XenoPort issued United States composition of matter patent covering gabapentin prodrug.XenoPort, Inc. (Santa Clara Santa Clara, city, Cuba Santa Clara (sän`tä klä`rä), city (1994 est. pop. 217,000), capital of Villa Clara prov., central Cuba. , CA) announced the issuance of United States United States, officially United States of America, republic (2005 est. pop. 295,734,000), 3,539,227 sq mi (9,166,598 sq km), North America. The United States is the world's third largest country in population and the fourth largest country in area. Patent 6,818,787 covering the composition of matter of its proprietary compound, XP13512, and related analogs. XP13512 is a Transported Prodrug prodrug /pro·drug/ (-drug) a compound that, on administration, must undergo chemical conversion by metabolic processes before becoming an active pharmacological agent; a precursor of a drug. of gabapentin that is currently being tested in two separate Phase 2a studies. "We are pleased to receive patent coverage for an important new family of gabapentin prodrugs, including XenoPort's development-stage compound, XP13512," said Mark A. Gallop, senior vice president, research, and a co-inventor on the '787 patent. "Our objective in this project was to provide better gabapentin pharmacokinetics through oral dosing of these prodrugs compared to oral dosing of gabapentin itself. Preclinical and human clinical studies have shown that XP13512 is efficiently absorbed in the intestine and then rapidly converted to gabapentin. XP13512's unique ability to be absorbed in the large intestine large intestine End section of the intestine. It is about 5 ft (1.5 m) long, is wider than the small intestine, and has a smooth inner wall. In the first half, enzymes from the small intestine complete digestion, and bacteria produce many B vitamins and vitamin K. has allowed XenoPort to successfully develop the sustained-release formulation of XP13512 that is now being tested in the clinic." "The '787 patent is the first to issue from XenoPort's portfolio of over 30 applications involving this important product candidate," said D. Byron Miller, vice president and chief patent counsel. "We anticipate the issuance of additional patents that will further strengthen worldwide protection for this product candidate." XP13512 is a Transported Prodrug of gabapentin. Gabapentin is approved for marketing in the United States as adjunctive therapy adjunctive therapy Medtalk A therapeutic maneuver(s) with an ancillary role in treating a disease by ↓ M&M, but not part of the immediate therapy required to stabilize the Pt. Cf Adjuvant therapy. for epilepsy and to treat post-herpetic neuralgia Post-herpetic neuralgia Lingering pain that can last for years after an attack of shingles. Mentioned in: Electrical Nerve Stimulation . Worldwide sales of Pfizer's branded gabapentin (Neurontin) were $2.7 billion in 2003. As a Transported Prodrug of gabapentin, XP13512 utilizes high capacity transport mechanisms located in both the small and large intestine and rapidly converts to gabapentin once in the body. In contrast to gabapentin, XP13512 is absorbed efficiently from the large intestine -- a critical requirement for the successful development of a sustained release Sustained-release (SR), extended-release (ER, XR, or XL), time-release or timed-release, controlled-release (CR), or continuous-release (CR or Contin formulation with reduced dosing frequency. Besides gabapentin, the metabolic breakdown products of XP13512 are molecules that have well-established safety properties and are found naturally in mammals and in food. XP13512 is currently being examined as a treatment for both restless legs syndrome Restless Legs Syndrome Definition Restless legs syndrome (RLS) is characterized by unpleasant sensations in the limbs, usually the legs, that occur at rest or before sleep and are relieved by activity such as walking. and post-herpetic neuralgia in separate Phase 2a clinical studies. XenoPort is a privately held biopharmaceutical company focused on harnessing the body's intrinsic cellular transport systems to improve the oral absorption, distribution and pharmacokinetics of drugs. XenoPort is currently applying its technology to off-patent drugs off-patent drugs see generic (2). to create patentable Transported Prodrugs with improved medicinal properties. XP13512 is the first of several product candidates in XenoPort's portfolio to enter human trials. XenoPort intends to develop its product candidates through clinical proof of concept prior to establishing partnerships for further development and commercialization. XenoPort, Inc. +1-408-616-7200 |
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