Drug intelligence / Profile preview

aprepitant + palonosetron

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

Overview

Aprepitant + palonosetron is a combination regimen used to prevent chemotherapy-induced nausea and vomiting (CINV). Aprepitant is a neurokinin-1 (NK-1) receptor antagonist that blocks the action of substance P in the brain, thereby preventing both acute and delayed phases of CINV. Palonosetron is a serotonin 5-HT3 receptor antagonist that blocks serotonin receptors in the gastrointestinal tract and central nervous system, primarily preventing acute CINV. This combination may be administered alongside dexamethasone for optimal antiemetic efficacy. The regimen leverages the complementary mechanisms of both drugs to provide broad-spectrum protection against nausea and vomiting associated with cancer chemotherapy[6][7].

Brand names
Emend + Aloxi
Other names
aprepitant and palonosetronaprepitant with palonosetron
02

Targets

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

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