Drug intelligence / Profile preview

tegaserod + omeprazole

Development stage
Phase 2
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

**Tegaserod + omeprazole** is an unbranded, non-standard combination therapy composed of two well-characterized drugs: **tegaserod**, a selective serotonin type-4 (5-HT4) receptor agonist used to stimulate gastrointestinal motility, and **omeprazole**, a proton pump inhibitor (PPI) that suppresses gastric acid secretion. Tegaserod mainly acts by activating 5-HT4 receptors to increase peristalsis and reduce visceral sensitivity, beneficial for conditions with impaired gut motility. Omeprazole irreversibly inhibits the H+/K+ ATPase in gastric parietal cells, reducing acid secretion and alleviating symptoms of acid reflux and dyspepsia. The combination has been trialed for functional dyspepsia and gastroesophageal reflux disease (GERD) in patients with chronic constipation, where it demonstrated efficacy and safety, with superior symptom relief compared to esomeprazole alone or either drug alone. There is no commercial product with this exact composition; use in studies is investigational[3][4].

02

Targets

HTR2A (Serotonin receptor 5-HT2A)HTR2B (5-Hydroxytryptamine Receptor 2B)HTR2C (5-hydroxytryptamine 2C receptor)HTR4 (5-Hydroxytryptamine receptor 4)ATP4A (Potassium–transporting ATPase alpha chain 1)MAOA (Monoamine oxidase A)TPH1 (Tryptophan 5-hydroxylase 1)TPH2 (Tryptophan hydroxylase 2)

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