Drug intelligence / Profile preview

rolapitant + palonosetron

Development stage
Phase 3
Lead developer
Hengrui Pharmaceutical
Modality
Small Molecules
Administration
Intravenous
01

Overview

Rolapitant + palonosetron is a fixed-dose combination antiemetic therapy consisting of rolapitant (a neurokinin-1 [NK1] receptor antagonist) and palonosetron (a 5-HT3 receptor antagonist). Rolapitant prevents nausea and vomiting by blocking the binding of substance P to NK1 receptors in the central nervous system, which is particularly effective for the delayed phase of emesis. Palonosetron is a second-generation 5-HT3 receptor antagonist with a long half-life and high binding affinity, primarily targeting the acute phase of emesis. This combination, often administered as an intravenous injection (sometimes using the prodrug fosrolapitant), is being evaluated by Henan Cancer Hospital for the prevention of nausea and vomiting in lung cancer patients undergoing concurrent chemoradiotherapy. The specific regimen studied often includes dexamethasone and olanzapine to optimize antiemetic control.

Other names
Rolapitant Palonosetron injectionFosrolapitant + PalonosetronRolapitant Palonosetron
02

Targets

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

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