SANTA CLARA, Calif., Oct. 26 /PRNewswire-FirstCall/ -- XenoPort, Inc. announced today that it has initiated a Phase 2a clinical trial of XP19986 in patients with gastroesophageal reflux disease, or GERD. The trial is a multi-center, randomized, double-blind, placebo-controlled, cross-over study designed to assess the safety, tolerability and efficacy of XP19986. The clinical trial is intended to test the ability of escalating single doses of a prototype sustained-release formulation of XP19986 to reduce reflux episodes. XenoPort expects to complete this Phase 2a clinical trial in the first half of 2006.
Ronald W. Barrett, Ph.D., XenoPort’s chief executive officer, stated, “We are excited to begin the exploration of XP19986 as a potential new treatment for GERD. There is increasing recognition of the need for new GERD pharmacotherapies beyond that of the existing acid suppressing agents. We believe that the favorable pharmacokinetics and unique mechanism of action of XP19986 may address these unmet medical needs of GERD patients.”
About XP19986
XP19986 is designed to overcome the deficiencies of baclofen, a currently marketed generic drug approved for the treatment of spasticity. Baclofen is a racemic drug (a 50:50 mixture of R- and S-isomers). Studies conducted by third parties have shown that the beneficial therapeutic properties of baclofen are attributable to the R-isomer of baclofen only. Baclofen has a short half-life in blood after oral dosing, which necessitates frequent daily dosing. Absorption of baclofen in the colon is limited, which has prevented the development of a sustained-release formulation that could improve therapy.
XP19986 is a new chemical entity that is a Transported Prodrug of R-baclofen. XP19986 is designed to engage natural nutrient transport mechanisms found on intestinal cell membranes, thereby gaining efficient entrance into the bloodstream. XP19986 is then rapidly converted to R-baclofen by high-capacity enzymes. In addition to R-baclofen, the metabolic breakdown products of XP19986 are natural substances with favorable safety characteristics.
XenoPort’s recent Phase 1 clinical trial testing multiple formulations of XP19986 identified the prototype sustained-release formulation that has been selected for further clinical trials. This formulation demonstrated a delayed time to maximal R-baclofen blood concentrations and a long terminal half-life, consistent with the requirements for twice-a-day dosing. Comparison with historical pharmacokinetic data for racemic baclofen dosed three or four times a day suggests that XP19986 taken twice-a-day should be associated with a decreased peak-to-trough ratio of R-baclofen blood levels over 24 hours compared to racemic baclofen.
About GERD and Baclofen
GERD is a digestive system disorder caused by inappropriate relaxations of the lower esophageal sphincter, which is a combination of muscles that controls the junction between the esophagus and the stomach. GERD is characterized by the frequent, undesirable passage of stomach contents into the esophagus that results in discomfort and potential damage to the lining of the esophagus. More than $10 billion is spent worldwide each year on GERD and heartburn medications, and approximately 7% of the global population experiences GERD symptoms daily. Conventional treatment for GERD includes medications that suppress stomach acid, including proton pump inhibitors and H2-receptor antagonists, as well as over-the-counter antacids. However, these treatments are not effective in all patients, and there is a subset of patients who suffer from GERD symptoms due to reflux of stomach contents that are not acidic.
Baclofen has recently been the subject of clinical trials demonstrating that it may be effective in treating GERD. Unlike acid suppressing agents, baclofen exerts its effects on the function of the lower esophageal sphincter. Baclofen reduces the frequency of transient lower esophageal sphincter relaxations and, therefore, passage of gastric contents into the esophagus. We believe that the favorable pharmacokinetics of XP19986 may make it well suited for treatment of GERD, either as monotherapy or in combination with an acid suppressing agent.
About XenoPort
XenoPort, Inc. is a biopharmaceutical company focused on developing a portfolio of internally discovered product candidates that utilize the body’s natural nutrient transport mechanisms to improve the therapeutic benefits of existing drugs. XenoPort’s most advanced product candidate, XP13512, has successfully completed a Phase 2b clinical trial for the treatment of restless legs syndrome, or RLS, and a Phase 2a clinical trial for the management of post-herpetic neuralgia. XenoPort anticipates commencing Phase 3 clinical trials of XP13512 in RLS patients in the first half of 2006. XenoPort has also completed an initial Phase 1 clinical trial of XP19986, a Transported Prodrug of R-baclofen. This trial demonstrated that XP19986 was suitable for twice-a-day dosing and was well tolerated with few adverse events at the doses tested. XenoPort has commenced additional studies of XP19986, including a Phase 2a clinical trial in gastroesophageal reflux disease, or GERD, patients.
To learn more about XenoPort, please visit the web site at www.XenoPort.com.
Forward-Looking Statements
This press release contains “forward-looking” statements, including, without limitation, all statements related to our future clinical development programs for XP13512 and XP19986, the therapeutic and commercial potential of XP13512 and XP19986 and our future clinical trials. Any statements contained in this press release that are not statements of historical fact may be deemed to be forward-looking statements. Words such as “believes,” “anticipates,” “plans,” “expects,” “will,” “intends” and similar expressions are intended to identify forward-looking statements. These forward-looking statements are based upon XenoPort’s current expectations. Forward-looking statements involve risks and uncertainties. XenoPort’s actual results and the timing of events could differ materially from those anticipated in such forward-looking statements as a result of these risks and uncertainties, which include, without limitation, the ability of the company to successfully conduct the clinical trials for XP13512 and XP19986; the uncertainty of the FDA approval process; and the therapeutic and commercial value of the company’s compounds. These and other risk factors are discussed under the heading “Risk Factors” in our Quarterly Report on Form 10-Q for the quarter ended June 30, 2005, filed with the Securities and Exchange Commission on August 11, 2005. XenoPort expressly disclaims any obligation or undertaking to release publicly any updates or revisions to any forward-looking statements contained herein to reflect any change in the company’s expectations with regard thereto or any change in events, conditions or circumstances on which any such statements are based.
NOTE: XenoPort is a registered U.S. trademark.
Source code: XNPT2C
XenoPort, Inc.
CONTACT: Jackie Cossmon of XenoPort, Inc., +1-408-616-7220, orir@XenoPort.com
Web site: http://www.xenoport.com/
