Beta-1-adrenergic receptor Agonists
2 drugsAbout Beta-1-adrenergic receptor
The Beta-1 adrenergic receptor (ADRB1) is a G protein-coupled receptor that mediates the effects of catecholamines, regulating heart rate and contractility. It is expressed in cardiac tissue and plays a crucial role in the sympathetic nervous system's control of cardiovascular function.
ADRB1 is a genetically validated drug target, with strong evidence linking it to hypertension (score 0.89) and cardiovascular disease (score 0.79). Loss-of-function variants are protective against hypertension, suggesting that receptor inhibition is a viable therapeutic strategy.
ADRB1 is targeted by 21 FDA-approved small molecule drugs, including BREVIBLOC and TIMOPTIC, across cardiovascular and ophthalmology indications. These drugs are marketed by 14 companies, including IPCA LABS LTD and RISING.
Strategic Insights
ℹ️ How we calculate- White space opportunity in Endometrial Cancer with only 1 trials.
Human Genetic Evidence Strong
ADRB1 has strong genetic support with a max score of 0.89 linking it to hypertension.
The strong genetic support for ADRB1 increases the probability of clinical trial success.
💡 Why inhibition?
- • Loss-of-function variants reduce disease risk (OR < 1)
- • 100% directional consistency across 3 traits
- • Strong signal in cardiovascular disease, phenotype pathways
Cross-Disease Effects
Trade-off: LowDirection of Effect
100% alignedEvidence Across Diseases
9 totalGWAS and other genetic studies link ADRB1 to 9 diseases.
Inhibiting this target may be therapeutic
Inhibiting this target may be therapeutic
🔗 Colocalization Evidence 20 strong
max H4: 1.00eQTL/pQTL signals for ADRB1 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
Fourteen companies have approved drugs targeting ADRB1, suggesting a moderately competitive landscape.
The presence of multiple players indicates relatively low barriers to entry in this market.
Drug Modality Landscape
Modalities
Routes of Administration
Beta-1-adrenergic receptor is druggable by small molecules, though no oral formulations are currently approved.
Exploring alternative modalities like antibodies or peptides could provide a competitive advantage.
Clinical Trials 30 trials
Completion by Phase
| Phase | Total | Completed | Failed | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 12 | 9 | 1 | 2 | 90% |
| Phase 2 | 4 | 2 | 1 | 1 | 67% |
| Phase 3 | 8 | 5 | 0 | 3 | 100% |
| Phase 4 | 6 | 2 | 1 | 3 | 67% |
Top Sponsors
By Modality
Drug Approval Timeline (1985 - 2024)
The first ADRB1-targeting drug was approved in 1978, with the most recent approval in 2024.
The continued approval of new drugs suggests ongoing innovation and market potential.
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 17 clinical trials targeting Beta-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