alpha-adrenergic receptor Agonists
16 drugsAbout alpha-adrenergic receptor
The alpha-adrenergic receptor binds catecholamines like norepinephrine and epinephrine, playing a key role in the sympathetic nervous system's fight-or-flight response. As part of a larger family of adrenergic receptors, they influence various physiological processes throughout the body.
Genetic evidence offers moderate support for alpha-adrenergic receptors as therapeutic targets, with associations to hypothyroidism (score 0.53) and coronary artery bypass (score 0.49). Strong eQTL/pQTL signals further support the therapeutic rationale.
Sixteen FDA-approved small molecule drugs target alpha-adrenergic receptors, including ADRENALIN, SYMJEPI and NEFFY (approved in 2024). These drugs are used across a range of therapeutic areas.
Strategic Insights
ℹ️ How we calculate- White space opportunity in Lumbar Disc Herniation with only 3 trials.
Human Genetic Evidence Moderate
Genetic evidence provides moderate support, with a max score of 0.53 linking ADRA1A to hypothyroidism.
Further investigation of the genetic associations could refine patient selection strategies.
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 Drugs
Thirteen companies have approved drugs, with ADAMIS PHARMS CORP, Fresenius Kabi, and PH HEALTH among the top players.
The presence of multiple players suggests a competitive market with moderate entry barriers.
| Drug | Company | Approved | Indications |
|---|---|---|---|
| XYLOCAINE W/ EPINEPHRINE | Fresenius Kabi | 1948 | 2 |
| EPINEPHRINE (AUTOINJECTOR) | Teva | 2018 | 2 |
| ORAVERSE | SEPTODONT HOLDING | 2008 | 2 |
| EPIPEN | Viatris | 1987 | 2 |
| EPIPEN JR. | Viatris | 1987 | 2 |
| SYMJEPI | ADAMIS PHARMS CORP | 2017 | 2 |
| EMERPHED | NEXUS | 2020 | 1 |
| NOREPINEPHRINE BITARTRATE | RISING | 2003 | 1 |
| LEVOPHED | Pfizer | 1950 | 1 |
| NOREPINEPHRINE BITARTRATE IN 0.9% SODIUM CHLORIDE | LONG GROVE PHARMS | 2021 | 1 |
| AKOVAZ | EXELA PHARMA | 2016 | 1 |
| NOREPINEPHRINE BITARTRATE IN 5% DEXTROSE | SAGENT | 2021 | 1 |
| CORPHEDRA | PH HEALTH | 2017 | 1 |
Drug Modality Landscape
Modalities
Routes of Administration
alpha-adrenergic receptor is druggable by small molecules, though no oral formulations are currently approved.
Exploring alternative modalities like antibodies or peptides could offer differentiation.
Clinical Trials 593 trials
Completion by Phase
| Phase | Total | Completed | Failed | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 94 | 63 | 13 | 16 | 83% |
| Phase 2 | 125 | 79 | 17 | 27 | 82% |
| Phase 3 | 116 | 72 | 9 | 33 | 89% |
| Phase 4 | 258 | 182 | 27 | 45 | 87% |
Top Sponsors
By Modality
Top Conditions
Drug Approval Timeline (1948 - 2026)
The first drug was approved in 1948, with the most recent approval in 2024, spanning 77 years.
The continued approvals suggest sustained interest, but market saturation may be a concern.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 14 companies competing
- • Market share by company
Full Drug Portfolio
- • All 16 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 16-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Competition: High (15 sponsors)
- • White space: 7 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 413 clinical trials targeting alpha-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