Dolasetron is an antinauseant and antiemetic used in chemotherapy and postoperatively. Dolasetron is a highly specific and selective serotonin 5-HT3 receptor antagonist.
- Mechanism
- Curator reviewed
Dolasetron is a selective serotonin 5-HT3 receptor antagonist. In vivo, the drug is rapidly converted into its major active metabolite, hydrodolasetron, which seems to be largely responsible for the drug's pharmacological activity. 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 emetogenic cancer chemotherapy, including initial and repeat courses of chemotherapy.Curator reviewed · 3 structured indications
- Formula / weight
- C19H20N2O3 · 324.38 g/mol (avg)
- First approval
- Canada, 2006 · United States, 1997
- Code names
- MDL 73147 EF
- Brand names
Resolves to
UKTAZPQNNNJVKR-KJGYPYNMSA-NSMILES[H][C@@]1(C[C@@]2([H])C[C@]3([H])C[C@@]([H])(C1)N2CC3=O)OC(=O)C1=CNC2=C1C=CC=C2What you can answer from here — as of September 30, 2026
Which drugs share a target with Dolasetron, and which of those have an active Phase 3 trial?
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