Drug intelligence / Profile preview

aprepitant + granisetron

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

Overview

Aprepitant + granisetron is a combination of two antiemetic drugs used primarily for the prevention of chemotherapy-induced nausea and vomiting (CINV). Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors, which blocks the action of substance P, a neuropeptide associated with emesis. Granisetron is a selective serotonin 5-HT3 receptor antagonist that inhibits serotonin-mediated signaling in both the central nervous system and gastrointestinal tract, thereby preventing nausea and vomiting. This combination is often used alongside dexamethasone as part of multi-drug regimens to enhance antiemetic efficacy in patients receiving highly or moderately emetogenic chemotherapy[1][4][6][8].

02

Targets

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

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