TY - JOUR
T1 - Lesogaberan
T2 - GABAB receptor agonist treatment of gastroesophageal reflux disease
AU - Lacy, Brian E.
AU - Chehade, Robert
AU - Crowell, Michael D.
PY - 2010/12
Y1 - 2010/12
N2 - (Chemical Equation Presented) Gastroesophageal reflux disease (GERD) is a highly prevalent medical disorder. Most patients require chronic medical therapy and proton pump inhibitors (PPIs) are the mainstay of treatment. Some patients, however, have persistent symptoms of reflux despite PPI therapy. A medication to treat the major pathophysiologic event that causes reflux, transient lower esophageal sphincter relaxations (TLESRs), could improve reflux symptoms and potentially reduce complications of persistent acid reflux. Baclofen, a GABAB receptor agonist, has been shown to reduce TLESRs and acid reflux in both healthy volunteers and patients with GERD. Central nervous system (CNS) side effects limited its use in clinical practice. Lesogaberan is a novel, peripherally acting, GABAB receptor agonist with limited CNS side effects that decreases TLESRs, reduces the number of acid reflux events and improves acid exposure time in the distal esophagus. This monograph will review the pharmacology, preclinical and clinical data, and discuss the safety of this new compound.
AB - (Chemical Equation Presented) Gastroesophageal reflux disease (GERD) is a highly prevalent medical disorder. Most patients require chronic medical therapy and proton pump inhibitors (PPIs) are the mainstay of treatment. Some patients, however, have persistent symptoms of reflux despite PPI therapy. A medication to treat the major pathophysiologic event that causes reflux, transient lower esophageal sphincter relaxations (TLESRs), could improve reflux symptoms and potentially reduce complications of persistent acid reflux. Baclofen, a GABAB receptor agonist, has been shown to reduce TLESRs and acid reflux in both healthy volunteers and patients with GERD. Central nervous system (CNS) side effects limited its use in clinical practice. Lesogaberan is a novel, peripherally acting, GABAB receptor agonist with limited CNS side effects that decreases TLESRs, reduces the number of acid reflux events and improves acid exposure time in the distal esophagus. This monograph will review the pharmacology, preclinical and clinical data, and discuss the safety of this new compound.
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U2 - 10.1358/dof.2010.035.012.1540661
DO - 10.1358/dof.2010.035.012.1540661
M3 - Review article
AN - SCOPUS:79956195307
SN - 0377-8282
VL - 35
SP - 987
EP - 992
JO - Drugs of the Future
JF - Drugs of the Future
IS - 12
ER -