Protein / target
Vitamin D3 receptor
Protein at a glance
Biological role
Bile acid nuclear receptor
Strongest disease association
Hypocalcemic vitamin D-resistant rickets
Therapeutic position
Established drug target
Derived from structured UniProt, Open Targets and literature data on this page.
Protein profile
Canonical identity and biological annotation from UniProt.
Function overview
Nuclear receptor for calcitriol, the active form of vitamin D3 which mediates the action of this vitamin on cells.
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Nuclear receptor for calcitriol, the active form of vitamin D3 which mediates the action of this vitamin on cells (PubMed:10678179, PubMed:15728261, PubMed:16913708, PubMed:28698609, PubMed:37478846). Enters the nucleus upon vitamin D3 binding where it forms heterodimers with the retinoid X receptor/RXR (PubMed:28698609). The VDR-RXR heterodimers bind to specific response elements on DNA and activate the transcription of vitamin D3-responsive target genes (PubMed:28698609). Plays a central role in calcium homeostasis (By similarity). Also functions as a receptor for the secondary bile acid lithocholic acid (LCA) and its metabolites (PubMed:12016314, PubMed:32354638)
Subcellular location
Domains and Gene Ontology detail (38)Hide
Domains & features
Gene Ontology
- Cchromatin
- Ccytoplasm
- Cnucleoplasm
- Cnucleus
- Creceptor complex
- CRNA polymerase II transcription regulator complex
- Fbile acid nuclear receptor activity
- Fcalcitriol binding
- FDNA binding
- FDNA-binding transcription factor activity, RNA polymerase II-specific
- Flithocholic acid binding
- Fnuclear receptor activity
Biological roles
What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.
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Nuclear receptor signalling
- ·Nuclear receptor for calcitriol, the active form of vitamin D3 which mediates the action…
- ·bile acid nuclear receptor activity
- ·nuclear receptor activity
- ·nuclear receptor-mediated bile acid signaling pathway
Ion channel gating
- ·phosphate ion transmembrane transport
Cell proliferation & survival
- ·negative regulation of cell population proliferation
Transcriptional regulation
- ·Nuclear receptor for calcitriol, the active form of vitamin D3 which mediates the action…
- ·RNA polymerase II transcription regulator complex
- ·DNA-binding transcription factor activity, RNA polymerase II-specific
- ·RNA polymerase II cis-regulatory region sequence-specific DNA binding
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Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.
Approved medicines with mapped indications
Approved therapies targeting this protein, grouped by what they are approved to treat — the disease-first view of the medicines below. Relationships come from the canonical approved-indication graph (ChEMBL phase-4), the same source as the drug cards.
9 medicines meet Open Targets' target-level approved-medicine definition; the 4 shown here are those on this page with a canonical approved disease indication in the graph. Approved indications from ChEMBL (phase-4), via the canonical drug→disease graph.
Drugs targeting this protein
How approved and investigational drugs engage this protein — mechanism and action type, direct vs complex targeting, and how broadly each acts across other targets. A drug-first view (the section above groups the approved ones disease-first); direct binders with few recorded targets are listed first.
Vitamin D receptor agonist
Indicated for Hypoparathyroidism, Kidney Failure, Chronic, Psoriasis
Vitamin D receptor agonist
Indicated for Hyperparathyroidism, Secondary, Parathyroid Diseases, Renal Insufficiency, Chronic
Vitamin D receptor agonist
Indicated for Anemia, Anemia, Iron-Deficiency, Osteoporosis
ChEMBL mechanism, action type, target identity and approved indications. Open Targets clinical status.
Translational evidence
Why this target matters therapeutically, strongest evidence first. Disease associations are gene-level (via the gene that encodes this protein) and open into the full confidence synthesis; the development universe, tractability and safety annotations are target-level, from Open Targets.
Strongest disease associations · via encoding gene VDR
Gene-level evidence surfaced through the gene VDRthat encodes this protein — not a direct protein–disease relationship. Ranked by Forefront's causal-directness weighting, so genetically- and clinically-evidenced diseases lead over ones that merely share the literature.
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The evidence agreement range shows how closely the independent evidence families agree — it is not a statistical confidence interval, and nothing here is fitted to outcome data. Derived from Open Targets evidence types under Forefront weighting; the per-type scores above show the calculation.
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Drug development
18 compounds recorded · 9 approved · 9 in clinical development
View all recorded compounds (10)Hide
Open Targets known-drugs universe. Drug name and highest clinical stage only — the disease relationship is NOT read from this slice (it carries trial-context noise); approved indications come from the canonical graph above.
Tractability
Small molecules — Strong
Protein degraders — Emerging
View underlying tractability evidence (8)Hide
Raw Open Targets tractability assessment buckets, by modality.
Safety-related annotations
Terms indexed against this target in Open Targets' safety data, with their datasource. These are annotations, not causal claims: the direction of effect (whether activation or inhibition is implicated), species and evidence strength are not captured here, so an entry does not mean that modulating this target is known to cause that condition.
Clinical trials
Trials of drugs that target this protein — reached indirectly through those drugs, so a trial listed here studies the drug, not the protein. Ranked by active status, then clinical phase and recency, and spread across the targeting drugs.
View all trials (26)Hide
ClinicalTrials.gov via the drug-target graph.
What's happening now
Recent therapeutic activity around this target — regulatory actions, clinical trials and safety signals for 4 drugs that target this protein, plus publications where such a drug is a genuine subject. Every item is reached indirectly through the drug, not the protein itself; incidental mentions (a paper that merely measures a drug) and press items are excluded.
- Label change
Label change: PARICALCITOL (NDA205917)
- New publicationRandomized trial of activated vitamin D for acute kidney injury prevention in critically ill patients.
- New publicationMolecular Insight into the Role of Vitamin D in Immune-Mediated Inflammatory Diseases.
- New publicationPembrolizumab ± paricalcitol in metastatic pancreatic cancer postmaximal cytoreduction.
- New publicationHigh-dose vitamin D supplementation does not improve outcome in a cutaneous melanoma population: results of a randomized double-blind placebo-controlled study (ViDMe trial).
- New publicationMultifaceted Roles of Vitamin D for Diabetes: From Immunomodulatory Functions to Metabolic Regulations.
- New publicationVitamin D and Metabolic Dysfunction-Associated Steatotic Liver Disease (MASLD): Novel Mechanistic Insights.
- New publicationRole of Calcitriol and Vitamin D Receptor (<i>VDR</i>) Gene Polymorphisms in Alzheimer's Disease.
- New publicationDiagnosis, treatment, and management of rickets: a position statement from the Bone and Mineral Metabolism Group of the Italian Society of Pediatric Endocrinology and Diabetology.
- New publicationEffects of vitamin D supplementation on metabolic parameters, serum irisin and obesity values in women with subclinical hypothyroidism: a double-blind randomized controlled trial.
- New publicationVitamin D<sub>3</sub> Receptors and Metabolic Enzymes in Hen Reproductive Tissues.
- Regulatory approval
Approval: PARICALCITOL (NDA205917)
Objective event titles are shown unmodified; the event kind and significance line are derived from structured fields. Forefront AttentionEvent stream aggregating Europe PMC Regulatory filings ClinicalTrials.gov.