Drug intelligence / Profile preview

tropisetron

Development stage
Phase 4
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Tropisetron is a selective serotonin 5-HT3 receptor antagonist and indole derivative used primarily as an antiemetic to prevent nausea and vomiting associated with chemotherapy, radiotherapy, and surgery. It works by competitively blocking the action of serotonin at 5-HT3 receptors located peripherally on vagus nerve terminals in the gastrointestinal tract and centrally in the chemoreceptor trigger zone of the area postrema in the central nervous system. This inhibition suppresses emesis triggered by cytotoxic therapy or surgical procedures. Tropisetron also acts as a partial agonist at α7-nicotinic acetylcholine receptors, potentially modulating their activity[1][2][3][6]. The drug is generally well tolerated; headache is its most common side effect[2].

Brand names
NavobanSetrovelTropisetron MYX
Other names
tropisetron hydrochloride
02

Targets

HTR3A (5-hydroxytryptamine receptor 3A)CHRNA7 (α7 nicotinic receptor)

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