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fosaprepitant
- Development stage
- Approved
- Lead developer
- Merck
- Modality
- Small Molecules
- Administration
- Intravenous
01
Overview
Fosaprepitant is an intravenously administered antiemetic drug used in combination with other agents to prevent acute and delayed nausea and vomiting associated with initial and repeat courses of highly or moderately emetogenic cancer chemotherapy in adults and children aged 6 months or older. It is a prodrug of aprepitant, which means it is converted into aprepitant in the body. The mechanism of action involves selective antagonism of the human substance P/neurokinin 1 (NK1) receptor, thereby blocking the action of neurokinin—a natural substance in the brain that causes nausea and vomiting. Fosaprepitant augments the antiemetic activity of 5-HT3-receptor antagonists (like ondansetron) and corticosteroids (like dexamethasone), inhibiting both acute and delayed phases of chemotherapy-induced emesis[1][2][3][5][6].
- Brand names
- EmendFocinvez
- Other names
- fosaprepitant dimeglumine
02
Targets
TACR1 (Neurokinin‑1 Receptor)
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