velusetrag

Velusetrag is a potent, highly selective small molecule agonist of the serotonin 5-hydroxytryptamine receptor 4 (5-HT4). It was originally discovered and developed by Theravance Biopharma for the treatment of gastrointestinal motility disorders, including gastroparesis, chronic idiopathic constipation, and irritable bowel syndrome. Velusetrag accelerates intestinal and colonic transit as well as gastric emptying by stimulating the 5-HT4 receptor in the enteric nervous system. The drug has demonstrated robust prokinetic activity in preclinical models and clinical trials, with high selectivity (>500-fold) for the human 5-HT4 receptor over other serotonin receptors. Clinical studies have shown efficacy in improving symptoms of chronic constipation and gastroparesis. Development has included collaboration with Alfasigma (formerly Alfa Wassermann), which acquired rights to velusetrag from Theravance Biopharma[1][2][3][4][5].

Other names

velusetrag