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fosnetupitant

Development stage
Phase 2
Lead developer
Helsinn
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

Fosnetupitant is a phosphorylated prodrug of netupitant, developed as an intravenous medication for the prevention of chemotherapy-induced nausea and vomiting (CINV). It is typically administered in combination with palonosetron and dexamethasone. Fosnetupitant acts as a highly selective neurokinin 1 (NK1) receptor antagonist; after administration, it is rapidly converted to netupitant, which blocks substance P from binding to NK1 receptors in the central nervous system. This mechanism inhibits both acute and delayed phases of CINV by preventing activation of pathways involved in emesis. The drug was approved by regulatory agencies such as the FDA (2018) and Japanese authorities (2022), and is considered a standard antiemetic for patients receiving highly or moderately emetogenic chemotherapy[3][5][6][7].

Brand names
Akynzeo
Other names
fosnetupitant chloride hydrochloride
02

Targets

TACR1 (Neurokinin‑1 Receptor)

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