Drug intelligence / Profile preview

palonosetron + dexamethasone

Development stage
Unknown
Lead developer
Helsinn
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intravenous, Oral
01

Overview

Palonosetron + dexamethasone is a combination regimen used primarily for the prevention of acute and delayed chemotherapy-induced nausea and vomiting (CINV). Palonosetron is a selective serotonin 5-HT3 receptor antagonist that blocks serotonin both peripherally on vagal nerve terminals in the gastrointestinal tract and centrally in the chemoreceptor trigger zone of the area postrema, thereby inhibiting emetic signaling. It has high affinity for 5-HT3 receptors, unique allosteric binding properties, induces receptor internalization, and inhibits cross-talk between 5-HT3 and NK-1 pathways. Dexamethasone is a synthetic glucocorticoid corticosteroid with anti-inflammatory and antiemetic effects; its addition to palonosetron enhances efficacy against CINV. This combination is widely used as standard supportive care in patients receiving moderately or highly emetogenic chemotherapy[2][4][5][6].

Brand names
Akynzeo
Other names
palonosetron hydrochloridedexamethasone sodium phosphateRS-25259-197RS25259-197RS 25259-197
02

Targets

HTR3A (5-hydroxytryptamine receptor 3A)GR (Glucocorticoid receptor)

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