Granisetron is a 5HT3 antagonist used to treat nausea and vomiting in cancer therapy and postoperatively. A serotonin receptor (5HT-3 selective) antagonist that has been used as an antiemetic and antinauseant for cancer chemotherapy patients.
- Mechanism
- Curator reviewed
Granisetron is a potent, selective antagonist of 5-HT3 receptors. The antiemetic activity of the drug is brought about through the inhibition of 5-HT3 receptors present both centrally (medullary chemoreceptor zone) and peripherally (GI tract). This inhibition of 5-HT3 receptors in turn inhibits the visceral afferent stimulation of the vomiting center, likely indirectly at the level of the area postrema, as well as through direct inhibition of serotonin activity within the area postrema and the chemoreceptor trigger zone.
- Primary indication
- For the prevention of nausea and vomiting associated with initial and repeat courses of emetogenic cancer therapy (including high dose cisplatin), postoperation, and radiation (including total body irradiation and daily fractionated abdominal radiation).Curator reviewed · 4 structured indications
- Formula / weight
- C18H24N4O · 312.417 g/mol (avg)
- First approval
- Canada, 2001 · United States, 1993 · European Union, 2016
- Code names
- APF-530 · BRL-43694
- Brand names
Resolves to
MFWNKCLOYSRHCJ-BTTYYORXSA-NSMILESCN1N=C(C(=O)N[C@@H]2C[C@@H]3CCC[C@H](C2)N3C)C2=C1C=CC=C2What you can answer from here — as of September 23, 2026
Which drugs share a target with Granisetron, and which of those have an active Phase 3 trial?
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