Drug intelligence / Profile preview

palonosetron

Development stage
Approved
Lead developer
Helsinn
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

Palonosetron is a selective serotonin 5-HT3 receptor antagonist used primarily to prevent acute and delayed nausea and vomiting associated with moderately or highly emetogenic cancer chemotherapy and for the prevention of postoperative nausea and vomiting. It works by blocking the action of serotonin at 5-HT3 receptors located on vagal nerve terminals in the periphery and centrally in the chemoreceptor trigger zone of the area postrema. Palonosetron has a high affinity for these receptors but little to no affinity for other receptor types. It is considered more effective than earlier 5-HT3 antagonists in controlling delayed chemotherapy-induced nausea and vomiting, making it unique among its class[1][2][6]. The drug was developed as an advancement over previous antiemetics to address both immediate (within 24 hours) and delayed (after 24 hours) symptoms[2].

Brand names
AloxiAkynzeoPosfrea
Other names
palonosetron hydrochloride
02

Targets

HTR3A (5-hydroxytryptamine receptor 3A)

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