Table 1: 5-HT4 receptor agonists in development for the treatment of GI motility disorders.
Compound Stage of development Mechanism of action Company Indication
Metoclopramide (PrimperanTM) Launched D2 antagonist, 5-HT3 antagonist,5-HT4 agonist Sanofi-Aventis Nausea-vomiting, GERD, diabetic gastroparesis
Clebopride (CleborilTM) Launched 5-HT4 agonist, 5-HT3 antagonist, D2 antagonist Almirall Nausea-vomiting
Cisapride (PrepulsidTM) Restricted use 5-HT4 agonist, 5-HT3 antagonist, 5-HT2 antagonist Johnson & Johnson GERD, gastroparesis
Mosapride (GasmotinTM) Launched 5-HT4 agonist, 5-HT3 antagonist Dainippon-Sumitomo Gastritis, GERD
Tegaserod (Zelnorm TM) Restricted use 5-HT4 agonist, 5-HT2 antagonist, 5-HT1 agonist, 5-HT3 antagonist Novartis IBS, Chronic idiopathic constipatio
Prucalopride (ResolorTM) Launched 5-HT4 agonist Movetis Chronic constipation
M0003, M0004 Phase II, discontinued 5-HT4 agonist Movetis GERD, gastroparesis
Renzapride Phase III, discontinued 5-HT4 agonist, 5-HT3 antagonist Alizyme IBS-C, IBS-M
E-3620 PhaseII, discontinued 5-HT4 agonist, 5-HT3 antagonist Eisai GI motility disorders
Naronapride Phase II 5-HT4 agonist ARYx Therapeutics Chronic idiopathic constipation, GERD, gastroparesis
Velusetrag Phase II 5-HT4 agonist Theravance Chronic constipation, gastroparesis
TD-8954 Phase I/II 5-HT4 agonist Theravance Eating disorder
YKP10811 Phase II 5-HT4 agonist SK biopharm Chronic constipation, IBS-C
TD-2749 Phase I 5-HT4 agonist Theravance GI motility disorders
AU-228 Phase I 5-HT4 agonist Abbott GI motility disorders
DA-6886 Phase I 5-HT4 agonist Dong-A ST IBS-C
RQ-10 Phase I 5-HT4 agonist RaQualia GI motility disorders
YH-12852 Phase I 5-HT4 agonist Yuhan IBS-C