Beta-1 adrenergic receptor Agonists
21 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.
Beta-1 adrenergic receptor 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 Beta-1 adrenergic receptor 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 | Company | Approved | Indications |
|---|---|---|---|
| ESMOLOL HYDROCHLORIDE | HQ SPCLT PHARMA | 2004 | 6 |
| ESMOLOL HYDROCHLORIDE DOUBLE STRENGTH IN PLASTIC CONTAINER | HQ SPCLT PHARMA | 2016 | 6 |
| ESMOLOL HYDROCHLORIDE IN PLASTIC CONTAINER | HQ SPCLT PHARMA | 2016 | 6 |
| BREVIBLOC IN PLASTIC CONTAINER | Baxter | 1986 | 6 |
| BREVIBLOC DOUBLE STRENGTH IN PLASTIC CONTAINER | Baxter | 1986 | 6 |
| RAPIBLYK | AOP HLTH US | 2024 | 3 |
| TOPROL-XL | MELINTA THERAP | 1992 | 3 |
| KAPSPARGO SPRINKLE | SPIL | 2018 | 3 |
| DORZOLAMIDE HYDROCHLORIDE AND TIMOLOL MALEATE | Teva | 2008 | 2 |
| COSOPT PF | THEA PHARMA | 2012 | 2 |
| TIMOPTIC-XE | BAUSCH AND LOMB INC | 1993 | 2 |
| BRIMONIDINE TARTRATE AND TIMOLOL MALEATE | SABA ILAC SANAYIVE | 2022 | 2 |
| TIMOLOL | EPIC PHARMA LLC | 2016 | 2 |
| ISTALOL | BAUSCH AND LOMB INC | 2004 | 2 |
| BETOPTIC | Novartis | 1985 | 2 |
| BETOPTIC S | Novartis | 1989 | 2 |
| COSOPT | THEA PHARMA | 1998 | 2 |
| TIMOPTIC | BAUSCH AND LOMB INC | 1978 | 2 |
Beta-1 adrenergic receptor Drug Modality Landscape
Modalities
Routes of Administration
Beta-1 adrenergic receptor 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-1 adrenergic receptor Clinical Trials 355 trials
Phase 1-4 trials started in 2008 or later that test an FDA-approved drug acting on Beta-1 adrenergic receptor. Source: ClinicalTrials.gov. How we count
Completion by Phase
| Phase | Total | Completed | Stopped | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 56 | 46 | 6 | 4 | 88% |
| Phase 2 | 74 | 58 | 7 | 9 | 89% |
| Phase 3 | 85 | 60 | 12 | 13 | 83% |
| Phase 4 | 140 | 100 | 23 | 17 | 81% |
Top Sponsors
By Modality
Top Conditions
Top Drugs
Beta-1 adrenergic receptor Drug Approval Timeline (1978 - 2024)
Supraventricular Tachycardia
Supraventricular Tachycardia
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
- • 13 companies competing
- • Market share by company
Full Drug Portfolio
- • All 21 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 21-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Sponsors: 203 (62 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-1 adrenergic receptor. A trial counts if an approved drug acting on Beta-1 adrenergic receptor 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.