Alosetron is a 5-HT3 antagonist used to treat diarrhea-predominant IBS. Alosetron was voluntarily withdrawn from the US market in November 2000 by the manufacturer due to numerous reports of severe adverse effects including ischemic colitis, severely obstructed or ruptured bowel, and death.
- Mechanism
- Curator reviewed
Alosetron is a potent and selective 5-HT3 receptor antagonist. 5-HT3 receptors are nonselective cation channels that are extensively distributed on enteric neurons in the human gastrointestinal tract, as well as other peripheral and central locations. Activation of these channels and the resulting neuronal depolarization affect the regulation of visceral pain, colonic transit and gastrointestinal secretions, processes that relate to the pathophysiology of irritable bowel syndrome (IBS). 5-HT3 receptor antagonists such as alosetron inhibit activation of non-selective cation channels which results in the modulation of serotonin-sensitive GI motor and sensory processes.
- Primary indication
- Only for the treatment of symptoms of severe diarrhea-predominant irritable bowel syndrome (IBS) in women with chronic symptoms (generally lasting greater than 6 months) who does not present with anatomic or biochemical GI abnormalities and...Curator reviewed · 1 structured indication
- Formula / weight
- C17H18N4O · 294.351 g/mol (avg)
- First approval
- United States, 2000
- Code names
- GR 68755
- Brand names
Resolves to
JSWZEAMFRNKZNL-UHFFFAOYSA-NSMILESCN1C2=C(C3=CC=CC=C13)C(=O)N(CC1=C(C)NC=N1)CC2What you can answer from here — as of September 23, 2026
Which drugs share a target with Alosetron, and which of those have an active Phase 3 trial?
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