Cơ Chế Tác Dụng :
XP19986 is in clinical development for the potential treatment of GERD, and is also a potential treatment for the symptoms of spasticity. XP19986 is a Transported Prodrug of the R-isomer of baclofen. Baclofen is a generic drug that is currently approved to treat spasticity and has been shown in investigator-led studies to be effective in the treatment of GERD. XP19986 is designed to overcome the deficiencies of baclofen by targeting high-capacity nutrient transporter mechanisms expressed throughout the length of the entire GI tract, including the colon.
XP19986 is well absorbed and rapidly converted to the R-isomer of baclofen.
XP19986 is new chemical entity that is a Transported Prodrug of R-baclofen with a covalently attached nutrient-mimic moiety that results in high-capacity absorption through GI tract and enables a sustained-release formation. XP19986 is designed to engage natural 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. By targeting high-capacity nutrient transporter mechanisms that exist throughout the length of the entire gastrointestinal tract, XenoPort believes that XP19986 can be formulated in a sustained-release pill to provide improved therapy.
Chỉ Định :
Investigated for use/treatment in gastroesophageal reflux disease (GERD).