Drug intelligence / Profile preview

fosrolapitant + palonosetron hydrochloride + dexamethasone acetate

Development stage
Unknown
Lead developer
Hengrui Pharmaceutical
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

Fosrolapitant + palonosetron hydrochloride + dexamethasone acetate is a triple-combination antiemetic regimen developed for the prevention of chemotherapy-induced nausea and vomiting (CINV). The regimen consists of HR20013—a fixed-dose intravenous combination of fosrolapitant (a prodrug of the neurokinin-1/NK1 receptor antagonist rolapitant) and palonosetron hydrochloride (a selective 5-HT3 receptor antagonist)—administered alongside the corticosteroid dexamethasone acetate. By simultaneously antagonizing NK1 and 5-HT3 receptors and activating glucocorticoid receptors, this combination targets multiple emetic pathways to prevent both acute and delayed phases of nausea and vomiting. It is primarily being evaluated in patients receiving highly or moderately emetogenic chemotherapy, including those with esophageal and lung cancer.

Other names
Fosrolapitant and Palonosetron Hydrochloride for Injection combined with dexamethasone acetate
02

Targets

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

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