Drug intelligence / Profile preview

fosaprepitant + palonosetron

Development stage
Unknown
Lead developer
Merck
Modality
Peptides, Small Molecules
Administration
Intravenous
01

Overview

Fosaprepitant + palonosetron is a fixed-dose combination of two antiemetic agents used primarily to prevent nausea and vomiting associated with cancer chemotherapy. Fosaprepitant is an intravenous prodrug of aprepitant, which acts as a neurokinin-1 (NK1) receptor antagonist by blocking the activity of substance P at NK1 receptors in the brain[3]. Palonosetron is a second-generation serotonin 5-HT3 receptor antagonist that prevents emesis by blocking serotonin binding to 5-HT3 receptors located on vagal nerve terminals in the gastrointestinal tract and centrally in the chemoreceptor trigger zone[2][6]. The combination provides synergistic efficacy for both acute and delayed chemotherapy-induced nausea and vomiting (CINV), often administered with dexamethasone for optimal effect[1][7].

02

Targets

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

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