Drug intelligence / Profile preview

tegaserod

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

Overview

Tegaserod is a small molecule drug classified as a serotonin-4 (5-HT4) receptor agonist. It is primarily indicated for the treatment of irritable bowel syndrome with constipation (IBS-C) in women under 65 years of age. Tegaserod works by activating 5-HT4 receptors located presynaptically on cholinergic neurons in the gastrointestinal tract, which stimulates acetylcholine release, leading to increased gastrointestinal motility and improved visceral sensation. This results in accelerated bowel transit and relief from symptoms such as abdominal pain, bloating, and constipation. Originally developed by Novartis and marketed under the brand name Zelnorm, it was withdrawn from the US market in 2007 due to concerns about cardiovascular risks but was reintroduced with restricted indications for lower-risk populations in 2019[1][3][7].

Brand names
Zelnorm
Other names
tegaserod maleate
02

Targets

NET (Norepinephrine Transporter)SERT (Sodium-dependent serotonin transporter)DAT (Dopamine plasma membrane transport protein)HTR4 (5-Hydroxytryptamine receptor 4)

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