Drug intelligence / Profile preview

ondansetron + dexamethasone + aprepitant

Development stage
Unknown
Lead developer
Merck
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a fixed combination regimen of three drugs—ondansetron, dexamethasone, and aprepitant—used primarily for the prevention of chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV). 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. Dexamethasone is a synthetic glucocorticoid corticosteroid with anti-inflammatory and antiemetic properties. Aprepitant is a selective high-affinity antagonist of human substance P neurokinin 1 (NK1) receptors. The triple combination targets multiple emetogenic pathways to provide superior prophylaxis against acute and delayed phases of CINV compared to regimens without all three agents[3][4][5][7][8]. This regimen is recommended for patients receiving highly emetogenic chemotherapy or at high risk for PONV.

Brand names
ZofranEmendDecadron
Other names
Triple antiemetic regimenAprepitant regimenAntiemetic regimen
02

Targets

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

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