# Dolasetron

Source: https://onco.cc/drugs/dolasetron/  
OnCo record `dolasetron` (Treatment). Data CC BY-NC 4.0, attribute "Data from OnCo (onco.cc)"; commercial use needs a licence.

## TL;DR

Dolasetron is one of the serotonin-blocking antiemetics that transformed chemotherapy in the 1990s, approved in 1997 to prevent nausea and vomiting; its intravenous form lost its chemotherapy indication in 2010 because of heart rhythm effects.

## Summary

Dolasetron, approved by the FDA in September 1997, joined ondansetron and granisetron as a first-generation 5-HT3 antagonist for prevention of nausea and vomiting from moderately emetogenic chemotherapy and after surgery. It is a prodrug converted to hydrodolasetron. In 2010 the FDA contraindicated the intravenous form for chemotherapy-induced nausea because of dose-dependent QT prolongation and arrhythmias, leaving the tablets. Guidelines treat the first-generation agents as interchangeable for acute emesis, with palonosetron preferred for delayed emesis and NK1 antagonists and olanzapine added for highly emetogenic regimens.

## Fields

- Kind: Treatment
- Status: established
- Last checked: 2026-09-08
- Also known as: Dolasetron mesylate
- Tags: gap-fill; chembl-universe
- Brand: Anzemet
- Modality: Oral 5-HT3 receptor antagonist antiemetic
- Mechanism: Blocks 5-HT3 serotonin receptors on vagal nerve endings in the gut and in the brainstem, cutting the signal that chemotherapy-released serotonin sends to the vomiting centre.
- Approvals: US 1997: Prevention of nausea and vomiting from moderately emetogenic chemotherapy (oral); intravenous chemotherapy indication removed in 2010

## Sources

- Wikipedia: https://en.wikipedia.org/wiki/Dolasetron
- Label (DailyMed): https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=dolasetron
- Wikipedia: https://en.wikipedia.org/wiki/Dolasetron
- ChEMBL CHEMBL1200880: https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1200880

## Connected records

- targets: [5-HT3 receptor (HTR3A)](https://onco.cc/targets/htr3a/)
- drugs: [Granisetron](https://onco.cc/drugs/granisetron/), [Ondansetron](https://onco.cc/drugs/ondansetron/), [Palonosetron](https://onco.cc/drugs/palonosetron/)

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JSON: https://onco.cc/api/v1/entities/dolasetron.json