Vitamin D3 receptor Inhibitors
7 drugsAbout Vitamin D3 receptor
The Vitamin D3 receptor (VDR) is a nuclear receptor protein that regulates gene expression in response to calcitriol, the active form of Vitamin D3. As a ligand-activated transcription factor, VDR modulates the transcription of target genes by binding to Vitamin D response elements (VDREs).
VDR's role in various physiological processes makes it a potential drug target, particularly in immunology. However, there is currently no genetic evidence directly linking VDR to specific diseases.
Three FDA-approved drugs, including WYNZORA, ENSTILAR, and SORILUX, target VDR for immunological conditions. All three drugs are small molecules developed by MC2, LEO PHARMA AS, and MAYNE PHARMA, respectively.
Vitamin D3 receptor Genetic Evidence Strong
There is no genetic evidence data available for the Vitamin D3 receptor.
Absence of genetic support suggests higher risk in clinical development; consider biomarker strategies.
💡 Why activation?
- • Loss-of-function variants increase disease risk (OR > 1) — restoring function may help
- • 100% directional consistency across 1 traits
- • Strong signal in endocrine system disease, genetic, familial or congenital disease, nutritional or metabolic disease pathways
Cross-Disease Effects
Trade-off: LowDirection of Effect
100% alignedEvidence Across Diseases
18 totalGWAS and other genetic studies link VDR to 18 diseases.
Loss-of-function causes disease; activation may help
🔗 Colocalization Evidence 8 strong
max H4: 1.00eQTL/pQTL signals for VDR 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 Vitamin D3 receptor Drugs
Three companies, MC2, LEO PHARMA AS, and MAYNE PHARMA, have approved drugs targeting VDR.
The competitive landscape is unconcentrated, suggesting relatively low barriers to entry.
| Drug | Company | Approved | Indications |
|---|---|---|---|
| PARICALCITOL | AMNEAL PHARMS | 2011 | 2 |
| WYNZORA | MC2 | 2020 | 1 |
| SORILUX | MAYNE PHARMA | 2010 | 1 |
| ENSTILAR | LEO PHARMA AS | 2015 | 1 |
Vitamin D3 receptor Drug Modality Landscape
Modalities
Routes of Administration
Vitamin D3 receptor is amenable to small molecule drugs, with oral options available for convenient dosing.
The modality landscape suggests an opportunity for alternative modalities like antibodies or peptides.
Vitamin D3 receptor Clinical Trials 145 trials
Phase 1-4 trials started in 2008 or later that test an FDA-approved drug acting on Vitamin D3 receptor. Source: ClinicalTrials.gov. How we count
Completion by Phase
| Phase | Total | Completed | Stopped | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 27 | 17 | 7 | 3 | 71% |
| Phase 2 | 43 | 34 | 3 | 6 | 92% |
| Phase 3 | 28 | 19 | 8 | 1 | 70% |
| Phase 4 | 47 | 30 | 10 | 7 | 75% |
Top Sponsors
By Modality
Top Conditions
Top Drugs
Vitamin D3 receptor Drug Approval Timeline (1998 - 2020)
The first drug targeting VDR was approved in 2010, and the most recent in 2020.
The approval timeline indicates a slow but steady interest in VDR as a drug target.
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Deep insights for drug target analysis
Competitive Landscape
- • 7 companies competing
- • Market share by company
Full Drug Portfolio
- • All 7 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 7-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Sponsors: 103 (24 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 Vitamin D3 receptor. A trial counts if an approved drug acting on Vitamin D3 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.