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Comparator: fosaprepitant dimeglumine
Fosaprepitant dimeglumine is a neurokinin-1 (NK1) receptor antagonist that blocks substance P signaling in the chemoreceptor trigger zone and vomiting center to prevent chemotherapy-induced nausea and vomiting.
Fosaprepitant dimeglumine is a neurokinin-1 (NK1) receptor antagonist that blocks substance P signaling in the chemoreceptor trigger zone and vomiting center to prevent chemotherapy-induced nausea and vomiting. Used for Prevention of acute and delayed chemotherapy-induced nausea and vomiting (CINV) in patients receiving highly emetogenic chemotherapy, Prevention of postoperative nausea and vomiting (PONV).
At a glance
| Generic name | Comparator: fosaprepitant dimeglumine |
|---|---|
| Also known as | EMEND® |
| Sponsor | Merck Sharp & Dohme LLC |
| Drug class | NK1 receptor antagonist |
| Target | NK1 receptor (neurokinin-1 receptor) |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | Phase 3 |
Mechanism of action
Fosaprepitant is a prodrug that is rapidly converted to aprepitant, which crosses the blood-brain barrier and competitively antagonizes NK1 receptors. Substance P is a key neurotransmitter involved in nausea and vomiting pathways, particularly in response to chemotherapy. By blocking NK1 receptors, fosaprepitant prevents the emetic signal cascade, providing antiemetic protection especially for highly emetogenic chemotherapy regimens.
Approved indications
- Prevention of acute and delayed chemotherapy-induced nausea and vomiting (CINV) in patients receiving highly emetogenic chemotherapy
- Prevention of postoperative nausea and vomiting (PONV)
Common side effects
- Fatigue
- Headache
- Constipation
- Diarrhea
- Hiccups
- Dizziness
Key clinical trials
- Study of the Pharmacokinetics, Pharmacodynamics, Safety and Tolerability of Fosaprepitant for the Prevention of Chemotherapy-Induced Nausea and Vomiting (CINV) in Children (MK-0517-029) (PHASE2)
- A Study of MK-0869 (Aprepitant) and MK-0517 (Fosaprepitant) in Pediatric Participants Receiving Chemotherapy (MK-0869-134) (PHASE1)
- Efficacy and Safety of Fosaprepitant Dimeglumine in Preventing Chemotherapy-Induced Nausea and Vomiting (MK-0517-031) (PHASE3)
- Aprepitant for the Prevention of Chemotherapy Induced Nausea and Vomiting (CINV)(0869-130)(COMPLETED) (PHASE3)
- Evaluation of Fosaprepitant (MK0517) in Single Dose Schedule (0517-017) (PHASE3)
- A Study to Assess the Bioequivalence of Aprepitant and Fosaprepitant and the Effect of Food on Aprepitant Bioavailability (0869-165) (PHASE1)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Comparator: fosaprepitant dimeglumine CI brief — competitive landscape report
- Comparator: fosaprepitant dimeglumine updates RSS · CI watch RSS
- Merck Sharp & Dohme LLC portfolio CI