Adenosine receptor Inhibitors
3 drugsAbout Adenosine receptor
Adenosine receptors (A1, A2A, A2B, and A3) are activated by adenosine, modulating physiological processes. They play a crucial role in cellular signaling.
Human genetic studies provide strong validation for ADORA1 as a therapeutic target, with variants linked to asthma (score 0.79). Loss-of-function variants are protective against asthma, suggesting inhibition may be beneficial.
Three FDA-approved small molecule drugs target adenosine receptors, including THEO-24, BUTALBITAL, ASPIRIN, CAFFEINE, AND CODEINE PHOSPHATE, and BUTALBITAL, ACETAMINOPHEN, CAFFEINE AND CODEINE PHOSPHATE. These drugs are used in pain and respiratory therapeutic areas.
Adenosine receptor Genetic Evidence Strong
ADORA1 has strong genetic support with a max score of 0.79 linked to asthma.
Strong genetic support increases the probability of clinical success, especially for asthma indications.
💡 Why inhibition?
- • Loss-of-function variants reduce disease risk (OR < 1)
- • 100% directional consistency across 1 traits
- • Strong signal in phenotype, respiratory or thoracic disease pathways
Cross-Disease Effects
Trade-off: LowDirection of Effect
100% alignedEvidence Across Diseases
10 totalGWAS and other genetic studies link ADORA1 to 10 diseases.
Inhibiting this target may be therapeutic
🔗 Colocalization Evidence 20 strong
max H4: 1.00eQTL/pQTL signals for ADORA1 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 Adenosine receptor Drugs
The competitive landscape includes three companies with approved drugs: STEVENS J, ENDO OPERATIONS, and Hikma.
The market is not highly concentrated, suggesting relatively low barriers to entry for new players.
Adenosine receptor Drug Modality Landscape
Modalities
Routes of Administration
Only one approved drug targets Adenosine receptor, using small molecule modality.
Exploring alternative modalities like antibodies or biologics could create whitespace opportunities.
Adenosine receptor Clinical Trials 1,138 trials
Phase 1-4 trials started in 2008 or later that test an FDA-approved drug acting on Adenosine receptor. Source: ClinicalTrials.gov. How we count
Completion by Phase
| Phase | Total | Completed | Stopped | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 219 | 169 | 18 | 29 | 90% |
| Phase 2 | 242 | 156 | 36 | 49 | 81% |
| Phase 3 | 229 | 126 | 36 | 66 | 78% |
| Phase 4 | 448 | 257 | 78 | 113 | 77% |
Top Sponsors
By Modality
Top Conditions
Top Drugs
Phase 3 Readout Calendar Pro
2 Phase 3 trials testing approved Adenosine receptor drugs across all sponsors.
Coverage: trials whose intervention is an approved drug targeting Adenosine receptor. Pre-approval candidates with development codes (e.g. AZD0901, MK-7240) are not yet linked. Anchored on CT.gov primary completion date.
Adenosine receptor Drug Approval Timeline (1983 - 1983)
The first drug was approved in 1983 (THEO-24), and the most recent in 2001, spanning 19 years.
The approval timeline suggests a potential for renewed interest and innovation in adenosine receptor-targeted therapies.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 3 companies competing
- • Market share by company
Full Drug Portfolio
- • All 3 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 3-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Sponsors: 579 (112 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 Adenosine receptor. A trial counts if an approved drug acting on Adenosine 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.