Product Candidates

XP20925
Migraine
Nausea

XP20925 is a Transported Prodrug of propofol, an intravenous anesthetic that is widely used in hospitals and outpatient settings to induce and maintain anesthesia during surgery, or to sedate patients undergoing diagnostic or medical procedures. Propofol was introduced in the United States in 1989 and is currently the world's leading IV anesthetic agent. Because propofol has very low oral bioavailability (due to its metabolism in the GI tract), it must be administered intravenously, limiting its uses to those procedures performed in hospital settings. Recent studies, however, have demonstrated that sub-anesthetic IV doses of propofol are effective in treating disorders such as nausea and vomiting and intractable migraine. Worldwide sales of anti-emetics for chemotherapy-induced nausea and for treatments of migraine each exceed $2 billion annually. We believe that XP20925 may be able to consistently achieve sub-anesthetic levels of propofol after oral dosing and may provide new methods for treating these disorders, especially for those patients who do not respond to current therapy.

We have designed XP20925 to utilize intestinal transporters to enhance absorption and simultaneously protect propofol from metabolism during absorption. Once absorbed, XP20925 is designed to convert rapidly to propofol, resulting in therapeutic exposure to the drug. Initial animal studies have demonstrated excellent oral bioavailability of propofol from XP20925. We plan to further develop XP20925 at an appropriate time in the future, depending on the availability of resources.

"The preclinical success of XP20925 is proof that we can take an intravenous drug like propofol and apply our Transported Prodrug technology to make it orally absorbable. This may represent a significant advance, because we may broaden considerably the potential indications that could benefit from the drug."

—Ken Cundy, Senior Vice President of Preclinical Development