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NK-1R antagonist
NK-1R antagonists block neurokinin-1 receptors to inhibit substance P signaling, reducing nausea, vomiting, and pain perception.
NK-1R antagonists block neurokinin-1 receptors to inhibit substance P signaling, reducing nausea, vomiting, and pain perception. Used for Chemotherapy-induced nausea and vomiting (CINV), Post-operative nausea and vomiting (PONV).
At a glance
| Generic name | NK-1R antagonist |
|---|---|
| Sponsor | Prof. Dr. Fridoon Jawad Ahmad |
| Drug class | NK-1 receptor antagonist |
| Target | NK-1R (Neurokinin-1 receptor) |
| Modality | Small molecule |
| Therapeutic area | Oncology, Gastroenterology, Pain Management |
| Phase | Phase 3 |
Mechanism of action
NK-1 receptor antagonists competitively bind to neurokinin-1 receptors in the central and peripheral nervous system, blocking the neuropeptide substance P. This mechanism is particularly effective for chemotherapy-induced nausea and vomiting (CINV) and may have analgesic and anxiolytic properties through modulation of pain and emotional processing pathways.
Approved indications
- Chemotherapy-induced nausea and vomiting (CINV)
- Post-operative nausea and vomiting (PONV)
Common side effects
- Headache
- Fatigue
- Constipation
- Dizziness
Key clinical trials
- A Clinical Study of Ifinatamab Deruxtecan (I-DXd) in People With Metastatic Prostate Cancer (MK-2400-001) (PHASE3)
- A Clinical Study of Raludotatug Deruxtecan in People With Ovarian Cancer (MK-5909-003) (PHASE1, PHASE2)
- A Clinical Study of Ifinatamab Deruxtecan Based Treatment Combinations or as Monotherapy to Treat Metastatic Castrate Resistant Prostate Cancer (mCRPC) (MK-2400-01A/IDeate-Prostate02) (PHASE1, PHASE2)
- A Study of Investigational Agents in Participants With Previously Treated Stage IV Nonsquamous Non-small Cell Lung Cancer (NSCLC) (MK-3475-01H/KEYMAKER-U01) (PHASE2)
- A Clinical Study of Gocatamig (MK-6070) and Infinatamab Deruxtecan (MK-2400) in People With Small Cell Lung Cancer (MK-6070-003) (PHASE1, PHASE2)
- A Study to Evaluate LY3537021 for the Treatment of Nausea and Vomiting Caused by Chemotherapy in Adults With Cancer (PHASE2)
- Substudy 06D: Combination Therapies in Second Line (2L) Gastroesophageal Adenocarcinoma (MK-3475-06D/Keymaker-U06) (PHASE1, PHASE2)
- Substudy 06E: Umbrella Study of Combination Therapies in Esophageal Cancer (MK-3475-06E/KEYMAKER-U06) (PHASE1, PHASE2)
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:
- NK-1R antagonist CI brief — competitive landscape report
- NK-1R antagonist updates RSS · CI watch RSS
- Prof. Dr. Fridoon Jawad Ahmad portfolio CI