Histamine H1 receptor Inhibitors
3 drugsAbout Histamine H1 receptor
The Histamine H1 receptor (HRH1) mediates histamine's effects, a signaling molecule involved in various physiological processes. Activation of HRH1 triggers downstream events contributing to inflammation, itching, and smooth muscle contraction.
Genetic evidence offers moderate support for HRH1 as a therapeutic target, with associations to cholelithiasis (score 0.46) and male infertility (score 0.45). Strong eQTL/pQTL signals further support HRH1's role in disease.
Three FDA-approved drugs target HRH1, including CARBINOXAMINE MALEATE, AZELASTINE HYDROCHLORIDE AND FLUTICASONE PROPIONATE, and DYMISTA. All three drugs are small molecules, addressing various conditions.
Strategic Insights
ℹ️ How we calculate- White space opportunity in Endometrial Cancer with only 1 trials.
Histamine H1 receptor Genetic Evidence Moderate
HRH1 has moderate genetic support with a max score of 0.46 linked to cholelithiasis.
Further research into the causal role of HRH1 in these genetically-linked diseases may reveal novel therapeutic opportunities.
Evidence Across Diseases
8 totalGWAS and other genetic studies link HRH1 to 8 diseases.
🔗 Colocalization Evidence 20 strong
max H4: 0.98eQTL/pQTL signals for HRH1 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 Histamine H1 receptor Drugs
The competitive landscape includes three companies with approved drugs: MIKART, PADAGIS ISRAEL, and Viatris.
The limited number of players suggests relatively low barriers to entry, but also a smaller market size.
Histamine H1 receptor Drug Modality Landscape
Modalities
Routes of Administration
Histamine H1 receptor is druggable by small molecules, though no oral formulations are currently approved.
Exploring alternative modalities like antibodies or biologics could provide a competitive advantage in targeting HRH1.
Histamine H1 receptor Clinical Trials 101 trials
Completion by Phase
| Phase | Total | Completed | Failed | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 16 | 14 | 2 | 0 | 88% |
| Phase 2 | 26 | 17 | 6 | 3 | 74% |
| Phase 3 | 32 | 29 | 3 | 0 | 91% |
| Phase 4 | 27 | 22 | 3 | 2 | 88% |
Top Sponsors
By Modality
Top Conditions
Top Drugs
Histamine H1 receptor Drug Approval Timeline (2012 - 2017)
Seasonal Allergic Rhinitis
The first HRH1-targeting drug was approved in 2003, with the most recent in 2017, spanning 15 years.
The relatively slow approval rate suggests a potentially saturated market or challenges in developing new HRH1-targeting drugs.
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Competitive Landscape
- • 3 companies competing
- • Market share by company
Full Drug Portfolio
- • All 3 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 3-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 54 clinical trials targeting Histamine H1 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