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Fosaprepitant for Injection
Fosaprepitant is an intravenous prodrug that is rapidly converted to aprepitant, a neurokinin-1 (NK1) receptor antagonist that blocks substance P signaling in the chemoreceptor trigger zone and vomiting center.
Fosaprepitant is an intravenous prodrug that is rapidly converted to aprepitant, a neurokinin-1 (NK1) receptor antagonist that blocks substance P signaling in the chemoreceptor trigger zone and vomiting center. Used for Prevention of acute and delayed nausea and vomiting associated with highly emetogenic cancer chemotherapy, Prevention of postoperative nausea and vomiting (PONV).
At a glance
| Generic name | Fosaprepitant for Injection |
|---|---|
| Sponsor | Montefiore Medical Center |
| Drug class | NK1 receptor antagonist |
| Target | NK1 receptor (neurokinin-1 receptor) |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | FDA-approved |
Mechanism of action
Fosaprepitant crosses the blood-brain barrier and is metabolized to aprepitant, which competitively antagonizes NK1 receptors. By blocking neurokinin-1 signaling, it prevents both the acute and delayed emetic responses triggered by chemotherapy. This mechanism is particularly effective for highly emetogenic chemotherapy regimens when combined with 5-HT3 antagonists and corticosteroids.
Approved indications
- Prevention of acute and delayed nausea and vomiting associated with highly emetogenic cancer chemotherapy
- Prevention of postoperative nausea and vomiting (PONV)
Common side effects
- Fatigue
- Headache
- Diarrhea
- Constipation
- Hiccups
- Infusion site reactions
Key clinical trials
- An Exploratory Study on Efficacy and Safety of Fosaprepitant and Palonosetron Hydrochloride for Injection in Preventing CINV From Multi-Agent HEC (PHASE4)
- To Evaluate the Efficacy and Safety of QLM2010 for Prevention of Chemotherapy-induced Nausea and Vomiting After Highly Emetogenic Chemotherapy. (PHASE3)
- Broadening Antiemetics Research by Comparing the Effectiveness of Fosaprepitant and Metoclopramide (PHASE4)
- Nanocrystalline Megestrol for Managing Chemotherapy-Induced Nausea and Vomiting (PHASE3)
- Electroacupuncture for the Prevention of Chemotherapy-induced Nausea and Vomiting in Patients With Breast Cancer (PHASE3)
- Triple Therapy of Dexamethasone, Palonosetron, and Fosaprepitant As PONV Prevention (NA)
- Safety of a Three-Day Fosaprepitant Regimen for the Prevention of Chemotherapy-Induced Nausea and Vomiting in Pediatric Participants (MK-0517-045) (PHASE4)
- An Relative Bioavailability Study of BH006 for Injection in Healthy Subjects (EARLY_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 |