Drug intelligence / Profile preview

aprepitant + ramosetron + dexamethasone

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

Overview

The combination of aprepitant, ramosetron, and dexamethasone is used primarily for the prevention of chemotherapy-induced nausea and vomiting (CINV), especially in patients receiving highly emetogenic chemotherapy regimens such as those containing cisplatin or paclitaxel/carboplatin. Aprepitant is a substance P/neurokinin 1 (NK1) receptor antagonist that blocks signals in the brain responsible for nausea and vomiting. Ramosetron is a selective serotonin 5-HT3 receptor antagonist that inhibits serotonin-mediated emetic signaling in the gastrointestinal tract and central nervous system. Dexamethasone is a synthetic glucocorticoid corticosteroid with anti-inflammatory and antiemetic properties, though its precise mechanism in CINV prevention is not fully understood. This triple-drug regimen has demonstrated efficacy in both acute and delayed phases of CINV, with high rates of complete response reported across multiple cycles of chemotherapy[2][1][5]. The combination is widely used clinically, particularly in Asian countries.

Brand names
None
Other names
RAD regimenaprepitant/ramosetron/dexamethasone
02

Targets

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

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