Beta-adrenoreceptor Inhibitors
7 drugsAbout Beta-adrenoreceptor
Beta-adrenoreceptors (β-adrenergic receptors) are G protein-coupled receptors that mediate the effects of catecholamines like adrenaline and noradrenaline, influencing heart rate, blood pressure, and bronchodilation.
Human genetic studies provide strong validation for ADRB1 as a therapeutic target, with variants linked to hypertension (score 0.89), essential hypertension (0.83), and cardiovascular disease (0.79). Loss-of-function variants are protective, suggesting agonist therapies may be beneficial.
Seven FDA-approved small molecule drugs target Beta-adrenoreceptors, including SOTALOL HYDROCHLORIDE, CARVEDILOL PHOSPHATE, and COREG CR. These drugs primarily address cardiovascular conditions, with one drug targeting a different therapeutic area.
Beta-adrenoreceptor Genetic Evidence Strong
ADRB1 has strong genetic support with a max score of 0.89 across 9 diseases.
The strong genetic support suggests a higher probability of clinical success for new ADRB1-targeting drugs.
💡 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 Beta-adrenoreceptor Drugs
Seven companies have approved drugs, including Aurobindo Pharma, REGCON HOLDINGS and AZURITY.
The relatively fragmented market suggests moderate entry barriers for new competitors.
| Drug | Company | Approved | Indications |
|---|---|---|---|
| CARVEDILOL PHOSPHATE | Sun Pharma | 2017 | 4 |
| SORINE | AIPING PHARM INC | 2001 | 4 |
| BETAPACE | LEGACY | 1992 | 3 |
| SOTYLIZE | AZURITY | 2014 | 3 |
Beta-adrenoreceptor Drug Modality Landscape
Modalities
Routes of Administration
Beta-adrenoreceptor is amenable to small molecule drugs, with oral options available for convenient dosing.
Exploring alternative modalities like antibodies or peptides could provide a competitive advantage.
Beta-adrenoreceptor Clinical Trials 75 trials
Phase 1-4 trials started in 2008 or later that test an FDA-approved drug acting on Beta-adrenoreceptor. Source: ClinicalTrials.gov. How we count
Completion by Phase
| Phase | Total | Completed | Stopped | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 13 | 7 | 4 | 2 | 64% |
| Phase 2 | 19 | 6 | 6 | 7 | 50% |
| Phase 3 | 13 | 8 | 2 | 3 | 80% |
| Phase 4 | 30 | 17 | 1 | 12 | 94% |
Top Sponsors
By Modality
Top Conditions
Top Drugs
Beta-adrenoreceptor Drug Approval Timeline (1992 - 2017)
The first drug was approved in 1992 (BETAPACE) and the most recent in 2017 (CARVEDILOL PHOSPHATE), spanning 26 years.
The approval timeline suggests a mature market with potential for incremental innovation rather than disruptive breakthroughs.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 6 companies competing
- • Market share by company
Full Drug Portfolio
- • All 7 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 7-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Sponsors: 64 (7 companies)
- • Completion rates by condition
Full summary • All drugs • Genetic evidence • Trials • Timeline
How We Count Trials
- Trials: phase 1-4 interventional trials on ClinicalTrials.gov that started in 2008 or later and test an FDA-approved drug acting on Beta-adrenoreceptor. A trial counts if an approved drug acting on Beta-adrenoreceptor is in any arm, including as a comparator, and a trial that tests two such drugs counts once. Trials that test only unapproved drugs are not counted. A trial listed as phase 1/2 counts as phase 1, and phase 2/3 as phase 2.
- Active: recruiting, not yet recruiting, enrolling by invitation, or active and no longer recruiting.
- Completion rate: of the trials that have ended, the share marked Completed rather than Terminated or Withdrawn. Completed means the trial ended as planned; it does not mean the drug worked. Suspended trials are not counted as ended.
- Stopped: terminated or withdrawn. Trials stop for many reasons, including slow enrolment and business decisions, not only safety or efficacy.
- Sponsors: the lead sponsor of each trial. Companies are the sponsors ClinicalTrials.gov classes as industry; the rest are universities, hospitals, cooperative groups, government bodies and individuals.