Lesogaberan is a peripherally restricted high-affinity GABAB-R-specific agonist, originally developed for the treatment of gastroesophageal reflux disease (GERD) that appears to be safe for human use. The toxicity profile shows no indication of hepatic effect. Lesogaberan has been shown to induce decreased body weight and decreased food consumption. A dose-dependent diuretic effect was also noted in rats. Treatment with lesogaberan significantly enhanced replication of human islet cells in vitro, which was abrogated by a GABAB-R antagonist. Lesogaberan may be a promising drug candidate for clinical studies of diabetes intervention and islet transplantation. Disappointingly, in phase IIb study it was shown that lesogaberan is only marginally superior to placebo in gastroesophageal reflux disease (GERD) patients who are partially responsive to proton pump inhibitor (PPI) therapy.