piboserod

Piboserod is a selective, orally available small molecule antagonist of the serotonin 4 (5-HT4) receptor. It was originally developed by GlaxoSmithKline and later investigated by other companies for several cardiovascular and gastrointestinal indications. Piboserod acts as a potent, competitive antagonist at the 5-HT4 receptor, blocking serotonin-mediated effects such as sensitization of the peristaltic reflex and defecation in animal models. In humans, it was studied for atrial fibrillation and irritable bowel syndrome (IBS), but development for both indications was discontinued after phase II trials. Later, it underwent phase II clinical evaluation in patients with chronic heart failure; while some improvement in left ventricular ejection fraction was observed, no significant changes were seen in other efficacy parameters[1][2][3][6].

Brand names

Serlipet

Other names

piboserod hydrochloride