Dopamine receptor Inhibitors
5 drugsAbout Dopamine receptor
The Dopamine receptor (DRD2) is a key neurotransmitter receptor in the central nervous system, mediating a wide range of neurological and psychiatric functions. As a crucial player in neurotransmission, it is an attractive target for therapeutic intervention in CNS disorders.
Human genetic studies provide strong validation for DRD2 as a therapeutic target, with variants linked to major depressive disorder (score 0.86), bipolar disorder (score 0.77), and substance-related disorder (score 0.73). Loss-of-function variants are protective, suggesting that inhibition may be beneficial.
DRD2 is targeted by 5 FDA-approved small molecule drugs, including LYBALVI, ZYPREXA, and NEUPRO, for CNS indications. CHEPLAPHARM, ALKERMES INC, and UCB INC are the key players in this space, with ZYPREXA being the first approved drug in 1996 and LYBALVI the most recent in 2021.
Dopamine receptor Genetic Evidence Strong
DRD2 has strong genetic support with a max score of 0.86 linked to major depressive disorder.
Strong genetic support increases clinical success probability, making DRD2 a promising target.
💡 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 Dopamine receptor Drugs
The DRD2 drug market is concentrated among three main companies: CHEPLAPHARM, ALKERMES INC, and UCB INC.
High market concentration suggests potential entry barriers for new companies.
| Drug | Company | Approved | Indications |
|---|---|---|---|
| ZYPREXA ZYDIS | CHEPLAPHARM | 2000 | 2 |
| ZYPREXA RELPREVV | CHEPLAPHARM | 2009 | 1 |
Dopamine receptor Drug Modality Landscape
Modalities
Routes of Administration
Dopamine receptor is amenable to small molecule drugs, with oral options available for convenient dosing.
Exploring alternative modalities like antibodies or biologics could create differentiation.
Dopamine receptor Clinical Trials 211 trials
Phase 1-4 trials started in 2008 or later that test an FDA-approved drug acting on Dopamine receptor. Source: ClinicalTrials.gov. How we count
Completion by Phase
| Phase | Total | Completed | Stopped | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 45 | 41 | 1 | 3 | 98% |
| Phase 2 | 49 | 27 | 10 | 11 | 73% |
| Phase 3 | 67 | 41 | 9 | 17 | 82% |
| Phase 4 | 50 | 39 | 8 | 3 | 83% |
Top Sponsors
By Modality
Top Conditions
Dopamine receptor Drug Approval Timeline (1996 - 2021)
DRD2 has a 26-year approval history, with the first drug approved in 1996 and the most recent in 2021.
The recent approval suggests continued interest and potential for further development.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 3 companies competing
- • Market share by company
Full Drug Portfolio
- • All 5 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 5-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Sponsors: 143 (38 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 Dopamine receptor. A trial counts if an approved drug acting on Dopamine 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.