Drug intelligence / Profile preview

aprepitant + ondansetron

Development stage
Phase 4
Lead developer
Merck
Modality
Small Molecules
Administration
Oral, Intravenous, Intramuscular
01

Overview

Aprepitant + ondansetron is a fixed-dose combination of two antiemetic agents used together to prevent and treat nausea and vomiting, particularly those induced by cancer chemotherapy, radiation therapy, or surgery. Aprepitant is a selective high-affinity antagonist of the human substance P/neurokinin 1 (NK1) receptor, blocking the action of substance P in the central nervous system to prevent both acute and delayed emesis. Ondansetron is a selective serotonin 5-HT3 receptor antagonist that blocks serotonin both peripherally on vagal nerve terminals and centrally in the chemoreceptor trigger zone. The combination has demonstrated superior efficacy compared to monotherapy with either agent for preventing radiation-induced or chemotherapy-induced nausea and vomiting[4][6][8].

02

Targets

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

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