Drug intelligence / Profile preview

dexamethasone + netupitant + palonosetron

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

Overview

This is a three-drug antiemetic regimen consisting of dexamethasone, netupitant, and palonosetron. It is used primarily for the prevention of acute and delayed nausea and vomiting associated with cancer chemotherapy. Netupitant is a selective neurokinin-1 (NK-1) receptor antagonist that blocks substance P-mediated emetic signaling in the central nervous system, targeting delayed-phase emesis. Palonosetron is a serotonin 5-HT3 receptor antagonist that prevents acute-phase nausea and vomiting by blocking serotonin-mediated signals in the gastrointestinal tract and brain. Dexamethasone, a corticosteroid, enhances antiemetic efficacy through multiple mechanisms including anti-inflammatory effects; it is co-administered as part of guideline-recommended regimens for highly or moderately emetogenic chemotherapy[1][2][4]. The fixed-dose combination of netupitant plus palonosetron (marketed as Akynzeo) simplifies dosing to one capsule or infusion on day 1 of chemotherapy, with dexamethasone administered orally according to protocol[4]. This triple regimen has demonstrated superior efficacy compared to older combinations in clinical trials for both acute and delayed phases of chemotherapy-induced nausea and vomiting (CINV)[3].

Brand names
Akynzeo plus dexamethasone
Other names
NEPA
02

Targets

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

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