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fosaprepitant + 5-hydroxytryptamine 3 antagonist
- Development stage
- Unknown
- Lead developer
- Merck
- Modality
- Small Molecules
- Administration
- Intravenous
01
Overview
Fosaprepitant + 5-hydroxytryptamine 3 (5-HT3) antagonist is a combination therapy used in the prevention of acute and delayed chemotherapy-induced nausea and vomiting (CINV). Fosaprepitant is a prodrug of aprepitant and acts as a neurokinin 1 (NK1) receptor antagonist, inhibiting the action of substance P at NK1 receptors. 5-HT3 antagonists (such as ondansetron or granisetron) block serotonin's (5-HT) action at 5-HT3 receptors, particularly in the gastrointestinal tract and the chemoreceptor trigger zone. This combination targets two key emetogenic pathways and is recommended, often with dexamethasone, for high emetogenic chemotherapy in pediatric and adult patients. The combination is more effective for preventing vomiting compared to 5-HT3 antagonist therapy alone and maintains a similar safety profile[1][3][7].
- Other names
- fosaprepitant plus 5-HT3 receptor antagonist
02
Targets
TACR1 (Neurokinin‑1 Receptor)HTR3A (5-hydroxytryptamine receptor 3A)
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