Delta-opioid receptor Agonists
4 drugsAbout Delta-opioid receptor
The Delta-opioid receptor (DOR) modulates pain perception and emotional responses within the central nervous system. As a member of the opioid receptor family, it is a G-protein coupled receptor that plays a crucial role in these processes.
Human genetic studies provide strong validation for OPRD1 (score 0.71), with variants linked to substance-related disorder, nicotine dependence (LoF protect), and chronic obstructive pulmonary disease. Loss-of-function variants are protective against nicotine dependence, supporting agonist-based therapies.
Four FDA-approved small molecule drugs target DOR, including SYMPROIC, BUPRENORPHINE, VIBERZI, and BUTRANS. Two drugs address pain, while the other two target other conditions, indicating potential for therapeutic expansion.
Delta-opioid receptor Genetic Evidence Strong
Genetic evidence shows strong support for OPRD1, with a max score of 0.71 linked to substance-related disorders.
Strong genetic support suggests a higher probability of clinical success, warranting further investment in DOR-targeted therapies.
💡 Why inhibition?
- • Loss-of-function variants reduce disease risk (OR < 1)
- • 100% directional consistency across 1 traits
- • Strong signal in psychiatric disorder, nervous system disease pathways
Cross-Disease Effects
Trade-off: LowDirection of Effect
100% alignedEvidence Across Diseases
4 totalGWAS and other genetic studies link OPRD1 to 4 diseases.
Inhibiting this target may be therapeutic
🔗 Colocalization Evidence 20 strong
max H4: 0.98eQTL/pQTL signals for OPRD1 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 Delta-opioid receptor Drugs
Four companies have approved drugs targeting DOR: BDSI, WATSON LABS TEVA, AbbVie, and PURDUE PHARMA LP.
The presence of multiple players suggests a moderately competitive market, requiring a differentiated approach for new entrants.
| Drug | Company | Approved | Indications |
|---|---|---|---|
| BUPRENORPHINE | WATSON LABS TEVA | 2018 | 1 |
Delta-opioid receptor Drug Modality Landscape
Modalities
Routes of Administration
Delta-opioid receptor is amenable to small molecule drugs, with oral options available for convenient dosing.
The absence of other modalities like antibodies or peptides represents a whitespace opportunity for novel therapeutic development.
Delta-opioid receptor Clinical Trials 225 trials
Phase 1-4 trials started in 2008 or later that test an FDA-approved drug acting on Delta-opioid receptor. Source: ClinicalTrials.gov. How we count
Completion by Phase
| Phase | Total | Completed | Stopped | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 43 | 35 | 3 | 5 | 92% |
| Phase 2 | 54 | 36 | 10 | 8 | 78% |
| Phase 3 | 51 | 35 | 9 | 6 | 80% |
| Phase 4 | 77 | 42 | 14 | 20 | 75% |
Top Sponsors
By Modality
Top Conditions
Top Drugs
Delta-opioid receptor Drug Approval Timeline (2010 - 2018)
The first drug was approved in 2010 (BUTRANS), and the most recent in 2018 (BUPRENORPHINE), spanning 9 years.
The recent approval suggests continued interest, but the relatively short span may indicate approaching market saturation.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 4 companies competing
- • Market share by company
Full Drug Portfolio
- • All 4 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 4-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Sponsors: 122 (31 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 Delta-opioid receptor. A trial counts if an approved drug acting on Delta-opioid 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.