D2 receptor Inhibitors
32 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.
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 |
|---|---|---|---|
| ARIPIPRAZOLE | Teva | 2015 | 3 |
| CAPLYTA | INTRA-CELLULAR | 2019 | 3 |
| SAPHRIS | AbbVie | 2009 | 3 |
| ABILIFY MAINTENA KIT | OTSUKA | 2013 | 3 |
| PERSERIS KIT | INDIVIOR | 2018 | 3 |
| RYKINDO | SHANDONG LUYE | 2023 | 3 |
| ZIPRASIDONE HYDROCHLORIDE | Dr. Reddy's | 2012 | 2 |
| PALIPERIDONE | Dr. Reddy's | 2015 | 2 |
| CLOZAPINE | ACCORD HLTHCARE | 1996 | 2 |
| ABILIFY ASIMTUFII | OTSUKA | 2023 | 2 |
| RISPERDAL | Johnson & Johnson | 1993 | 2 |
| SEROQUEL | CHEPLAPHARM | 1997 | 2 |
| ERZOFRI | LUYE INNOMIND PHARMA | 2024 | 2 |
| RISPERDAL CONSTA | Johnson & Johnson | 2003 | 2 |
| LATUDA | SUNOVION PHARMS INC | 2010 | 2 |
| VERSACLOZ | DOUGLAS PHARMS | 2013 | 2 |
| VRAYLAR | AbbVie | 2015 | 2 |
| UZEDY | Teva | 2023 | 2 |
| FANAPT | VANDA PHARMS INC | 2009 | 2 |
| INVEGA SUSTENNA | Johnson & Johnson | 2009 | 2 |
| TETRABENAZINE | BIONPHARMA | 2015 | 1 |
| DOPAMINE HYDROCHLORIDE IN DEXTROSE 5% IN PLASTIC CONTAINER | Baxter | 1983 | 1 |
| SECUADO | HISAMITSU PHARM CO | 2019 | 1 |
| ARISTADA | ALKERMES | 2015 | 1 |
| INVEGA HAFYERA | Johnson & Johnson | 2015 | 1 |
| INVEGA TRINZA | Johnson & Johnson | 2015 | 1 |
| ONAPGO | MDD US | 2025 | 1 |
| BARHEMSYS | LXO IRELAND | 2020 | 1 |
| ARISTADA INITIO KIT | ALKERMES | 2018 | 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 639 trials
Phase 1-4 trials started in 2008 or later that test an FDA-approved drug acting on D2 receptor. Source: ClinicalTrials.gov. How we count
Completion by Phase
| Phase | Total | Completed | Stopped | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 109 | 96 | 5 | 8 | 95% |
| Phase 2 | 104 | 64 | 22 | 16 | 74% |
| Phase 3 | 200 | 152 | 25 | 22 | 86% |
| Phase 4 | 226 | 149 | 46 | 31 | 76% |
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
- • 22 companies competing
- • Market share by company
Full Drug Portfolio
- • All 32 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 32-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Sponsors: 272 (84 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 D2 receptor. A trial counts if an approved drug acting on D2 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.