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MK0869, aprepitant
Aprepitant is a selective antagonist of neurokinin-1 (NK1) receptors that blocks substance P signaling in the chemoreceptor trigger zone and vomiting center of the brain.
Aprepitant is a selective antagonist of neurokinin-1 (NK1) receptors that blocks substance P signaling in the chemoreceptor trigger zone and vomiting center of the brain. Used for Chemotherapy-induced nausea and vomiting (CINV) prevention in patients receiving highly emetogenic chemotherapy, Post-operative nausea and vomiting (PONV) prevention.
At a glance
| Generic name | MK0869, aprepitant |
|---|---|
| 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
Aprepitant crosses the blood-brain barrier and competitively binds to NK1 receptors, preventing substance P from activating these receptors. Substance P is a key neurotransmitter involved in the emetic (vomiting) pathway, particularly in response to chemotherapy. By blocking NK1 receptors, aprepitant suppresses both acute and delayed chemotherapy-induced nausea and vomiting (CINV).
Approved indications
- Chemotherapy-induced nausea and vomiting (CINV) prevention in patients receiving highly emetogenic chemotherapy
- Post-operative nausea and vomiting (PONV) prevention
Common side effects
- Fatigue
- Constipation
- Diarrhea
- Headache
- Hiccups
Key clinical trials
- To Evaluate the Efficacy and Safety of QLM2010 for Prevention of Chemotherapy-induced Nausea and Vomiting After Highly Emetogenic Chemotherapy. (PHASE3)
- Aprepitant in the Management of Immune Checkpoint Inhibitors Pruritus in Solid Cancer Patients (PHASE1)
- Olanzapine With or Without Fosaprepitant Dimeglumine in Preventing Chemotherapy Induced Nausea and Vomiting in Cancer Patients Receiving Highly Emetogenic Chemotherapy (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)
- Aprepitant- and Olanzapine- Containing Anti-emetic Regimens With High Dose Melphalan (PHASE3)
- Comparison of Adding EMEND to PONV/PDNV Treatment Regimen (NA)
- 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 |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- MK0869, aprepitant CI brief — competitive landscape report
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- Merck Sharp & Dohme LLC portfolio CI