Drug intelligence / Profile preview

palonosetron + dexamethasone + fosaprepitant

Development stage
Unknown
Lead developer
The Sixth Affiliated Hospital of Sun Yat-Sen University
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

This triple-combination antiemetic therapy consists of fosaprepitant (150 mg), palonosetron (0.075 mg), and dexamethasone (5 mg). It is being investigated by the Sixth Affiliated Hospital of Sun Yat-sen University for the prevention of postoperative nausea and vomiting (PONV) in high-risk patients, particularly those undergoing laparoscopic gastrointestinal surgery. The regimen utilizes three distinct mechanisms of action: fosaprepitant acts as a neurokinin-1 (NK-1) receptor antagonist, palonosetron is a second-generation 5-HT3 receptor antagonist, and dexamethasone is a corticosteroid that functions as a glucocorticoid receptor agonist. A Phase 3 randomized, double-blind trial demonstrated that this triple therapy significantly reduced the incidence of PONV during the first 24 postoperative hours compared to dual therapy with palonosetron and dexamethasone alone.

Other names
Fosaprepitant Triple Therapy
02

Targets

TACR1 (Neurokinin‑1 Receptor)GR (Glucocorticoid receptor)HTR3A (5-hydroxytryptamine receptor 3A)

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