Kappa opioid receptor Agonists
2 drugsAbout Kappa opioid receptor
The Kappa-opioid receptor (KOR) is a G protein-coupled receptor involved in pain modulation and other physiological processes. Activation of KOR leads to diverse effects, making it a target for various therapeutic areas. The gene symbol for KOR is OPRK1.
Human genetics provide moderate support for KOR as a therapeutic target, with a max genetic score of 0.50. Genetic associations include placental retention (score 0.50) and smoking initiation (score 0.50).
KOR is targeted by 10 FDA-approved small molecule drugs, including KORSUVA, SYMPROIC, and BUPRENORPHINE. These drugs are developed by 9 companies, including BDSI, ALKEM LABS LTD, and VIFOR INTL, and address pain and other therapeutic needs.
Strategic Insights
ℹ️ How we calculate- White space opportunity in Pruritus with only 1 trials.
- phase2 represents biological uncertainty with 50% completion.
Human Genetic Evidence Moderate
Genetic evidence offers moderate support for KOR, with a max score of 0.50.
Further research is needed to validate KOR's role in genetically-supported indications.
Evidence Across Diseases
11 totalGWAS and other genetic studies link OPRK1 to 11 diseases.
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
Nine companies have approved drugs targeting KOR, with BDSI among the top players.
The presence of multiple players suggests a competitive market with moderate entry barriers.
Drug Modality Landscape
Modalities
Routes of Administration
Kappa opioid receptor is amenable to small molecule drugs, with oral options available for convenient dosing.
Exploring alternative modalities like antibodies or peptides may offer differentiation.
Clinical Trials 35 trials
Completion by Phase
| Phase | Total | Completed | Failed | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 10 | 9 | 0 | 1 | 100% |
| Phase 2 | 10 | 5 | 2 | 3 | 71% |
| Phase 3 | 10 | 8 | 0 | 1 | 100% |
| Phase 4 | 5 | 3 | 1 | 1 | 75% |
Top Sponsors
By Modality
Drug Approval Timeline (2015 - 2021)
The first KOR-targeting drug was approved in 2010 (BUTRANS), with the most recent in 2023 (BRIXADI).
The recent approval suggests continued interest, but market saturation should be considered.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 2 companies competing
- • Market share by company
Full Drug Portfolio
- • All 2 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 2-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 20 clinical trials targeting Kappa opioid receptor.
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