossover pilot studies comparing topiramate extended-release formulations to immediate-release topiramate in healthy adult subjects. In the trials, the subjects received either IR topiramate as a single 100 mg dose, IR topiramate as two individual 100 mg doses (administered 12 hours apart), or a single 200 mg dose of ER topiramate. Due to the long half-life of topiramate, each of the study arms included a 14-day sampling period.
The study program was designed to identify an optimal ER topiramate formulation meeting the following a priori PK goals:
Only one ER formulation met all single-dose and simulated steady-state a priori PK goals, including lower Cmax, higher Cmin, and equivalent extent of exposure as compared with IR topiramate. No unexpected adverse events were seen; adverse events were consistent with those expected for topiramate.
Upsher-Smith's Expanding CNS PipelineUpsher-Smith's central nervous system (CNS) pipeline includes a number of investigational drug programs. In addition to USL255 (extended-release topiramate), USL is developing an intranasal midazolam (USL261), for the rescue treatment of seizures in patients on stable anti-epileptic drug regimens who require control of intermittent bouts of increased seizure activity, frequently referred to as seizure clusters. Another program is USL260 (tonabersat), an investigational drug and first-in-class neuronal gap junction modulator which is also a potential treatment for epilepsy.
About EpilepsyEpilepsy is a medical condition that produces seizures affecting a variety of mental and physical functions. Almost three million people in the U.S. have some form of epilepsy with about 200,000 new cases of epilepsy diagnosed each year.(1)
About Upsher-SmithUpsher-Smith Laboratories, Inc., founded in 1919, is a rapidly growing, privately held pharmaceutical company that develops, manufactures, and markets prescription and consumer products. Upsher-Smith's product portfolio focuses in the areas of women's health, dermatology, cardiology, and CNS diseases. The company's focus is growing a CNS pipeline for diseases with significant unmet need, including epilepsy and Parkinson's disease. To expand its CNS pipeline, Upsher-Smith seeks alliances and co-development programs, pursues licensing and acquisitions, and leverages its core competency in formulation development. For more information, visit http://www.upsher-smith.com.
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Upsher-Smith Presents Data Highlighting Topiramate Extended-Release Formulation at 100th Annual APhA Meeting