alpha 1 adrenergic receptor Agonists
1 drugsAbout alpha 1 adrenergic receptor
The alpha-1 adrenergic receptor (adrenoceptor alpha 1) is a G protein-coupled receptor crucial for cellular communication. It is a significant drug target, particularly in cardiovascular and pain therapeutics, modulating cellular activity to achieve therapeutic effects.
Human genetics provide moderate support for ADRA1A as a therapeutic target, with a max genetic score of 0.53 linked to hypothyroidism. Other associations include coronary artery bypass (0.49) and respiratory system neoplasm (0.48), suggesting potential for novel treatments.
The alpha-1 adrenergic receptor is targeted by 11 FDA-approved small molecule drugs, including IMMPHENTIV, CARVEDILOL PHOSPHATE, and COREG. These drugs are used across cardiovascular, pain, and other therapeutic areas.
Strategic Insights
ℹ️ How we calculate- White space opportunity in Alcohol Use Disorder (AUD) with only 1 trials.
Human Genetic Evidence Moderate
Genetic evidence offers moderate support, with a top score of 0.53 for hypothyroidism.
Further investigation into the genetic associations may reveal novel therapeutic opportunities.
Evidence Across Diseases
5 totalGWAS and other genetic studies link ADRA1A to 5 diseases.
🔗 Colocalization Evidence 4 strong
max H4: 1.00eQTL/pQTL signals for ADRA1A 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
Ten companies have approved drugs targeting the alpha-1 adrenergic receptor, including Aurobindo Pharma and Hikma.
The presence of multiple players suggests a competitive market with moderate entry barriers.
Drug Modality Landscape
Modalities
Routes of Administration
Only one approved drug targets alpha 1 adrenergic receptor, using small molecule modality.
Exploring alternative modalities like antibodies or peptides could provide a competitive advantage.
Clinical Trials 33 trials
Completion by Phase
| Phase | Total | Completed | Failed | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 14 | 13 | 0 | 1 | 100% |
| Phase 2 | 10 | 6 | 0 | 3 | 100% |
| Phase 3 | 5 | 5 | 0 | 0 | 100% |
| Phase 4 | 4 | 3 | 1 | 0 | 75% |
Top Sponsors
By Modality
Top Conditions
Top Drugs
Drug Approval Timeline (2005 - 2005)
The first drug was approved in 1995 (COREG), with the most recent approval in 2025 (TONMYA).
The continued approvals indicate sustained interest and potential for further 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 17 clinical trials targeting alpha 1 adrenergic 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