Drug intelligence / Profile preview

palonosetron + fosnetupitant + netupitant

Development stage
Approved
Lead developer
Helsinn
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

**palonosetron + fosnetupitant + netupitant** refers to the fixed antiemetic NEPA product family marketed as **Akynzeo**, which pairs the second-generation serotonin 3 receptor antagonist palonosetron with the neurokinin 1 receptor antagonist netupitant, or with its intravenous water-soluble prodrug fosnetupitant. It was developed by Helsinn for prevention of acute and delayed chemotherapy-induced nausea and vomiting, typically in combination with dexamethasone. Palonosetron blocks serotonin-mediated emetic signaling during the acute phase, while netupitant produced directly or via conversion from fosnetupitant blocks substance P signaling at neurokinin 1 receptors and extends control into the delayed phase. The marketed product exists as oral netupitant + palonosetron capsules and intravenous fosnetupitant + palonosetron injection; the input name is best understood as the umbrella combination spanning these closely linked NEPA formulations rather than a single discrete chemical entity containing both fosnetupitant and netupitant simultaneously in one dosage form.

Brand names
Akynzeo
Other names
netupitant + palonosetronfosnetupitant + palonosetronnetupitant/fosnetupitant + palonosetron
02

Targets

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

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