lesogaberan

Lesogaberan is a peripherally restricted, high-affinity gamma-aminobutyric acid type B (GABAB) receptor agonist developed by AstraZeneca as an investigational small molecule for the treatment of gastroesophageal reflux disease (GERD)[1][2][4][5]. Its mechanism of action involves selective activation of GABAB receptors, which reduces transient lower esophageal sphincter relaxations (TLESRs), thereby decreasing reflux events[3][4][6]. Unlike baclofen, another GABAB agonist, lesogaberan was designed to minimize central nervous system side effects by being actively transported out of the CNS[1][7]. Clinical trials showed that it reduced TLESRs and reflux episodes in GERD patients partially responsive to proton pump inhibitors but was only marginally superior to placebo in symptom improvement[6]. Lesogaberan has also been studied for refractory chronic cough and shown some effect on cough hypersensitivity but did not significantly reduce overall cough frequency[7]. Preclinical studies indicated additional effects such as decreased body weight and food consumption in animals. Development for GERD was discontinued after phase IIb due to limited efficacy over placebo[5].

Other names

lesogaberan hydrochloride