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fosaprepitant + 5-HT3 receptor antagonist + dexamethasone

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

Overview

**This combination drug is used as an antiemetic regimen for the prevention of acute and delayed nausea and vomiting associated with highly emetogenic chemotherapy (HEC).** It contains: - **Fosaprepitant:** a water-soluble intravenous prodrug of aprepitant, a neurokinin-1 (NK1) receptor antagonist. - **5-HT3 receptor antagonist:** typically ondansetron, granisetron, or palonosetron, which inhibit serotonin (5-HT3) receptors involved in emetic signaling in the gut and central nervous system. - **Dexamethasone:** a synthetic glucocorticoid with anti-inflammatory and antiemetic properties, which also enhances the efficacy of the antiemetic regimen. **Mechanism of action:** - Fosaprepitant blocks NK1 receptors, preventing substance P-mediated emesis. - 5-HT3 receptor antagonists block serotonin-mediated emesis at peripheral and central sites. - Dexamethasone modulates inflammation and nausea through multiple pathways, with partially unclear antiemetic mechanisms. The combination is **standard of care for antiemetic prophylaxis in patients receiving highly emetogenic chemotherapy**, such as cisplatin, and has been shown in multiple studies to significantly improve rates of complete response (no vomiting or rescue therapy) compared to doublet therapy without NK1 antagonists[1][4].

Other names
triple antiemetic therapy for HECtriplet antiemetic regimen for chemotherapy
02

Targets

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

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