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Development of palliative medicine in the United Kingdom and Ireland
Published in Eduardo Bruera, Irene Higginson, Charles F von Gunten, Tatsuya Morita, Textbook of Palliative Medicine and Supportive Care, 2015
Given serotonin's role in GI tract modulation and our increasing understanding of the multiple subtypes of serotonin receptors, several serotonergic agents have been studied. The 5 -HT4 agonist tegaserod has been FDA approved for constipation-predominant irritable bowel syndrome [66] The 5-HT4 agonist, prucalopride, has been approved for chronic constipation in Canada and Europe [67,68], but not in the United States; another 5-HT4 agonist, velusetrag, gave encouraging results in a phase 2 trial.
Current and emerging therapeutic options for the management of functional dyspepsia
Published in Expert Opinion on Pharmacotherapy, 2020
A. Vandenberghe, J. Schol, K. Van den Houte, I. Masuy, F. Carbone, J. Tack
Velusetrag is a highly selective 5-HT4agonist with a recently completed phase 2 study in gastroparesis. The underlying mechanism is a strong enhancement of the gastric emptying rate [51]. Data about the optimal dose of Velusetrag are controversial as symptoms are improved by a very low dose of 5 mg and not with higher doses, and with a seemingly higher efficacy in idiopathic compared to diabetic gastroparesis [52]. However, delayed gastric emptying improves when doses of 30 mg or higher are administered, illustrating the well-known dissociation between delayed gastric emptying and symptoms.
Drugs under development for the treatment of functional dyspepsia and related disorders
Published in Expert Opinion on Investigational Drugs, 2019
Jan Tack, Imke Masuy, Karen Van Den Houte, Lucas Wauters, Jolien Schol, Tim Vanuytsel, Alain Vandenberghe, Florencia Carbone
Another highly selective 5-HT4 agonist, was recently also evaluated in a phase 2b study for gastroparesis. In controlled trials evaluating 5, 15 and 30 mg doses, velusetrag 30 mg significantly enhanced gastric emptying [26], but significant symptom improvement was only observed with the 5 mg dose. Moreover, idiopathic gastroparesis patients seemed to show a better response to the 5 mg dose over placebo than those with diabetic gastroparesis [27]. A phase 3 study in idiopathic gastroparesis is planned.
Gastroparesis: pharmacotherapy and cardiac risk
Published in Scandinavian Journal of Gastroenterology, 2018
Per M. Hellström, Ahmad Al-Saffar
Other 5HT4 receptor stimulants such as mosapride have weak effects on hERG channels and less arrhythmogenic potential [27] when compared to cisapride. Furthermore, velusetrag as a new generation of 5-HT4 receptor agonist with high receptor selectivity is devoid of cardiac effects. This drug was primarily developed for treatment of chronic constipation [27], but is now in clinical trials for efficacy in diabetic and idiopathic gastroparesis.