NK-1R Inhibitors
1 drugsAbout NK-1R
The neurokinin-1 receptor (NK-1R) is a GPCR activated by substance P, mediating pain, emesis, and mood regulation. It triggers intracellular signaling cascades involved in these processes, making it a therapeutic target.
NK-1R has been explored as a therapeutic target for various conditions, but there is currently no genetic evidence data available linking NK-1R to specific diseases. The existence of AKYNZEO demonstrates the clinical viability of NK-1R modulation.
NK-1R is targeted by one FDA-approved drug, AKYNZEO (aprepitant), a small molecule developed by HELSINN HLTHCARE. AKYNZEO was first approved in 2014 and has two indications in the 'other' therapeutic area.
Strategic Insights
ℹ️ How we calculate- White space opportunity in Breast Carcinoma with only 1 trials.
Human Genetic Evidence Moderate
There is no genetic evidence data available for NK-1R.
Absence of genetic support suggests higher risk in clinical development; consider biomarker strategies.
Evidence Across Diseases
9 totalGWAS and other genetic studies link TACR1 to 9 diseases.
🔗 Colocalization Evidence 3 strong
max H4: 0.99eQTL/pQTL signals for TACR1 colocalize with these GWAS traits, providing causal evidence that gene expression changes drive disease risk.
Understanding these scores
Association Score (0-1): Combines all evidence types (genetic, literature, drugs, animal models). Higher = more evidence linking target to disease. This is a ranking heuristic, not a confidence score.
L2G Score: Open Targets uses a machine learning model (Locus-to-Gene) to predict which gene is causal at each GWAS locus. L2G=0.5 means ~50% probability of being the causal gene. Only associations with L2G > 0.05 are included.
Odds Ratio (OR): From gene burden studies (UK Biobank, AstraZeneca PheWAS). Measures how loss-of-function variants affect disease risk. OR<1 = protective (inhibiting target may help), OR>1 = risk (losing function causes disease).
Beta (β): Effect size for continuous traits. β<0 = protective, β>0 = risk.
Clinical Translation (~1.8x): Based on Nelson et al. 2015: drug targets with genetic evidence have ~2x higher success rates in clinical trials. We estimate: Strong support (score ≥0.7) → ~1.8x, Moderate (0.3-0.7) → ~1.3x, Weak → baseline.
Colocalization (H4): Tests whether a GWAS signal and an eQTL/pQTL signal share the same causal variant. H4 is the posterior probability that both traits are associated AND share a causal variant. H4 > 0.8 = strong evidence that gene expression/protein levels drive disease risk. This links genetic variation → gene expression → disease, supporting the target-disease connection.
Top Drugs
HELSINN HLTHCARE is the only company with an approved NK-1R targeting drug.
Low competition suggests a potential market entry opportunity, but also indicates higher risk.
Drug Modality Landscape
Modalities
Routes of Administration
Only one approved drug targets NK-1R, using small molecule modality.
The lack of diverse modalities represents a whitespace opportunity for novel biologics targeting NK-1R.
Clinical Trials 33 trials
Completion by Phase
| Phase | Total | Completed | Failed | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 11 | 9 | 1 | 1 | 90% |
| Phase 2 | 7 | 5 | 1 | 1 | 83% |
| Phase 3 | 9 | 9 | 0 | 0 | 100% |
| Phase 4 | 6 | 3 | 1 | 2 | 75% |
Top Sponsors
By Modality
Top Conditions
Top Drugs
Drug Approval Timeline (2014 - 2014)
The first and only drug, AKYNZEO, was approved in 2014.
A single approval nearly a decade ago suggests market saturation or challenges in NK-1R drug development.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 1 companies competing
- • Market share by company
Full Drug Portfolio
- • All 1 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 1-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Competition: High (15 sponsors)
- • White space: 10 underexplored indications
- • Success rates by condition
Full summary • All drugs • Genetic evidence • Trials • Timeline
How We Calculate These Metrics
Target Attractiveness Score
A 0-100 score based on trial activity, sponsor diversity, and completion rates. Calculated from 22 clinical trials targeting NK-1R.
Completion rate: Percentage of trials that reached their planned endpoint. Trials terminated early, withdrawn, or suspended are not counted—these often indicate safety issues, lack of efficacy, or strategic pivots.
- Highly Attractive (80+): High trial activity, many sponsors, strong completion rates
- Attractive (60-79): Good trial activity and validation
- Moderate (40-59): Moderate interest from sponsors
- Low (under 40): Limited trial activity or validation concerns
Strategic Insights
Auto-generated insights based on trial analytics including competition intensity, white space opportunities, modality shifts, and failure patterns. We analyze trial sponsors, phases, indications, and outcomes.
Risk Signals
- High Competition: Many sponsors competing for this target (may reduce market opportunity)
- High Failure Risk: Low trial completion rates suggest development challenges
- Low Validation: Limited trial activity or poor outcomes indicate uncertain viability
- White Space Available: Underexplored indications present opportunities