beta-adrenergic receptor Agonists
19 drugsAbout beta-adrenergic receptor
The beta-adrenergic receptor (β-adrenergic receptor) is a GPCR mediating catecholamine effects, influencing heart rate, bronchodilation, and metabolism.
Human genetics strongly support beta-adrenergic receptor targeting, with hypertension (score 0.89), essential hypertension (0.83), and cardiovascular disease (0.79) associations. Loss-of-function variants are protective, suggesting inhibition is beneficial.
Nineteen small molecule drugs target beta-adrenergic receptors, including ADRENALIN, COREG, and NEFFY, spanning 'other' indications (15), cardiovascular (2), and ophthalmology (2).
beta-adrenergic receptor Genetic Evidence Strong
Strong genetic evidence supports ADRB1's role in hypertension and cardiovascular disease.
High genetic scores suggest clinical trials targeting hypertension have increased likelihood of 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-adrenergic receptor Drugs
Sixteen companies have approved beta-adrenergic receptor drugs, including GLENMARK PHARMS LTD and ADAMIS PHARMS CORP.
A fragmented market suggests moderate entry barriers, but established players have an advantage.
| Drug | Company | Approved | Indications |
|---|---|---|---|
| EPINEPHRINE (AUTOINJECTOR) | Teva | 2018 | 2 |
| BRIMONIDINE TARTRATE AND TIMOLOL MALEATE | SABA ILAC SANAYIVE | 2022 | 2 |
| ADRENACLICK | IMPAX LABS | 2003 | 2 |
| XYLOCAINE W/ EPINEPHRINE | AstraZeneca | 1948 | 2 |
| NEFFY | ARS PHARMS OPERATION | 2024 | 2 |
| COMBIGAN | AbbVie | 2007 | 2 |
| EPIPEN | Viatris | 1987 | 2 |
| EPIPEN JR. | Viatris | 1987 | 2 |
| SYMJEPI | ADAMIS PHARMS CORP | 2017 | 2 |
| NOREPINEPHRINE BITARTRATE IN 0.9% SODIUM CHLORIDE | LONG GROVE PHARMS | 2021 | 1 |
| NOREPINEPHRINE BITARTRATE | Novartis | 2003 | 1 |
| EMERPHED | NEXUS | 2020 | 1 |
| LEVOPHED | Pfizer | 1950 | 1 |
| NOREPINEPHRINE BITARTRATE IN 5% DEXTROSE | SAGENT | 2021 | 1 |
| CORPHEDRA | PH HEALTH | 2017 | 1 |
| AKOVAZ | EXELA PHARMA | 2016 | 1 |
beta-adrenergic receptor Drug Modality Landscape
Modalities
Routes of Administration
beta-adrenergic receptor is amenable to small molecule drugs, with oral options available for convenient dosing.
Exploring alternative modalities like antibodies or peptides may offer differentiation opportunities.
beta-adrenergic receptor Clinical Trials 831 trials
Phase 1-4 trials started in 2008 or later that test an FDA-approved drug acting on beta-adrenergic receptor. Source: ClinicalTrials.gov. How we count
Completion by Phase
| Phase | Total | Completed | Stopped | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 105 | 72 | 21 | 12 | 77% |
| Phase 2 | 191 | 115 | 34 | 41 | 77% |
| Phase 3 | 148 | 108 | 14 | 25 | 89% |
| Phase 4 | 387 | 269 | 54 | 63 | 83% |
Top Sponsors
By Modality
Top Conditions
Top Drugs
beta-adrenergic receptor Drug Approval Timeline (1950 - 2024)
Approvals span 77 years from 1948 (XYLOCAINE W/ EPINEPHRINE) to 2024 (NEFFY).
Consistent approvals indicate sustained interest, but recent approvals may signal renewed focus.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 17 companies competing
- • Market share by company
Full Drug Portfolio
- • All 19 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 19-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Sponsors: 511 (68 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-adrenergic receptor. A trial counts if an approved drug acting on beta-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.