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Comparator: MK0517
MK0517 is a selective antagonist of the neurokinin-1 (NK1) receptor that blocks substance P signaling in the central nervous system.
MK0517 is a selective antagonist of the neurokinin-1 (NK1) receptor that blocks substance P signaling in the central nervous system. Used for Chemotherapy-induced nausea and vomiting (CINV).
At a glance
| Generic name | Comparator: MK0517 |
|---|---|
| Sponsor | Merck Sharp & Dohme LLC |
| Drug class | Neurokinin-1 (NK1) receptor antagonist |
| Target | NK1 receptor |
| Modality | Small molecule |
| Therapeutic area | Oncology; Gastroenterology |
| Phase | Phase 3 |
Mechanism of action
MK0517 crosses the blood-brain barrier and competitively binds to NK1 receptors, preventing substance P from activating these receptors. Substance P is a neuropeptide involved in pain transmission and emetic signaling, so NK1 antagonism is hypothesized to reduce chemotherapy-induced nausea and vomiting (CINV) and potentially treat other conditions involving pain or mood dysregulation.
Approved indications
- Chemotherapy-induced nausea and vomiting (CINV)
Common side effects
- Headache
- Fatigue
- Constipation
- Diarrhea
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 the Safety and Efficacy of Aprepitant for the Prevention of Chemotherapy-Induced Nausea and Vomiting (CINV) in Pediatric Participants (MK-0869-208) (PHASE3)
- A Study to Evaluate Aprepitant for the Prevention of Post-Operative Nausea and Vomiting in Children (MK-0869-219) (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/MK0869 for Prevention of Chemotherapy Induced Nausea and Vomiting Associated With Cisplatin (0869-169)(COMPLETED) (PHASE3)
- Aprepitant for the Prevention of Chemotherapy Induced Nausea and Vomiting (CINV)(0869-130)(COMPLETED) (PHASE3)
- 2 Doses of an Approved Drug Being Studied for a New Indication for the Prevention of Postoperative Nausea and Vomiting (0869-091) (PHASE3)
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: MK0517 CI brief — competitive landscape report
- Comparator: MK0517 updates RSS · CI watch RSS
- Merck Sharp & Dohme LLC portfolio CI