alpha-1 adrenergic receptor Agonists
12 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.
alpha-1 adrenergic receptor 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 alpha-1 adrenergic receptor 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 | Company | Approved | Indications |
|---|---|---|---|
| CARVEDILOL PHOSPHATE | Sun Pharma | 2017 | 4 |
| DOXAZOSIN MESYLATE | NESHER PHARMS | 2000 | 2 |
| OMIDRIA | RAYNER SURGICAL | 2014 | 2 |
| SILODOSIN | Lupin | 2017 | 1 |
| PHENYLEPHRINE HYDROCHLORIDE | SAGENT PHARMS INC | 2012 | 1 |
| CARDURA XL | Viatris | 2005 | 1 |
| TONMYA | TONIX | 2025 | 1 |
| RYZUMVI | FAMYGEN LIFE SCI | 2023 | 1 |
| CARVEDILOL | Sun Pharma | 2007 | - |
alpha-1 adrenergic receptor Drug Modality Landscape
Modalities
Routes of Administration
alpha-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.
alpha-1 adrenergic receptor Clinical Trials 415 trials
Phase 1-4 trials started in 2008 or later that test an FDA-approved drug acting on alpha-1 adrenergic receptor. Source: ClinicalTrials.gov. How we count
Completion by Phase
| Phase | Total | Completed | Stopped | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 50 | 31 | 12 | 7 | 72% |
| Phase 2 | 97 | 57 | 18 | 20 | 76% |
| Phase 3 | 77 | 44 | 16 | 15 | 73% |
| Phase 4 | 191 | 125 | 25 | 41 | 83% |
Top Sponsors
By Modality
Top Conditions
Top Drugs
alpha-1 adrenergic receptor Drug Approval Timeline (1995 - 2025)
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
- • 10 companies competing
- • Market share by company
Full Drug Portfolio
- • All 12 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 12-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Sponsors: 262 (39 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 alpha-1 adrenergic receptor. A trial counts if an approved drug acting on alpha-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.