drugsTreatmentEstablished

Dolasetron

aka Dolasetron mesylate

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.

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.

See it in action

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. Connects to 5-HT3 receptor (HTR3A).

1. What happens next: the small molecule schematic

How supportive care & survivorship works, step by step · animated schematic, not to scale; chosen from the modality "Oral 5-HT3 receptor antagonist antiemetic"

Supportive Care & Survivorship →

2. Step by step

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1.Dolasetron slips into a pocket on 5-HT3 receptor (HTR3A).

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.

Brand / code

Anzemet

Regulatory

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Approvals

Region	Year	Indication
US	1997	Prevention of nausea and vomiting from moderately emetogenic chemotherapy (oral); intravenous chemotherapy indication removed in 2010

Trials

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Dolasetron

intervention: Dolasetron

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