Drug intelligence / Profile preview

tegaserod + proton pump inhibitor

Development stage
Unknown
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

Tegaserod + proton pump inhibitor refers to the therapeutic co-administration of tegaserod, a selective serotonin 5-HT4 receptor agonist, with a member of the proton pump inhibitor (PPI) class, such as omeprazole or esomeprazole. Tegaserod functions by stimulating 5-HT4 receptors in the gastrointestinal tract, which promotes the release of neurotransmitters that enhance the peristaltic reflex and increase intestinal secretion, thereby improving motility. PPIs work by irreversibly inhibiting the H+/K+-ATPase enzyme system (the proton pump) in gastric parietal cells, which suppresses the final step of gastric acid production. This combination regimen has been investigated in clinical research for patients with gastroesophageal reflux disease (GERD) who remain symptomatic despite PPI monotherapy, as well as for functional dyspepsia, aiming to address both acid hypersensitivity and impaired gastric motility. While tegaserod (Zelnorm) was originally developed by Novartis and faced regulatory challenges including a temporary market withdrawal due to cardiovascular safety concerns, it remains a subject of study in combination with acid-suppressive therapies for refractory motility-related disorders.

Other names
tegaserod and PPItegaserod plus PPItegaserod + PPI
02

Targets

HTR4 (5-Hydroxytryptamine receptor 4)HTR2A (Serotonin receptor 5-HT2A)HTR2C (5-hydroxytryptamine 2C receptor)ATP4A (Potassium–transporting ATPase alpha chain 1)HTR2B (5-Hydroxytryptamine Receptor 2B)

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