Upsher-Smith Presents Data Highlighting Topiramate Extended-Release Formulation at 100th Annual APhA Meeting Findings Lead to Selection of an Optimal Formulation of Once-Daily USL255 (Extended-Release Topiramate) for Development in Epilepsy

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. 

  • "Development of a Once-Daily, Extended-Release Topiramate Formulation"
    Poster # 296.  Authors:  Lawrence J. Lambrecht, Wesley M. Todd, Mark B. Halvorsen

About The Poster
All 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:

  • Topiramate ER Cmax less than or equal to IR topiramate Cmax after a single-dose and at simulated steady-state.
  • Topiramate ER Cmin greater than or equal to IR topiramate Cmin at simulated steady-state.
  • Topiramate ER AUC that is equivalent for extent of exposure to IR topiramate after a single-dose and at simulated steady-state.

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 Pipeline
Upsher-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 Epilepsy
Epilepsy 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-Smith
Upsher-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.

*Topamax® (immediate-release topiramate) is a registered trademark of Johnson & Johnson Corporation.

1. Epilepsy Foundation. Available at: http://www.epilepsyfoundation.org/.  Accessed on February 10, 2012.

SOURCE Upsher-Smith Laboratories, Inc.



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