D2 receptor Inhibitors
20 drugsAbout D2 receptor
The D2 receptor, a subtype of dopamine receptor, is a GPCR crucial in the CNS, influencing motor control, reward, and hormone regulation via neurotransmission.
Human genetic studies provide strong validation for DRD2 as a therapeutic target (max score 0.86), with variants linked to major depressive disorder, bipolar disorder and substance-related disorder. Loss-of-function variants are protective, suggesting agonist-based therapies may be beneficial.
With 20 FDA-approved small molecule drugs like aripiprazole (Abilify) and paliperidone (Invega), the D2 receptor is a significant target in CNS disorders, including schizophrenia and Huntington's disease.
Strategic Insights
ℹ️ How we calculate- White space opportunity in Bipolar Depression with only 4 trials.
D2 receptor Genetic Evidence Strong
DRD2 has strong genetic support with a max score of 0.86 across 34 diseases.
Strong genetic support suggests prioritizing DRD2 agonist development for CNS indications.
💡 Why inhibition?
- • Loss-of-function variants reduce disease risk (OR < 1)
- • 50% directional consistency across 2 traits
- • Strong signal in psychiatric disorder, nervous system disease pathways
Cross-Disease Effects
Trade-off: ModerateDirection of Effect
50% alignedEvidence Across Diseases
20 totalGWAS and other genetic studies link DRD2 to 34 diseases.
Activating this target may be therapeutic
Inhibiting this target may be therapeutic
🔗 Colocalization Evidence 20 strong
max H4: 0.99eQTL/pQTL signals for DRD2 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 D2 receptor Drugs
Sixteen companies have approved drugs targeting the D2 receptor, including Teva and AbbVie.
The fragmented market suggests opportunities for new entrants with differentiated D2 receptor therapies.
| Drug | Company | Approved | Indications |
|---|---|---|---|
| PERSERIS KIT | INDIVIOR | 2018 | 3 |
| SAPHRIS | AbbVie | 2009 | 3 |
| CLOZAPINE | Teva | 1996 | 2 |
| UZEDY | Teva | 2023 | 2 |
| LATUDA | SUNOVION PHARMS INC | 2010 | 2 |
| PALIPERIDONE | RK PHARMA | 2015 | 2 |
| VERSACLOZ | DOUGLAS PHARMS | 2013 | 2 |
| ABILIFY ASIMTUFII | OTSUKA | 2023 | 2 |
| VRAYLAR | AbbVie | 2015 | 2 |
| TETRABENAZINE | Sun Pharma | 2015 | 1 |
| SECUADO | HISAMITSU | 2019 | 1 |
| INVEGA HAFYERA | Johnson & Johnson | 2015 | 1 |
| DOPAMINE HYDROCHLORIDE IN DEXTROSE 5% IN PLASTIC CONTAINER | Pfizer | 1983 | 1 |
| ARISTADA | ALKERMES INC | 2015 | 1 |
| BARHEMSYS | ACACIA | 2020 | 1 |
| ARISTADA INITIO KIT | ALKERMES INC | 2018 | 1 |
| ONAPGO | MDD US | 2025 | 1 |
D2 receptor Drug Modality Landscape
Modalities
Routes of Administration
D2 receptor is amenable to small molecule drugs, with oral options available for convenient dosing.
Explore novel modalities like antibodies or PROTACs to differentiate from existing small molecule drugs.
D2 receptor Clinical Trials 481 trials
Completion by Phase
| Phase | Total | Completed | Failed | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 77 | 68 | 3 | 5 | 96% |
| Phase 2 | 76 | 51 | 15 | 8 | 77% |
| Phase 3 | 153 | 124 | 19 | 9 | 87% |
| Phase 4 | 175 | 120 | 34 | 21 | 78% |
Top Sponsors
By Modality
Top Conditions
Top Drugs
Phase 3 Readout Calendar Pro
1 Phase 3 trial testing approved D2 receptor drugs across all sponsors.
Coverage: trials whose intervention is an approved drug targeting D2 receptor. Pre-approval candidates with development codes (e.g. AZD0901, MK-7240) are not yet linked. Anchored on CT.gov primary completion date.
D2 receptor Drug Approval Timeline (1983 - 2025)
Shock
D2 receptor drugs have been approved over 43 years, from 1983 to 2025.
The continued approval of D2 receptor drugs indicates sustained interest and potential for further innovation.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 16 companies competing
- • Market share by company
Full Drug Portfolio
- • All 20 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 20-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Competition: High (15 sponsors)
- • White space: 8 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 346 clinical trials targeting D2 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