Drug intelligence / Profile preview

netupitant + olanzapine + palonosetron

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

Overview

This is a combination therapy primarily used for preventing chemotherapy-induced nausea and vomiting (CINV). It comprises three distinct medications: netupitant, a neurokinin 1 (NK1) receptor antagonist that blocks neurokinin, with an elimination half-life of approximately 88 hours; palonosetron, a second-generation 5-HT3 receptor antagonist that blocks serotonin, with a longer elimination half-life (44-50 hours) compared to older 5-HT3 antagonists; and olanzapine, an atypical antipsychotic found effective in controlling CINV when combined with other antiemetics. Each component works through different mechanisms to provide comprehensive control of both acute (0-24 hours) and delayed (24-120 hours) phases of CINV.

Other names
olanzapine + netupitant + palonosetron regimendexamethasone-free antiemetic regimen
02

Targets

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

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