Drug intelligence / Profile preview

aprepitant + granisetron + dexamethasone

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

Overview

Aprepitant + granisetron + dexamethasone is a three-drug combination regimen used primarily for the prevention of chemotherapy-induced nausea and vomiting (CINV), especially in patients receiving highly emetogenic chemotherapy. - **Aprepitant** is a selective high-affinity antagonist of the human substance P/neurokinin 1 (NK1) receptor, blocking signals that trigger nausea and vomiting[6][7]. - **Granisetron** is a selective serotonin (5-HT3) receptor antagonist, inhibiting serotonin-mediated emetic signaling in the gut and central nervous system[2]. - **Dexamethasone** is a synthetic glucocorticoid corticosteroid with anti-inflammatory and antiemetic properties; its precise mechanism in CINV prophylaxis remains unclear but may involve inhibition of prostaglandin synthesis or reduction of inflammation[2][3]. This triple regimen targets multiple pathways involved in CINV, providing superior protection against both acute (within 24 hours) and delayed (24–120 hours) phases compared to two-drug regimens. It has demonstrated efficacy across various cancer types, including gastric cancer and hematologic malignancies undergoing high-dose chemotherapy[1][4].

02

Targets

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

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